cas 274693-27-5, Ticagrelor | Articles data

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PROCESS FOR THE PREPARATION OF TICAGRELOR
The present invention relates to a process for the preparation of ticagrelor, which provides a product of high purity, in particular, with no detectable levels of Nnitrosmine impurities. The process comprises a first step of treating 2- [[(3aR,4S,6R,6aS)-6-[[5-amino-6-chloro-2-(propylthio)-4-pyrimidinyl]amino]tetrahydro-2,2-dimethyl-4H-cyclopenta-1,3-dioxol-4-yl]oxy]ethanol starting material with sodium nitrite, followed by acidic washing; in a second step, the 2-[[(3aR,4S,6R,6aS)-6-[7-chloro-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl]tetrahydro-2,2-dimethyl-4H- cyclopenta-1,3-dioxol-4-yl]oxy]ethanol obtained in the previous step is coupled with trans-(1 fl,2S)-2-(3,4-difluorophenyl)cyclopropylamine, and the reaction is followed by a first washing at basic pH a second washing at acidic pH; and in an third step, the compound obtained in the previous step is deprotected by treatment with mineral acid, followed by acidic washing.
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(2021/12/28)

Method for preparing ticagrelor
The present invention discloses a method for preparing ticagrelor. In the method, 4,6-dihalo-5-nitro-2-propylthiopyrimidine (II) as raw materials and a series of reactions of substitution, reduction,ring formation, substitution, deprotection, etc. are conducted to obtain the ticagrelor. The method has cheap and readily available raw materials, simple process conditions, convenient post-processing, high total yield, and is more suitable for industrial production.
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(2020/12/09)

Synthesis of ticagrelor analogues belonging to 1,2,3-triazolo[4,5-d]pyrimidines and study of their antiplatelet and antibacterial activity
Based on the recent observation that the antiplatelet agent ticagrelor and one of its metabolite exert bactericidal activity against gram-positive bacteria, a series of 1,2,3-triazolo[4,5-d]pyrimidines structurally related to ticagrelor were synthesized and examined as putative antiplatelet and antibacterial agents. The aim was to assess the possibility of dissociating the two biological properties and to find novel 1,2,3-triazolo[4,5-d]pyrimidines expressing antiplatelet activity and devoid of in vitro antibacterial activity. The new compounds synthesized were known metabolites of ticagrelor as well as structurally simplified analogues. Some of them were found to express antiplatelet activity and to lose the antibacterial activity, supporting the view that the two activities were not necessarily linked.
Goffin, Eric,Jacques, Nicolas,Lancellotti, Patrizio,Musumeci, Lucia,Nchimi, Alain,Pirotte, Bernard,Oury, Cécile
(2020/09/11)

Production process of ticagrelor fine product
The present invention discloses a production process of a ticagrelor fine product. The process comprises the steps of adopting 4,6-dichloro-5-amino-2-propylthiopyrimidine (IIa) and a compound (IIb) asstarting raw materials, and carrying out five processes including a substitution process I, a cyclization process, a substitution process II, a hydrolysis process and a refining process to finally obtain the ticagrelor fine product. The method provides a ticagrelor production process, uses cheap and easily available raw materials, has the advantages of low production cost, simple reaction conditions, convenient post-treatment, high yield and high product purity, and is more suitable for industrial production.
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(2020/12/09)

Synthesis method for ticagrelor
The invention discloses a synthesis method for ticagrelor. The synthesis method comprises the following steps: (a) allowing 6-halogenated-2-propylthio-8-azapurine serving as a raw material to react with (1R,2S)-2-(3,4-difluorophenyl)cyclopropylcarbamic acid tert-butyl ester in alkali and an organic solvent at a room temperature so as to obtain an intermediate (II); (b) dissolving the intermediate(II) and a compound (III) in an organic solvent at a room temperature, and carrying out a reaction under the action of triphenylphosphine and diethyl azodicarboxylate so as to obtain an intermediate (IV); and (c) deprotecting the intermediate (IV) under the action of acid so as to obtain ticagrelor (I). The method provided by the invention has the advantages of cheap and easily-available raw materials, low production cost, short reaction steps, mild reaction conditions, convenient post-treatment and high yield, and is more applicable to industrial production.
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(2020/12/09)

Preparation method of platelet aggregation inhibitor ticagrelor
The invention discloses a preparation method of platelet aggregation inhibitor ticagrelor, and belongs to the field of drug synthesis. According to the method, a compound 2 and a compound 3 are used as raw materials, substitution reaction, cyclization reaction, amination reaction and deprotection are sequentially carried out, a crude product is recrystallized by ethyl acetate and normal hexane toobtain the ticagrelor, and the purity of the ticagrelor is up to 99.5% or above. Compared with methods reported in existing literatures, the method has the advantages that the reaction route is obviously shortened, the process stability is high, use of toxic solvents and high-pollution reagents is avoided, and the method is relatively more environmentally friendly and suitable for large-scale production.
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(2020/11/12)

Preparation method of amorphous ticagrelor
The invention discloses a preparation method of amorphous ticagrelor, which comprises the steps of preparation of a ticagrelor crude product and preparation of amorphous ticagrelor. The preparation method has the advantages that: 1, a preparation technology of an amorphous ticagrelor product is simple and convenient, mild in technological condition and strong in operability; a single solvent can be used in the reaction for preparing the amorphous product at the same time; the solvent can be recycled for many times; less waste liquid and less pollution are generated; and the production cost islowered by 20-30% as compared with the production cost of the traditional preparation method at the same time; and 2, the solvents used are low boiling point volatile solvents; the product is easy todry to remove the solvents to meet ICH (International Conference on Harmonization) standard requirements in a drying procedure; and large-scale industrial production is facilitated.
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Paragraph 0019-0025

(2019/10/01)

Crystal form I of Ticagrelor Fumarateand its preparing method
The present invention relates to: a type I crystal which is a novel crystalline form of ticagrelor fumarate; and a method for manufacturing the same. The type I crystal according to the present invention is very hygroscopic and is very advantageous for storage and distribution, thereby having an advantage that it is also very advantageous for storage and distribution of formulations made by using the same. In addition, the type I crystal according to the present invention exhibits a spherical shape and has a similar size of crystalline, thereby exhibiting very good physical properties to make formulations such as reducing sticking phenomenon during tableting, being easily mixed with other additives, and ensuring a content uniformity. On the other hand, a manufacturing method according to the present invention can manufacture the type I crystal having a high yield and purity with a simple process.COPYRIGHT KIPO 2020
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Paragraph 0036-0037

(2019/12/10)

A method for the preparation of intermediate [...]
The invention relates to a preparation method of a ticagrelor intermediate, specifically to a preparation method of a compound or its salt which is used as a medical intermediate and is as shown in the formula (2) and an application of the compound (2) or its salt in preparation of a triazolopyrimidine compound. According to the method provided by the invention, synthetic process is simple and reaction post-treatment is greatly simplified. By the technical scheme for preparation of the triazolopyrimidine compound, the whole synthetic process is easy to carry out, and yield of the intermediate for preparation of the triazolopyrimidine compound is greatly increased. The preparation method is especially suitable for industrial production.
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(2019/01/14)

Preparation method of ticagrelor
The invention relates to synthesis of a pharmaceutical compound and in particular relates to a preparation method of ticagrelor. The method disclosed by the invention comprises the steps as follows: step 1, synthesizing an intermediate Im-1; step 2, synthesizing an intermediate Im-2; step 3, synthesizing an intermediate Im-3; step 4, synthesizing a crude product Im-4; and step 5, carrying out refining, namely recrystallizing the crude product of ticagrelor by using 10-15 times of mixed solution of dichloromethane and tertiary butanol, and carrying out washing, filtering and drying to obtain arefined product of ticagrelor, wherein the volume ratio of dichloromethane to tertiary butanol in the mixed solution of dichloromethane and tertiary butanol is 1:(2-3).
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(2018/08/28)

Synthesizing method of ticagrelor
The invention relates to synthesis of a medicine compound, in particular to a synthesizing method of ticagrelor. The synthesizing method comprises the following steps of S1, synthesizing an intermediate Im-1; S2, synthesizing an intermediate Im-2; S3, synthesizing an intermediate Im-3; S4, synthesizing a crude product Im-4; S5, refining: recrystallizing a crude product of the ticagrelor by a mixedsolution of dichloromethane and tertiary butanol, washing, filtering, and drying, so as to obtain a refined product of the ticagrelor.
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(2018/07/30)

Preparation method of high-purity ticagrelor
The invention discloses a preparation method of high-purity ticagrelor. The preparation method comprises the following steps: preparing intermediates TG-1, TG-2, TG-3 and TG-4; and refining the ticagrelor. According to the preparation method, matching of reactants is adjusted, the reaction time and temperature are optimized, and a post-processing manner is adopted; a specific catalyst and a specific devitrification solvent are selected, so that the reaction efficiency of the intermediates is improved, the reaction time is shortened and the purity of the intermediates is improved; after a crudeproduct of the ticagrelor is obtained, different devitrification solvents and a staged crystallization process are adopted to obtain the ticagrelor with high purity, so that the production cost is reduced, the advantages of being high efficiency and clean in production are achieved, and the operability is strong; and the purity of the obtained ticagrelor product is not lower than 99.8%, and no single impurity exceeds 0.06%.
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(2019/01/06)

Preparation method of ticagrelor
The invention provides a preparation method of ticagrelor. According to the preparation method, a compound shown in a formula (i) is used as a raw material, and the ticagrelor is prepared by means ofcondensation, ring formation, condensation and deprotection; the preparation method is simple and convenient in technological process and easy to operate, thus being suitable for large-scale production; furthermore, the preparation method provided by the invention is mild in synthesis conditions, high in product yield and good in product purity, can effectively control the preparation cost, and reduces the medication burden of patients.
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(2019/04/30)

For the improvement of the [...] intermediates preparation method
The invention relates to an improved preparation method for the intermediate 4, 6-dihalogen-2-(propythio)pyrimidine-5-amine used for preparing the anticoagulation drug ticagrelor, and application of the intermediate in preparation of ticagrelor. By use of a phase transfer reagent, the method reduces the halogenating reagent consumption and emission and treatment of toxic substances. Also, the obtained product has high yield and good purity. Thus, the method is a greener and more economical preparation method more suitable for industrial application.
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(2018/02/04)

A [...] preparation method and intermediate
The present invention relates to a preparation method and an intermediate of ticagrelor. The preparation method comprises that a compound represented by a formula VIII and a compound represented by a formula VII or a salt thereof as raw materials to carry out a reaction, and the obtained intermediate is subjected to acetonylidene protection group removing, optionally substituted azobenzene protection group removing, and cyclization, and then reacts with a compound represented by a formula II or a salt thereof to prepare the ticagrelor. The preparation method of the present invention has characteristics of short step, high total yield, mild reaction conditions and simple post-treatment, and is suitable for industrial production.
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(2018/04/21)

Ticagrelor preparation method
The invention discloses a ticagrelor preparation method. Compared with existing routes, the method has the advantages of great increase of the reaction yield and great reduction of the production costdue to step shortening and bare hydroxyl group protection.
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Paragraph 0062; 0071-0073; 0088

(2018/11/03)

For [...] novel intermediate and its preparation method
The invention discloses a novel intermediate of ticagrelor, i.e., a compound represented by a formula (I), and a preparation method thereof. The preparation method for the compound represented by the formula (I) comprises a step of subjecting a compound represented by a formula (II) or a proper salt of the compound represented by the formula (II) and a compound represented by a formula (III) to a substitution reaction, wherein R in the formulas represents substituted or unsubstituted benzyl and benzoyl groups. The invention further discloses a preparation method for a ticagrelor compound represented by a formula (A) from the novel intermediate, i.e., the compound represented by the formula (I). The method for preparing ticagrelor from the novel intermediate has the advantages of short reaction time, easy and convenient post-treatment, high yield and high product purity.
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(2018/06/21)

NOVEL CRYSTALLINE FORM OF TICAGRELOR
The present invention relates to novel crystalline form, Form N of Ticagrelor and process for preparation of the same.
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Page/Page column 7

(2018/10/25)

A method for preparing for standard auspicious Luo river
The invention provides a preparation method for ticagrelor. The method comprises the reaction steps shown in the specification, and concretely comprises the following steps: (1) in the presence of an alkali, coupling a formula II compound with a formula III compound to generate a formula IV compound; (2) under an acidic condition, performing reduction and deprotection on the formula IV compound, so as to obtain a formula V compound; (3) performing diazotization and ring closure on the formula V compound, so as to generate a formula VI compound; and (4) under an alkali condition, coupling the formula VI compound with a formula VII compound, so as to obtain ticagrelor shown as a formula I. The method is mild in reaction conditions and simple in post-treatment, is capable of effectively controlling impurities and improving the optical purity of the product, is suitable for industrialized production and has relatively large application value.
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(2017/07/14)

A for the card Grey crystal form and its preparation method
The invention relates to a crystal form of an anti-thrombotic medicament ticagrelor, a preparation method for the crystal form, a medicinal composition containing the crystal form and an application of the crystal form to the preparation of the anti-thrombotic medicines. The crystal form of ticagrelor is a crystal form A with a structure as shown below. A Cu-Kalpha radiation mode is adopted. An X-ray powder diffraction pattern of the crystal form A, represented by an angle 2Theta has characteristic diffraction peaks at the following positions: 6.2+/-0.2 degrees, 11.5+/-0.2 degrees, 15.0+/-0.2 degrees and 20.6+/-0.2 degrees. The crystal form A of ticagrelor has the advantages of convenience of the preparation method, high stability and preparation adaptability and the like, so that the crystal form A is industrially practical.
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(2017/08/25)

Process suitable for ticagrelor industrial production
The invention discloses a process suitable for ticagrelor industrial production, which comprises the following steps of step 1, using tartrate of a compound III as a starting material, using sulfolane and diisopropylethylamine as a solvent, and reacting for 3 hours at 105-108DEG C; step 2, using mild tetrahydrofuran and oxalic acid dihydrate as a solvent, and using diisopropylethylamine to replace triethylamine in an original study patent, thereby reducing reaction time, and reducing a potential genotoxicity risk of the triethylamine; and step 3, an optimized reaction temperature in the invention is -5-0DEG C; using methyl tertiary butyl ether to replace ethyl acetate as an extraction agent; using an ethyl acetate and cyclohexane mixing solvent to replace a methyl tertiary butyl ether and cyclohexane mixing solvent to purify a finished product; wherein polarity of the ethyl acetate is greater than that of the methyl tertiary butyl ether; using the methyl tertiary butyl ether during extraction and using the ethyl acetate during purification may remove impurities and improve purity to the greatest extend.
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(2017/07/20)

A [...] crystallization and containing the pharmaceutical compositions
The invention provides a ticagrelor crystal and a medicinal composition comprising the same. The purity of the ticagrelor crystal is greater than 99 percent, and an impurity N is less than 0.1 percent. The crystal is prepared by adopting a one-pot method and is obtained by adopting a further crystal refining method. By adopting the methods, the ticagrelor with the purity being obviously improved can be obtained, and the raw material and medicinal composition with excellent quality are further acquired.
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(2017/10/06)

Improved method for preparing ticagrelor
The invention discloses an improved method for preparing ticagrelor. The method comprises the following steps of conducting an acid binding agent reaction kettle heating reaction on ethylene glycol, FTG-SM1, FTG-SM2 and triethylamine; then conducting extracting, concentrating and methyl alcohol/water salify crystallization to obtain TFG-3; conducting diazotization, loop closing, an FTG-SM3 substitution reaction and acidification protecting group separation continuous reaction on FTG-3 in methylbenzene to obtain a coarse product of ticagrelor; conducting recrystallization on the coarse product to obtain a finished product. According to the improved method for preparing ticagrelor, cheap reagents and raw materials are utilized, and the technology cost is lowered; regarding refining of a middle body FTG-1, a methyl alcohol/water system is adopted, and the content of related substances is effectively controlled; by conducting three-step reaction continuous compounding, solvents are saved, the operation is simplified, and the technology cycle is shortened; the dose of the solvent is less, the pollution is lowered, and the method is environmentally friendly. The improved method for preparing ticagrelor is simple and safe in operation condition and simple in after-treatment, the product is easy to obtain, high in yield and high in purity. The technology cost is low, and the improved method is suitable for industrial large-scale production.
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(2017/12/06)

Synthesis method of ticagrelor
The invention discloses a synthesis method of ticagrelor. The method comprises the steps of 1, adding thiourea and alkali to a solution where bi-aminomalonic acid diethyl ester is dissolved, wherein the mole ratio of bi-aminomalonic acid diethyl ester, thiourea and alkali is 1:(1.0-1.5):(2-2.3), and performing a reaction under the protection of nitrogen at 25-100 DEG C for 5-72 h to obtain a compound 2; 2, adding bromopropane to a solution where the compound 2 is dissolved at -2 DEG C-2 DEG C, and conducting stirring at 25-50 DEG C for 2-72 h to obtain a compound 3; 3, adding organic alkali and a chloride agent to the compound 3, raising the temperature to 20-75 DEG C, and performing a reaction for 3-8 h to obtain a compound 4; 4, synthesizing ticagrelor, wherein the compound ticagrelor is obtained by conducting substitution, loop closing, substitution and a hydrolysis reaction on the compound 4 (4,6-dichloro-2-propylthiopyrimidine-5-amine), the operation steps are greatly simplified, and the yield is drastically increased. The synthesis method of ticagrelor is simple in operation and high in reaction yield.
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(2017/09/26)

Preparation process for ticagrelor
The invention discloses a preparation process for ticagrelor. By adding organic weak base to neutralize acetic acid and acetic acid generated from degrading of ethyl acetate in the process of preparing the ticagrelor, oxide impurities generated in ticagrelor final products are avoided; a test proves that oxide impurity sulphone and sulfoxide in original final products are removed effectively; and according to the preparation process, the product quality is improved greatly, and the process is simple, feasible and suitable for industrialized production.
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(2017/08/28)

Method of synthesis of Ticagrelor
The invention provides a method of synthesis of Ticagrelor (1). The method comprises the steps that firstly a compound (2) and a compound (3) are subject to a substitution reaction to prepare a compound (4); the compound (4) after being subject to the substitution reaction of sulfur alcohol is prepared into a compound (5); the compound (5) and a compound (6) after being subject to the substitution reaction of palladium catalyst non-symmetric terpene propyl alcohol is prepared into a compound (7); the compound (7) after being subject to non-asymmetric di-hydroxylation reaction is prepared into a compound (8); the compound (8) after being subject to di-hydroxy protective reaction is prepared into a compound (9); the compound (9) after being subject to the substitution reaction of hydroxyl is prepared into a compound (10); finally Ticagrelor (1) is obtained by subjecting the compound (10) to the deprotection reaction of hydroxyl. The method of synthesis of Ticagrelor is simple to operate, low in production cost, high in product quality, and suitable for industrial production. (The picture file is appended to the application.).
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(2017/10/26)

Method for synthesizing compound ticagrelor and synthesized intermediate thereby
The invention discloses a method for synthesizing a compound ticagrelor and a synthesized intermediate thereby. The method comprises the following steps: carrying out a substitution reaction between a compound (2) and a compound (3) to prepare a compound (4); carrying out a reduction reaction on the compound (4) to prepare a compound (5); carrying out a chlorination reaction on the compound (5) to prepare a compound (6); carrying out a substitution reaction between the compound (6) and a compound (7) to prepare a compound (8); and finally, carrying out a hydroxyl deprotection reaction on the compound (8), thereby obtaining the ticagrelor (1). The reaction formulas are as shown in the specification. The invention provides a novel method for synthesizing ticagrelor. The synthetic method has the advantages of novel technical route, simple and convenient operation, high synthesis yield, high product purity, cheap and readily available raw materials and the like, and is suitable for industrialized production. Meanwhile, the synthesized ticagrelor intermediate provides a novel intermediate raw material for preparation of the ticagrelor.
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Paragraph 0008; 0009; 0053; 0054; 0064; 0072; 0080

(2018/03/24)

Preparation method of ticagrelor
The invention discloses a preparation method of ticagrelor. According to the preparation method disclosed by the invention, a compound II reacts with thionyl chloride and ammonium thiocyanate to prepare a compound III; the compound III is subjected to substitution to prepare a compound IV; the compound IV is condensed and hydrolyzed under the acid condition to generate a compound V; finally, by reduction, a final product ticagrelor (I) is prepared. The preparation method is low in cost of raw materials used for the reaction, mild in reaction condition, and simple and convenient to operate; a process route is shortened; total yield is improved; the preparation method is suitable for industrial production.
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(2017/08/31)

CRYSTALLINE FORM OF TICAGRELOR
A crystalline form of ticagrelor, designated as Form-AM, has a defined interplanar spacing as illustrated by Figure 1.
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Page/Page column 9; 10

(2017/08/01)

A method for preparing for standard auspicious Luo river
The invention provides a ticagrelor preparation method. The method using a compound of structural formula 2 as an initiator comprises the following steps: 1, reacting the compound of structural formula 2 with di-tert-butyl pyrocarbonate to obtain a compound of structural formula 3; 2, reacting the compound of structural formula 3 with a compound of structural formula 4 to obtain a compound of structural formula 5; 3, reacting the compound of structural formula 5 with a compound of structural formula 6 to obtain a compound of structural formula 7; and 4, carrying out nitro group reduction on the compound of structural formula 7, cyclizing, and carrying out protective group removal to obtain ticagrelor of structural formula 1.
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Paragraph 0124-0125

(2017/08/25)

A method for preparing for card Grey
The invention provides a preparation method of ticagrelor. Compared with an existing route, the method has the steps shortened, so that the reaction yield is substantially improved, and the cost of production is greatly reduced. The ticagrelor synthetic method shown in the route provided by the invention is not described in disclosed literature.
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(2019/02/04)

SOLID FORM OF INTERMEDIATE OF TICAGRELOR
A process for the preparation of a solid form of a compound of formula (VII) (Formula (VII)) comprises coupling(1R,2S)-2-(3,4-difluorophenyl)cyclopropanamine (R)-Mandelic acid of Formula (VI) with (2-[[(3a R,4S,6R,6aS)-6-[7-chloro-5-(propylthio)-3H-1,2,3-triazolo[4,5-d]pyrimidin-3-yl]-2,2- dimethyltetrahydro-3aH-cyclopenta[d[[1,3]dioxol-4-yl]oxy]-1-ethanol) of formula (V) in the presence of a suitable base and a first a suitable solvent at a suitable temperature to form 2- [[(3aR,4S,6R,6aS)-6-[7-[[(1R,2S)-2-(3,4-difluorophenyl)cyclopropyl]amino]-5-(propylthio)-3H-1,2,3- triazolo[4,5-d]pyrimidin-3-yl]-2,2-dimethyltetrahydro-3aH-cyclopenta[d][1,3]dioxol-4-yl]oxy]-1- ethanol of formula (VI)I; and isolating the compound of formula (VII) using a second suitable solvent so as to produce the compound of formula (VII) in solid form. A process for preparing Ticagrelor of formula (I) or a salt thereof (Formula (I)) comprises the conversion of a compound of formula (VII) in a solid form either as free base or as an acid addition salts thereof, into a compound of formula (I).
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(2016/03/22)

Synthesis method for ticagrelor
The invention discloses a synthesis method for ticagrelor.The synthesis method includes the following steps that 1, a compound I and a compound II are subjected to a coupling reaction under alkali existence, and then a compound III is obtained through extraction and recrystallization; 2, the compound III is subjected to a diazo reaction, extraction and washing, and a compound IV is obtained; 3, the compound IV is coupled with a compound V under the alkaline condition, and a compound VI is obtained through extraction, washing and concentration; 4, the compound VI is subjected to a deprotection reaction under the acid condition, and a compound VII, namely, ticagrelor is obtained through extraction and recrystallization.A solvent selected in the preparation method is free of toxins and environmentally friendly, the impurity removal process is simple, cost is low, and the yield and purity of the obtained product are both high.
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(2016/10/17)

PROCESSES FOR THE PREPARATION OF TICAGRELOR AND ITS INTERMEDIATES
The present invention provides a process for the preparation of ticagrelor. The present invention further provides compounds of Formula IV, Formula V, Formula VI, Formula VIa, Formula VII, and Formula VIII, processes for their preparation, and their use for the preparation of ticagrelor.
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(2016/04/20)

Method for preparing ticagrelor and novel intermediate used therefor
The present invention relates to a novel synthesis method for Ticagrelor, represented by chemical formula 1, (1S,2S,3R,5S)-3-[7-[(1R,2S)-2-(3,4-difluorophenyl)cyclopropylamino]-5-(propylthio)-3H-[1,2,3]triazolo[4,5-d]pyrimidin-3-yl]-5-(2-hydroxyethoxy)cyclopentane-1,2-diol, and novel intermediates for use in the novel synthesis method. According to the present invention, Ticagrelor can be easily synthesized from the novel intermediates.COPYRIGHT KIPO 2016
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(2017/01/31)

Preparation method of Ticagrelor and intermediates thereof
Disclosed in the present invention is a method for preparing Ticagrelor (I), comprising the following steps: a cyclization reaction of 5-amino-1,4-di-substituted-1,2,3-triazole (II) and dialkyl carbonate (HI), to obtain 9-substituted-2,6-dihydroxy-8-azapurine (IV); chlorination of intermediate (IV), to obtain 9-substituted-2,6-dichloro-8-azapurine (V); an amination reaction of intermediate (V) and trans-(1R,2S)-2-(3,4-difluorophenyl)cyclopropanamine (VI) generates 9-substituted-6-amino-substituted-2-chloro-8-azapurine (VII); and a propanethiolation reaction of intermediate (VII) and propanethiol (VIII), to obtain Ticagrelor (I). The preparation method is simple in process, has a high chemical and chiral purity and provides a new preparation method for industrializing Ticagrelor. In addition, also provided in the present invention are intermediates of Ticagrelor and a preparation method thereof, wherein raw materials of the preparation method are easily available, the conditions thereof are mild, and the yield thereof is high.
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(2016/05/10)

PREPARATION OF TICAGRELOR
The present application relate to processes for preparing Ticagrelor and to intermediates that are useful in the processes.
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(2016/01/25)

AN IMPROVED PROCESS FOR PREPARATION OF TICAGRELOR AND INTERMEDIATES THEREOF
An improved, industrially viable, environment friendly and economically significant process for preparation of Ticagrelor is disclosed alongwith novel intermediates for the Ticagrelor synthesis.
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(2016/09/22)

INTERMEDIATE OF TICAGRELOR AND PREPARATION METHOD THEREFOR, AND PREPARATION METHOD FOR TICAGRELOR
Disclosed are intermediates of Ticagrelor and a preparation method therefor, and a preparation method for Ticagrelor. Specifically, disclosed is an intermediate, namely, a compound of Formula (VI), for preparing Ticagrelor. Further disclosed is a method for preparing the intermediate and a method for preparing Ticagrelor by using the intermediate. Ticagrelor is prepared by using the intermediate, so that the synthesis process is simple, and a defect that long reaction times under high temperature that are required in the existing methods are avoided. The method is suitable for mass production in industry, energy consumption is reduced, pollution of the environment is reduced, and discharge of waste is reduced.
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(2016/05/02)

PREPARATION OF TICAGRELOR
Provided are processes for preparing Ticagrelor and its intermediates that are useful in the processes. Also provided are salts of Ticagrelor, their processes and solid dispersion of Ticagrelor having Ticagrelor in amorphous form.
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(2015/03/16)

PROCESS FOR THE PREPARATION OF TRIAZOLO[4,5-D] PYRIMIDINE CYCLOPENTANE COMPOUNDS
The present invention relates to a process for the preparation of triazolo[4,5-d] pyrimidine cyclopentane compounds of formula (I), and pharmaceutically acceptable salts thereof. The invention also provides novel compounds that can be used as intermediates in the process for preparing triazolo[4,5-d] pyrimidine cyclopentane compounds. The process and the intermediates are particularly useful for the preparation of ticagrelor and pharmaceutically acceptable salts thereof.
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Page/Page column 27; 28

(2016/06/28)

PROCESS FOR PREPARING TRIAZOLE PYRIMIDINE COMPOUNDS AND INTERMEDIATES THEREOF
A method is disclosed for preparing Ticagrelor using the compounds as represented by intermediates of formula (2), formula (1-b), formula (1-c), formula (1-d) and formula (1-e), wherein the definition of R is as described in the description, and also disclosed is a method for preparing the intermediate of formula (2) and the use thereof in the preparation of Ticagrelor.
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Paragraph 0118-0119

(2015/11/30)

NOVEL PROCESSES FOR PREPARING TRIAZOLO [4,5-D]- PYRIMIDINES, INCLUDING TICAGRELOR, VIANEW INTERMEDIATES AND NEW ROUTE OF SYNTHESIS.
The present invention relates to novel processes for preparing triazolo [4,5-d] pyrimidines, including Ticagrelor, via new intermediates and new routes of synthesis. The synthesis begins with readily available and inexpensive starting material such as 5-nitro-2,4,6-trichloropyrimidine and leads to series of novel intermediates, which are commercially viable and industrially advantageous (solid intermediates, high yields and convenient experimental condition) for the preparation of highly pure Ticagrelor.
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(2015/11/10)

PROCESS FOR PREPARATION OF TICAGRELOR
A process of the preparation of amorphous ticagrelor and a process of preparation of dimethyl formamide solvate of ticagrelor are provided.
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Page/Page column 22

(2015/11/16)

A PRODUCTION METHOD AND A NEW CRYSTALLINE FORM OF AN INTERMEDIATE OF SYNTHESIS OF TICAGRELOR
The invention relates to preparation of ticagrelor of formula I and comprises a reaction of a compound of formula IV with a deprotection agent in a solvent to a compound of formula V, which is advantageously isolated by crystallization and subsequently used for the preparation of ticagrelor. The substituent R in formulae IV and V is CH2CH2OH, CH2COOH, or CH2COOR1; R1 is a branched or unbranched R1-C4 alkyl; and X is NH2, NO2f or NHCHO.
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Page/Page column 19

(2015/05/26)

A PROCESS FOR PREPARATION OF TICAGRELOR AND INTERMEDIATES THEREOF
An improved process for the preparation of ticagrelor and its intermediates thereof; wherein the said process substantially eliminates the potential impurities.
-
(2014/07/21)

SELECTIVE ALKYLATION OF CYCLOPENTYL ALCOHOLS
There is described an oxygen-selective alkylation reaction of an amino alcohol of general formula (I) with a compound of general formula (IV) to produce an O-alkylated compound of general formula (II), avoiding the need to protect the amino group of the starting compound, according to the scheme. There is also described a process for the preparation of allosteric antagonists of ADP receptors, in particular Ticagrelor, or of intermediates useful for their preparation, which uses the oxygen-selective alkylation reaction.
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Page/Page column 15

(2014/10/15)

METHOD FOR THE PREPARATION OF TICAGRELOR AND INTERMEDIATES SUITABLE THEREFORE
A method for the preparation of ticagrelor of formula I, wherein the key reaction of the entire synthesis is condensation of an amino cyclopentane diol with pyrimidine, providing the isolated intermediate of formula IV. The amino cyclopentane diol is used for the reaction with pyrimidine without any protecting group on the hydroxyls in positions 1 and 2. Using the compound without a protecting group eliminates the necessity of deprotection in the subsequent synthetic steps.
-
(2014/09/29)

TICAGRELOR ADDUCTS WITH DIVALENT METAL SALTS
The present invention relates to amorphous adducts of ticagrelor with divalent metal salts useful in the treatment or prevention of arterial thrombotic complications in patients with coronary artery, cerebrovascular or peripheral vascular disease.
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Page/Page column 12

(2014/01/18)

TICAGRELOR SOLID DISPERSION
The present invention provides a novel amorphous solid dispersion of ticagrelor in combination with a pharmaceutically acceptable carrier, process for its preparation and pharmaceutical compositions comprising it.
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Page/Page column 7

(2014/08/19)

Chemical Properties

Appearance/Colour :white powder
Boiling Point: 777.551 °C at 760 mmHg
Flash Point:424.048 °C
Density: 1.676 g/cm³
Solubility:Methanol (Slightly)
Storage Temp.:Keep in dark place,Inert atmosphere,Store in freezer, under -20°C
Refractive Index: 1.744
PKA: 13.26±0.70(Predicted)
PSA: 163.74000
LogP: 2.08670

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Chemical Properties

Appearance/Colour :white powder

Boiling Point: 777.551 °C at 760 mmHg

Flash Point:424.048 °C

Density: 1.676 g/cm³

Solubility:Methanol (Slightly)

Storage Temp.:Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

Refractive Index: 1.744

PKA: 13.26±0.70(Predicted)

PSA: 163.74000

LogP: 2.08670

Global suppliers and manufacturers of 274693-27-5total 260 suppliers on LookChem

Article Database

274693-27-5

Articles about 274693-27-5Total 62 be found

More Articles about upstream products of 274693-27-5

More Articles about downstream products of 274693-27-5

Chemical Properties

Appearance/Colour :white powder

Boiling Point: 777.551 °C at 760 mmHg

Flash Point:424.048 °C

Density: 1.676 g/cm3

Solubility:Methanol (Slightly)

Storage Temp.:Keep in dark place,Inert atmosphere,Store in freezer, under -20°C

Refractive Index: 1.744

PKA: 13.26±0.70(Predicted)

PSA: 163.74000

LogP: 2.08670

Global suppliers and manufacturers of 274693-27-5total 260 suppliers on LookChem

Density: 1.676 g/cm³