- Preparation method of hypoglycemic drug linagliptin intermediate
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The invention provides a preparation method of a hypoglycemic drug linagliptin intermediate, wherein the method comprises the steps: in the presence of a catalyst and an organic solvent, carrying out condensation reaction on o-aminoacetophenone (1) and 2-chloroacetamide (2) to obtain an intermediate II; carrying out condensation, bromination, substitution and other reactions on 4-(methylamino)-1H-imidazol-5-carboxamide (3) to generate an intermediate III; and finally, carrying out alkylation reaction on the intermediate II and the intermediate III to generate an intermediate I. According to the preparation method, generation of side reactions are avoided. Moreover, the reaction cost is saved, the operation conditions are mild, the yield is high, the post-treatment is simple, and the method is suitable for industrial large-scale production.
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- Novel preparation process of linagliptin
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The invention discloses a novel preparation process of linagliptin. 8-bromo-3-methyl xanthine (SM1) is used as an initial raw material, DMF is used as a solvent and reacts with 1-bromo-2-butyne (SM2)under the alkaline condition to obtain an intermediate I, then the intermediate I reacts with 2-chloromethyl-4-methyl quinazol (SM3) under the solvent system to obtain an intermediate II, the intermediate II and (R) 3-aminopiperidine dihydrochloride (SM4) are subjected to a substitution reaction, and finally anti-type 2 diabetes drug linagliptin (I) is prepared. By adopting a one-pot method, the method has the advantages that the raw material cost is low, the yield is high, the post-treatment operation of each step of chemical reaction in multi-step reaction is reduced, the production period is greatly shortened, few impurities are generated in the reaction, the product quality is high, the use amount of chemical reagents is relatively reduced, and the method is relatively green and environment-friendly, and is beneficial to industrial production.
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- Novel preparation process of linagliptin
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The invention discloses a novel preparation process of linagliptin. 8-bromine-3-methyl xanthine (SM1) is used as an initial raw material, DMF is used as a solvent to react with 1-bromine-2-butyne (SM2) under an alkaline condition to obtain an intermediate I, then the intermediate I reacts with 2-chloromethyl-4-methyl quinazol (SM3) under the solvent system to obtain an intermediate II, and the solvent system reacts with (R)-3-Boc-aminopiperidine (SM4) under the alkaline condition to obtain an intermediate III; and the protecting group is dissociated by using acid to obtain the linagliptin (I) for resisting type 2 diabetes mellitus. By adopting a one-pot method, the method has the advantages that the raw material cost is low, the yield is high, the post-treatment operation of each step of chemical reaction in multi-step reaction is reduced, the production period is greatly shortened, few impurities are generated in the reaction, the product quality is high, the use amount of chemical reagents is relatively reduced, and the method is relatively green and environment-friendly, and is beneficial to industrial production.
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- Preparation method of linagliptin
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The invention relates to a preparation method of linagliptin. The method comprises the following steps: taking a raw material I, namely 2-chloromethyl-4-methylquinazoline, and a raw material II, namely 8-bromo-7-(2-butynyl)-3-methyl-1H-purine-2, 6 (3H, 7H)-diketone as raw materials, performing reaction to obtain an intermediate III, namely 8-bromo-7-(2-butynyl)-3,7-dihydro-3-methyl-1-[(4-methylquinazoline-2-yl)-methyl]-1H-purine-2, 6-diketone, and performing reaction with a raw material IV: (R)-3-aminopiperidine hydrochloride to prepare a target product. In the reaction process, a protecting group does not need to be added, the step of removing the protecting group after the reaction is completed is omitted, and the generation of reaction byproducts in the process of removing the protecting group is reduced. The solvents used in the method are beneficial to recycling, low in price, environment-friendly, green and environmentally friendly, and the obtained product is high in yield, high in purity and suitable for large-scale production.
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Paragraph 0009; 0032-0033; 0036-0037
(2021/06/21)
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- Linagliptin intermediate compound V
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The invention belongs to the field of pharmaceutical chemicals, and provides a linagliptin intermediate compound V and an important intermediate for synthesizing linagliptin by using the intermediateV. The method solves the problems of self-coupling of linagliptin intermediates and generation of large impurities in the prior art, and the synthesized novel intermediate compound V has the advantages of high yield, simple operation, significantly reduced production cost, and suitableness for industrial production.
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- Linagliptin intermediate compound IV
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The invention belongs to the field of pharmaceutical chemicals, and discloses a linagliptin intermediate IV and a novel route for synthesizing an important linagliptin intermediate from the linagliptin intermediate IV. The linagliptin intermediate IV synthesized in the invention has the advantages of high yield, simple operation, substantial reduction of production cost, suitableness for industrial production; and the synthesis route solves the problems of self-coupling of linagliptin intermediates and generation of large impurities in the prior art.
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- Xanthine compound, preparation method and applications thereof
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The invention belongs to the technical field of medicinal chemistry, and particularly relates to a new compound I (represented by a formula I), a preparation method and applications thereof. The invention relates to an important application of the new compound I, ie., a method for synthesizing a compound III capable of being used for treating type II diabetes mellitus by taking the compound I as araw material, wherein the method is high in conversion rate, simple in process and mild in reaction condition, provides an economic and environment-friendly route for preparation of the compound III,and has the advantages of being high in yield, good in purity, easy and convenient to operate, low in cost and suitable for industrial production compared with the method for preparing the compound III through linagliptin in the prior art. The compound I of the invention is a solid and is easy to store and purify, and the preparation route of the compound I is mild in reaction condition and simple to operate.
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Paragraph 0053-0064
(2020/04/01)
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- Route for synthesizing diabetes medicine linagliptin
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The invention relates to synthesis of a diabetes medicine linagliptin and particularly relates to a new preparation method for 1-[(4-methylquinazoline-2-yl)methyl]-3-methyl-7-(2-butyne-1-yl)-8-bromo-xanthine.
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- PROCESS AND INTERMEDIATES FOR THE PREPARATION OF BOC-LINAGLIPTIN
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This invention relates to novel processes for the synthesis of Linagliptin, the pharmaceutically active ingredient, and the key intermediate thereof, BOC-Linagliptin. (I) The processes are performed via new intermediate compounds of Formula (5) and Formula (3).
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Page/Page column 8; 9
(2020/03/02)
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- Industrial preparation method of linagliptin
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The invention belongs to the technical field of medicines, and particularly relates to an industrial preparation method of linagliptin. The preparation method comprises the following steps: adding N,N-dimethylacetamide into a reaction kettle, sequentially adding 8-bromo-7-(2-butyne)-3-methylxanthine, 2-chloromethyl-4-methylquinazoline, anhydrous sodium carbonate, anhydrous potassium carbonate andmethyl tert-butyl ether, and sequentially heating, cooling, stirring, filtering, carrying out HPLC monitoring and the like to obtain intermediates I and II, thereby finally obtaining linagliptin. Theindustrial preparation method of linagliptin provided by the invention is simple, high in intermediate purity, low in environmental pollution and low in cost, and meets the requirements of industrialmedicinal products.
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Paragraph 0040-0043; 0047-0050; 0054-0057; 0061-0064
(2020/02/08)
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- Linagliptin intermediate isomer impurity, preparation method and application thereof
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The invention relates to a linagliptin intermediate isomer, and provides a preparation method and purification method for obtaining a linagliptin intermediate isomer through a reaction of 4-methyl-2-halogenated methyl quinazoline and 8-bromo-3,7-dihydro-3-methyl-1H-purine-2,6-dione under the action of a silicon ester reagent and an alkali, wherein the preparation method has the advantages that theoperation is simple, the cost is low, and the purity of the obtained linagliptin intermediate isomer is high, and effective synthesis and purification of the linagliptin intermediate isomer lays a good foundation for quality research and control of linagliptin and an intermediate thereof.
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Paragraph 0026-0027
(2020/07/06)
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- Preparation method of linagliptin for treating diabetes
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The invention provides a preparation method of linagliptin. The preparation method comprises the following steps: in the presence of cuprous chloride catalyst, cyclizing 2-aminoacetophenone and a corresponding amide, which are taken as starting materials, to obtain a quinazoline compound; and in addition, sulfonyl is easier to remove compared with halogen, and is introduced into reaction raw materials, sulfonyl is easier to be replaced in subsequent substitution reaction, and a high-yield coupling product is obtained. The method has the advantages of short reaction route, high yield and few byproducts, lowers the production cost, and is beneficial to industrial production.
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Paragraph 0040-0042
(2020/01/03)
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- CRYSTALLINE LINAGLIPTIN INTERMEDIATE AND PROCESS FOR PREPARATION OF LINAGLIPTIN
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The present invention provides novel crystalline forms B1 and B2 of linagliptin intermediate of structural formula V and methods for production of novel crystalline form of linagliptin intermediate represented by the following structural formula V.
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Page/Page column 7; 8
(2019/04/26)
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- Industrial production method of linagliptin
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The invention provides an industrial production method of linagliptin. The method includes: adding In accordance with the molar ratio of 8-bromo-7-(2-butyne)-3-methylxanthine and 2-chloromethyl-4-methyl quinazoline into a dipolar aprotic organic solvent according to a mole ratio, then adding alkali and potassium iodide, performing crystallization, and conducting filtering and drying to obtain an intermediate I; adding the intermediate I and in accordance with the molar ratio (R)-3-t-butyloxycarborylamino piperidine into the dipolar aprotic organic solvent according to a mole ratio, then adding alkali, performing crystallization, and conducting filtration washing to remove inorganic salt, reducing pressure and removing the solvent to obtain a crude product, and then carrying out crystallization by methanol and isopropanol to obtain an intermediate II; and adding the intermediate II and a deprotection reagent into a reaction solvent according to a volume ratio, performing crystallization to obtain a crude product, then conducting recrystallization with ethanol, and carrying out filtering and drying to obtain a linagliptin final product. The method provided by the invention can greatly shorten the production cycle, save the production cost, obtain intermediates with higher purity, and achieve better impurity removal effect. The method is safe and reliable, is simple and easy to operate, and has good repeatability.
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Paragraph 0016; 0017; 0018; 0019; 0027; 0028
(2017/06/02)
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- A as dipeptidyl peptidase -4 inhibitor compounds
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The invention relates to a compound as a dipeptidyl peptidase-4 (DPP-IV) inhibitor, which can be used for treating all symptoms or diseases that get benefits by inhibiting DPP-IV activity, such as type I and II diabetes, diabetes complications and other related diseases.
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Paragraph 0067; 0068; 0069; 0070; 0071
(2016/10/08)
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- Linagliptin impurity, and preparation method and application thereof
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The invention discloses a linagliptin impurity as shown in a formula (I) which is described in the specification, a preparation method for the linagliptin impurity and application of the linagliptin impurity as an impurity reference substance for inspection of substance related to linagliptin. As the linagliptin impurity is applied as a standard reference substance, linagliptin quality can be effectively controlled, and security risks of a drug can be reduced, so security and validity of the linagliptin preparation in clinical application can be guaranteed.
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Paragraph 0029; 0030; 0031
(2016/10/10)
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- A as dipeptidyl peptidase -4 inhibitor for the preparation of compounds of the
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The invention relates to a preparation method of a biguanide derivative as a dipeptidyl peptidase-4 inhibitor (DPP-IV). The biguanide derivative can be used for treating all symptoms or diseases benefited by inhibiting the activity of DPP-IV, for example type 1 and 2 diabetes, diabetic complication and other related diseases.
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Paragraph 0057; 0058
(2016/10/08)
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- Intermediate for preparing compound as dipeptidyl peptidase-4 inhibitor
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The present invention relates to an intermediate for preparing a compound as a dipeptidyl peptidase-4 inhibitor. The biguanide derivative can be used for the treatment of all conditions or disorders benefiting from inhibition of DPP-IV activity, such as type I and type II diabetes, diabetic complications and other related diseases.
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Paragraph 0061; 0062; 0063; 0064; 0065
(2016/10/08)
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- A preparation as dipeptidyl peptidase -4 inhibitors of the intermediate compounds
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The invention relates to an intermediate for preparing a compound as a dipeptidyl peptidase-4 inhibitor. Biguanide derivatives can be used for treating all symptoms or disorders benefiting due to inhibition of DPP-IV activity, such as type 1 diabetes and type 2 diabetes, diabetes complication and other related diseases.
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Paragraph 0055; 0060; 0061; 0062; 0063; 0064
(2016/10/09)
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- Synthesis and characterization of process-related impurities of antidiabetic drug linagliptin
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Linagliptin, a xanthine derivative, is a highly potent, selective, long-acting and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes. During the process development of linagliptin, five new process-related impurities were detected by high performance liquid chromatography (HPLC). All these impurities were identified, synthesized, and subsequently characterized by their respective spectral data (MS, HRMS, 1H-NMR, 13C-NMR and IR) as described in this article. The identification of these impurities should be useful for quality control and the validation of the analytical method in the manufacture of linagliptin.
- Huang, Yiwen,He, Xiaoqing,Wu, Taizhi,Zhang, Fuli
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- A method for preparing advantage Geleg sandbank (by machine translation)
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The invention discloses a method for preparing advantage Geleg sandbank, comprising the following steps: the tert-butoxy-carbonyl-Leigh geleg sandbank (g) is added to the methanol aqueous solution, the stirring is then started, in an inert atmosphere and heating to reflux of the reaction is carried out under the state, get advantage Geleg sandbank, wherein the reaction temperature is 25-50°C, the reaction time is 3-12h, tert-butoxy-carbonyl-Leigh geleg sandbank (g) with the weight proportion of the methanol water solution 100 : (400-550). Method for preparing advantage Geleg sandbank of this invention, is under the protection of inert gas and methanol aqueous solution Boc protecting group on the method, no longer need expensive trifluoro acetate-DCM Boc protecting group on the reaction, only use the cheap methanol-water systems can be, and after treatment is simple, and three suitable the reaction of acid-DCM system, generating a plurality of impurities, the after-treatment and purification process is extremely tedious. Furthermore, it is also possible to avoid the use of the strong acid intermediate (g) and row Gurley sandbank impurity such as in the breaking of amide linkage. (by machine translation)
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- Simple preparation method of high-purity linagliptin
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The invention relates to a simple preparation method of high-purity linagliptin. The method includes the steps of making 8-bromine-3-methyl xanthine and 1-bromo-2-butyne react, directly adding 2-chloromethyl-4-methylquinazoline without processing after reaction is completed, preparing a key intermediate 8-bromine-7-(2-butyne-1-yl)-3,7-dihydro-3-methyl-1-[(4-methyl-2-quinazolinyl)methyl]-1H-purine-2,6-diketone of linagliptin through a one-pot method, making the intermediate react with (R)-3-piperidinamine dihydrochloride after being filtered and separated to obtain a linagliptin solution, and obtaining a linagliptin pure product after processing the linagliptin solution. The key intermediate is prepared through the one-pot method, operation is convenient, and yield is increased; the key intermediate reacts with (R)-3-piperidinamine dihydrochloride after being separated, and therefore high-purity linagliptin is obtained, and the requirements for production and declaration of pharmaceutical enterprises are met to the maximum extent.
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- A method for synthesizing advantage Geleg sandbank (by machine translation)
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The invention discloses a method for synthesizing advantage Geleg sandbank, comprising the following steps : (1) the 8- [...] the 3 [...] methyl xanthine (a) and the 1 [...] -2 the butyne [...] (b) reaction, from the 3 [...] methyl -7 the [...] (2 the [...] butyne-l-yl) - 8 the [...] bromo-xanthine (c) ; (2) the 3 [...] methyl -7 the [...] (2 the [...] butyne-l-yl) - 8 the [...] bromo-xanthine (c) and 2 the [...] methyl -4 the methyl [...] quinazoline (d) reaction, to obtain the 1 [...] [(4 the [...] methyl quinazoline -2 the [...] ) methyl] - 3 the [...] methyl -7 the [...] (2 the [...] butyne -1 the [...] yl) - 8 the xanthine [...] (e) ; (3) to the 1 [...] [(4 the [...] methyl quinazoline -2 the [...] ) methyl] - 3 the [...] methyl -7 the [...] (2 the [...] butyne -1 the [...] yl) - 8 the xanthine [...] (e), (R) - 3 the ??Boc-amino piperidine (f), the potassium carbonate and acetonitrile added into the reactor, and they are uniformly mixed, under the state of the heating under reflux for reaction, the tert-butoxy-carbonyl-Leigh geleg sandbank (g) ; (4) the tert-butoxy-carbonyl-Leigh geleg sandbank (g) removing the protecting group Boc in aqueous solution of methanol, to obtain advantage Geleg sandbank. The synthetic method of this invention has no environmental pollution, high yield, no impurities. (by machine translation)
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- METHOD FOR PREPARING AN IMPORTANT INTERMEDIATE OF LINAGLIPTIN
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The present invention discloses an improved process for preparing an important intermediate of linagliptin. In particular, disclosed are a process for preparing a compound V which is an important intermediate of linagliptin and has the structure V, and an industrial process of preparing linagliptin having excellent chemical and optical purities, which is an inhibitor of dipeptidyl peptidase-4 (DPP-IV), from the compound V. The process employs a phase-transfer catalyst, is high in yield, easy and simple to handle, environmentally friendly, suitable for industrial mass production, and can be implemented by a “one-pot process”.
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- PROCESS FOR THE PREPARATION OF LINAGLIPTIN AND AN INTERMEDIATE THEREOF
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The present invention provides an improved process for the preparation of linagliptin and an intermediate thereof.
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Page/Page column 12
(2015/06/25)
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- AN IMPROVED PROCESS FOR PREPARING LINAGLIPTIN AND ITS KEY INTERMEDIATES
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The present invention relates to a process for the preparation of Linagliptin or a pharmaceutically acceptable slat thereof. Further aspects of the present invention relates to process for the preparation of Linagliptin key intermediate, having purity more than 98.0 %.
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Page/Page column 18
(2015/02/02)
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- PROCESS FOR THE PREPARATION OF DIPEPTIDYLPEPTIDASE INHIBITORS
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Provided is a process for the preparation of linagliptin of Formula I, comprising deprotecting a compound of Formula II wherein R1 and R2 together with the nitrogen to which they are attached form a phthalimido group, wherein the aromatic ring of the phthalimido group is substituted with one or more R3 substituents selected from the group consisting of halogen, alkyi, nitro and amino; or R1 is H and R2 is selected from the group consisting of trialkylsilyl, 2-trialkylsilylethoxycarbamates, acetyl, trihaloacetyl, 9-fluorenylmethoxycarbonyl, trityl, alkylsulfonyl, arylsulfonyl, diphenylphosphine and sulfonylethoxycarbonyl.
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Paragraph 0148
(2015/09/23)
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- AN IMPROVED PROCESS FOR THE PREPARATION OF LINAGLIPTIN
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The present invention relates to a process for preparing Linagliptin by purifying the intermediate compounds converting the purified intermediates into Linagliptin. The present invention also relates to the preparation of an amorphous Linagliptin.
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- Discovery of highly potent DPP-4 inhibitors by hybrid compound design based on linagliptin and alogliptin
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Highly potent DPP-4 inhibitors have been identified by hybrid compound design based on linagliptin and alogliptin. The most promising compound 2h (IC50 = 0.31 nM) exhibited 8.5-fold and 2.5-fold more potent activity than that of alogliptin (IC50 = 2.63 nM) and linagliptin (IC 50 = 0.77 nM), respectively. Compound 2h had a good inhibition selectivity for DPP-4 over DPP-8/9 and thus was selected for further biological evaluation, including oral glucose tolerance, plasma DPP-4 inhibitory activity, pharmacokinetic profile, acute toxicity and hERG inhibition. The assay results showed that 2h displayed significant in vivo glucose-lowering effect and low risk of toxicity. Further studies are expected to confirm 2h as a potential drug candidate for the treatment of type 2 diabetes.
- Lai, Zeng-Wei,Li, Chunhong,Liu, Jun,Kong, Lingyi,Wen, Xiaoan,Sun, Hongbin
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p. 547 - 560
(2014/07/21)
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- Selective inhibitors of fibroblast activation protein (FAP) with a xanthine scaffold
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Fibroblast activation protein (FAP) is a serine protease that is selectively expressed in many diseases involving activated stroma, including cancer, arthritis and hepatic and pulmonary fibrosis. FAP is closely related to dipeptidyl peptidase IV (DPPIV), of which many inhibitors are known and several are marketed as drugs. One of these is the xanthine derivative linagliptin. In a broad literature screen amongst reported DPPIV inhibitors, linagliptin was the only druglike compound identified that possessed significant FAP potency. Hence, this compound served as a starting point for a SAR study that aimed to identify structural determinants that selectively increase FAP-potency of linagliptin analogues. By investigating the influence of the substitution pattern on N1, N7 and C8 of the xanthine scaffold, we managed to decouple DPPIV and FAP potency and identified the first selective xanthine-based FAP inhibitors with low micromolar potency. Furthermore, these compounds are the only known FAP-inhibitors that do not rely on a warhead functionality to obtain potencies in this range.
- Jansen, Koen,De Winter, Hans,Heirbaut, Leen,Cheng, Jonathan D.,Joossens, Jurgen,Lambeir, Anne-Marie,De Meester, Ingrid,Augustyns, Koen,Van Der Veken, Pieter
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p. 1700 - 1707
(2014/12/12)
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- IMPROVED PROCESS FOR PREPARATION OF PURE LINAGLIPTIN
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The present application provides a process for preparation of Linagliptin reacting (R)-piperidine-3-amine of Formula II or an acid addition salt thereof with 1-[(4-methyl- quinazolin-2-yl)methyl]-3-methyl-7-(2-butyn-1-yl)-8-bromoxanthine of Formula III in the presence of a suitable base in an inert organic solvent.
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Page/Page column 20; 21
(2013/07/19)
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- SOLID STATE FORMS OF LINAGLIPTIN
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The present invention provides solid state forms of Linagliptin, processes for preparing the solid state forms, and pharmaceutical compositions thereof.
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Paragraph 0182
(2013/05/22)
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- Process for the preparation of Linagliptin
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The present invention relates to processes for the preparation of 8-(3R)-3-aminopiperidinyl)-7-butyn-2-yl-3-methyl-1-(4-methyl-quinazolin-2-ylmethyl)-3,7-dihydropurine-2,6-dione and novel intermediates useful in its synthesis.
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Page/Page column 8
(2012/07/03)
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- 8-(3-(R)-aminopiperidin-1-yl)-7-but-2-ynyl-3-methyl-1-(4-methyl-quinazolin- 2-ylmethyl)-3,7-dihydropurine-2,6-dione (BI 1356), a highly potent, selective, long-acting, and orally bioavailable DPP-4 inhibitor for the treatment of type 2 diabetes
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A new chemical class of potent DPP-4 inhibitors structurally derived from the xanthine scaffold for the treatment of type 2 diabetes has been discovered and evaluated. Systematic structural variations have led to 1 (BI 1356), a highly potent, selective, long-acting, and orally active DPP-4 inhibitor that shows considerable blood glucose lowering in different animal species. 1 is currently undergoing clinical phase IIb trials and holds the potential for once-daily treatment of type 2 diabetics.
- Eckhardt, Matthias,Langkopf, Elke,Mark, Michael,Tadayyon, Moh,Thomas, Leo,Nar, Herbert,Pfrengle, Waldemar,Guth, Brian,Lotz, Ralf,Sieger, Peter,Fuchs, Holger,Himmelsbach, Frank
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p. 6450 - 6453
(2008/04/12)
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- METHOD FOR PRODUCING CHIRAL 8-(3-AMINO-PIPERIDIN-1-YL)-XANTHINES
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The invention relates to an improved method for producing enantiomer-free 8-(3-amino-piperidin-1-yl)-xanthines.
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Page/Page column 10
(2008/06/13)
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- NOVEL 3-METHYL-7-BUTINYL-XANTHINES, PRODUCTION THEREOF, AND USE THEREOF AS MEDICAMENTS
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The invention relates to novel substituted xanthines of general formula (I), wherein R1, R2, and X are defined as mentioned in the claims, the tautomers, enantiomers, diastereomers, mixtures, and salts thereof, which have valuable pharmaceutical properties, especially an inhibitive effect on the activity of the dipeptidyl peptidase-IV (DPP-IV) enzyme.
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Page/Page column 21
(2008/06/13)
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- NOVEL 8-(PIPERAZINE-1-YL)- AND 8-([1,4]DIAZEPAN-1-YL)-XANTHINE, THE PRODUCTION AND USE THEREOF IN THE FROM OF A DRUG
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The invention relates to a substituted XANTHINE of formula (I), wherein R1 to R3 and n are such as defined in claims from 1 to 8 and tautomers, enantiomers, diastereomers, mixtures, prodrugs and the salts thereof, said substances exhibiting valuable pharmacological properties, in particular an inhibition on the activity of dipeptidylpeptidasa-IV enzyme (DPP-IV).
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Page/Page column 18
(2008/06/13)
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