cas 417716-92-8, Lenvatinib | Articles data

Articles about 417716-92-8Total 39 be found

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Preparation method of lenvatinib and preparation method of lenvatinib intermediate
The invention discloses a preparation method of lenvatinib and a preparation method of a lenvatinib intermediate. The preparation method of an amide compound as shown in a formula II comprises the following step: in a solvent, carrying out amidation react
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Paragraph 0117; 0122-0123; 0134-0136

(2021/07/01)

Synthesis method of lenvatinib
The invention relates to a systhesis method of lenvatinib. The method comprises the following steps: by taking 2-chloro-4-methyl hydroxybenzoate and 4-chloro-7-methoxyquinoline-6-amide as starting raw materials, carrying out substitution reaction to obtain 4-[3-chloro-4-methoxycarbonyl phenoxy]-7-methoxy-6-quinolinecarboxamide, carrying out an alkaline hydrolysis reaction to obtain 4-(3-chloro-4-carboxyphenoxy)-7-methoxy-6-quinolinecarboxamide, carrying out a Curtius rearrangement reaction on the 4-(3-chloro-4-carboxyphenoxy)-7-methoxy-6-quinolinecarboxamide and diphenyl azide phosphate (DPPA), and carrying out a reaction on the obtained product and cyclopropylamine to obtain lenvatinib through a one-pot method. The invention provides a novel method for synthesizing lenvatinib. The method has the advantages of simple reaction steps, simple and easily available raw materials, simple operation and low production cost.
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(2021/08/28)

Synthetic method of anti-cancer drug lenvatinib
The invention provides a synthetic method of an anti-cancer drug lenvatinib. The synthetic method comprises the following steps of synthesis of a compound 2, synthesis of a compound 4, synthesis of acompound 5, synthesis of a compound 6, synthesis of a compound 7, synthesis of a compound 8, synthesis of a compound 9, synthesis of a compound 10, synthesis of a compound 11 and synthesis of a compound 12. Synthesis of a compound 2 is as follows: sequentially adding raw materials of Meldrum's acid (40g, 277.8 mmol) and trimethyl orthoformate (147g, 1.387 mol) into a 500ml of three-neck flask, slowly performing heating to 90 DEG C for reaction under a stirring condition, slowly performing cooling to room temperature under a solution stirring condition after the reaction is finished, performingfiltering after crystallization, recrystallizing a product by using petroleum ether/ethyl acetate according to a ratio of 5: 1, and performing drying to obtain a faint yellow product 2; by improvingthe synthesis method of the anti-cancer drug lenvatinib, the synthesis method has the advantages of reasonable design, simple operation flow, easily available raw materials, stable yield and easinessin industrial production, so that the problems and defects of the synthesis method are effectively solved and overcome.
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Paragraph 0010

(2021/01/25)

Novel method for the synthesis of lenvatinib using 4-nitrophenyl cyclopropylcarbamate and their pharmaceutical salts
4-Nitrophenyl cyclopropylcarbamate was deployed as a novel synthon for the synthesis of anticancer drug lenvatinib. 4-Nitrophenyl cyclopropylcarbamate was prepared by the reaction of 4-nitrophenyl chloroformate and cyclopropyl amine in acetonitrile at room temperature. Furthermore, lenvatinib was synthesized by reacting 4-(4-amino-3-chlorophenoxy)-7-methoxyquinoline-6-carboxamide with 4-nitrophenyl cyclopropylcarbamate in good yields. Apart from the synthesis of lenvatinib, citrate, phosphate, malate and oxalate salts of?lenvatinib were also reported in good yields.
Sadineni, Ravi Kumar,Rapolu, Rajesh Kumar,Raju, V. V. N. K. V. Prasada,Srinivasu,Malladi, Sireesha,Mulakayala, Naveen
p. 1475 - 1483
(2020/11/05)

Synthesis method of lenvatinib and new intermediate
The invention discloses a synthesis method of lenvatinib and a new intermediate. The method comprises the following steps: step 1, taking 4-amino-3-chlorophenol hydrochloride and 4-chloro-7-methoxy-6-amido quinoline as initial raw materials, and carrying
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Paragraph 0049; 0059-0061

(2020/07/24)

Preparation method of lenvatinib intermediate
The invention discloses a preparation method of a lenvatinib intermediate. The preparation method comprises the following steps: carrying out a nucleophilic substitution reaction among a compound shown as a formula I, a compound shown as a formula II and
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Paragraph 0026; 0029-0031; 0034-0036; 0039-0041; 0045-0047

(2020/07/12)

Preparation method of high-purity lenvatinib mesylate crystal form C
The invention belongs to the technical field of pharmaceutical chemicals and especially relates to a preparation method of a lenvatinib mesylate crystal form C. According to the method, the conditions of high temperature, acid serving as a solvent and the
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Paragraph 0047; 0051-0053

(2020/10/04)

Preparation method of lenvatinib
The invention discloses a preparation method of lenvatinib, which comprises the following steps: by using 4-nitro-2-chlorobenzonitrile as an initial raw material, introducing nitro into molecules forelectron withdrawing, thereby greatly lowering the elect
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(2020/05/01)

Method for refining Lenvatinib mesylate
The invention discloses a method for refining Lenvatinib mesylate. The method for refining the Lenvatinib mesylate, provided by the invention, comprises the following step: subjecting a solution formed by an organic solvent and crude Lenvatinib mesylate t
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(2020/03/02)

PROCESS FOR THE PREPARATION OF LENVATINIB
The present invention relates to a process for the preparation of Lenvatinib of formula (I) from 4-amino-3-chloro-phenol and 4-chloro-7-methoxyquinoline-6-carboxamide.
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(2020/04/09)

Preparation method of high-purity lenvatinib
The invention relates to a preparation method of lenvatinib, which comprises the following steps: by using 3-chloro-4-nitrophenol and 7-methoxy-4-chloro-quinoline-6-formamide as raw materials, generating 4-(3-chloro-4-nitrophenoxy)-7-methoxyquinoline-6-formamide, and carrying out catalytic hydrogenation reaction to generate 4-(4-amino-3-chlorophenoxy)-7-methoxyquinoline-6-formamide; and then carrying out a reaction with N-cyclopropyl-1H-imidazole-1-formamide in an organic weak base environment, so as to generate the final product lenvatinib. The method has the advantages of short route, recyclable solvent, environmental protection, simple steps, mild conditions, high total yield of the route, high purity of the obtained product, and easy industrialization.
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(2020/07/24)

Preparation method of high-purity lenvatinib and salt thereof
The invention relates to a preparation method of lenvatinib and salt thereof. The adopted method for preparing the lenvatinib has the advantages that the process is simple, the cost is low, the purity is high, the single-purity content meets the regulatio
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Paragraph 0065-0067

(2019/10/10)

PROCESS FOR THE PREPARATION OF LENVATINIB OR ITS SALTS THEREOF
The present invention provides a process for the preparation of Lenvatinib or its salts thereof. The present invention also provides a crystalline form of Lenvatinib, which is characterized by the PXRD pattern as shown in figure 1. The present invention a
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Page/Page column 10

(2019/05/30)

Preparation method of lenvatinib and its salts
The invention discloses a preparation method of lenvatinib and its salts, wherein N-methylpyrrolidone is used as a reaction solvent in the step of condensation with phenyl chloroformate. The preparation method has the advantages that the danger is success
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Paragraph 0056-0058

(2019/06/30)

NOVEL POLYMORPHS OF 4-[3-CHLORO-4-(N'-CYCLOPROPYL UREIDO)PHENOXY]-7-METHOXYQUINOLINE-6-CARBOXAMIDE, ITS SALTS AND PROCESS FOR THE PREPARATION THEREOF
The present invention relates to novel polymorphs of 4-[3-chloro-4-(N'- cyclopropyl ureido) phenoxy]-7- methoxyquinoline- 6- carboxamide methanesulfonate represented by following structural formula-1a and process for preparation thereof. Further, the pres
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Page/Page column 28; 29

(2019/06/23)

A [...] synthetic method
The invention provides a method of synthesizing [...]. First of all the invention to 4 - cyano - 3 - hydroxy aniline as the starting material, by dimethyl carbonate methylation, after third acid in the oximation reaction at room temperature, the conditions in the PPA shut-ring forms the 6 - cyano - 7 - methoxy - 4 - quinolinone, in thionyl chloride formed under the action of the 6 - cyano - 7 - methoxy - 4 - [...], under acidic conditions [...] cyano hydrolysis synthesis of one of the intermediates 6 - formamido - 7 - methoxy - 4 - chloroquinolin. Then the 4 - hydroxy - 2 chloroaniline with cyanogen bromide at low temperature 4 - hydroxy - 2 - chloro cyaniding amine, the 4 - hydroxy - 2 - chloro cyaniding amine with bearing-displacement generating Reeth reaction synthesis [...] another key intermediate 1 - (2 - chloro - 4 - hydroxy-phenyl) - 3 - ring propyl urea. Finally the two intermediate 6 - formamido - 7 - methoxy - 4 - chloroquinolin and 1 - (2 - chloro - 4 - hydroxy-phenyl) - 3 - ring propyl urea in the alkaline environment for carrying out the alkylation reaction [...]. This scheme has mild reaction conditions, no highly toxic reagent, environmental protection and the like.
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(2019/05/22)

Method for synthesizing lenvatinib
The invention belongs to the field of chemical pharmacy, and specifically relates to a method for synthesizing lenvatinib. The method comprises the following steps: step 1, taking 4-aminosalicylic acid as a raw material, and preparing 4-chloro-7-methoxyquinoline-6-formamide through methylation, condensation with meldrum's acid, high-temperature cyclization, chlorination and ammoniation; step 2, taking 3-chloro-4-aminophenol as a raw material, and reacting with phenyl chloroformate and cyclopropylamine to obtain 1-(2-chloro-4-hydroxy phenyl)-3-cyclopropyl urea; and step 3, enabling the 4-chloro-7-methoxyquinoline-6-formamide prepared in step 1 to react with the 1-(2-chloro-4-hydroxy phenyl)-3-cyclopropyl urea prepared in step 2 under action of potassium tert-butoxide to obtain the lenvatinib. The invention provides a brand-new route for synthesising the lenvatinib. The used reagent is cheap and is easily available, is simple in operation, has a yield higher than that of other methods, and is easy for industrial production.
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(2019/03/28)

AN IMPROVED PROCESS FOR THE PREPARATION OF LENVATINIB
The present invention relates to an improved and economic industrial process for the preparation of Lenvatinib and salt thereof. The present invention also relates to method and novel use of a reagent for preparing an amorphous form of Lenvatinib mesylate
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(2019/02/06)

Method for synthesizing lenvatinib
The invention discloses a method for synthesizing lenvatinib. The method comprises the following steps: with 7-methoxy-4-oxo-1,4-dihydro-quinoline-6-formamide as an initial raw material, carrying outan oxo-arylation reaction on the initial raw material an
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Paragraph 0036-0038; 0042; 0046

(2018/04/03)

Synthesis method for lenvatinib
The invention provides a synthesis method for lenvatinib. The synthesis method takes m-chlorophenol as a raw material and a target product, i.e., the lenvatinib, is obtained through four-step reaction. According to the synthesis method provided by the invention, steps of an original synthesis route are reduced and relatively high yield is kept; and the cost of the raw material is reduced and the atom economy is improved.
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Paragraph 0009; 0034-0036; 0040; 0042

(2018/11/22)

Preparation method of lenvatinib
The invention relates to a preparation method of lenvatinib, and belongs to the field of medicine chemistry. The preparation method of lenvatinib uses a brand-new preparation scheme; a target compoundmeeting the requirement can be obtained no matter from which intermediates. The method provided by the invention has the advantages that the steps are short; the reaction operation is simple; the safety and the reliability are realized; the yield is high; the cost is low; the purity is high; the pollution is low; the operation is simple, and the like. The total yield of lenvatinib can reach about84 percent; the purity can reach 99.7 percent.
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Paragraph 0064; 0065; 0066; 0068

(2018/10/19)

[...] intermediate and its preparation and [...] preparation (by machine translation)
The present invention relates to the field of drug synthesis, discloses a [...] key intermediate 1 - (2 - chloro - 4 - hydroxy-phenyl) - 3 - ring propyl urea and its preparation and [...] preparation. The music-cutting of the Buddhist intermediate, its pu
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Paragraph 0130; 0131; 0132; 0133; 0134; 0135; 0136-0138

(2019/01/08)

Preparation method of lenvatinib impurity
The invention provides a preparation method of a lenvatinib impurity, and particularly provides a preparation method of the lenvatinib impurity 4,4'-[4,4'-carbonylbis(azanediyl)bis(3-chloro-4,1-phenylene)]bis(oxy)bis(7-methoxyquinoline-6-carboxamide).
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Paragraph 0059-0062

(2018/11/03)

CRYSTALLINE FORMS OF SALTS OF LENVATINIB
The present invention provides a crystalline form of lenvatinib hydrochloride, a crystalline form of lenvatinib hydrobromide, a crystalline form of lenvatinib tosylate, processes for their preparation, and pharmaceutical compositions thereof. The present
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Page/Page column 12

(2018/04/12)

A method for preparing le Fati Nepal
The invention discloses a preparation method of lenvatinib. The preparation method comprises the following steps : adopting 4-amino-3-irgasan as a starting material, firstly adopting amino groups for protection, then carrying out butt jointing with 4-chloro-7-methoxyquinoline-6-amide, removing amino-group protective groups, reacting with cyclopropylamine and preparing to obtain the lenvatinib. The preparation method disclosed by the invention is simple and easy to implement, high in yield, good in quality and convenient in industrial production.
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(2017/08/25)

HIGH-PURITY QUINOLINE DERIVATIVE AND METHOD FOR MANUFACTURING SAME
Provided is a compound represented by formula (IV) or a salt thereof, wherein the content of the compound represented by formula (I) is 350 ppm by mass or less.
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Paragraph 0148; 0149

(2017/09/02)

Preparation method of lenvatinib
The invention belongs to the field of medical chemistry, and provides a preparation method of a compound of lenvatinib. The method is characterized by comprising the following steps that (1) under the existence of an organic solvent and an alkali reagent,
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(2017/08/17)

Preparation method of lenvatinib
The invention relates to a preparation method of lenvatinib, and concretely relates to a method for preparing lenvatinib through a one-step reaction formation reaction. The preparation method of lenvatinib has the advantages of small amount of generated impurities difficult to remove, easy post-treatment, convenient quality control in the bulk drug production process, and provision of convenience for researches of subsequent preparations.
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Paragraph 0038; 0039; 0040; 0041; 0042; 0043

(2017/07/22)

Lenvatinib synthesizing method
The invention discloses a lenvatinib synthesizing method.The method includes the steps that 4-amino-3-chlorophenol and benzyl chloroformate are subjected to amidation reaction, the obtained 4-(carbobenzoxy)amino-3-chlorophenol and 4-chlorine-7-methoxyquinoline-6-formamide are subjected to condensation reaction, the obtained 4-[3-chlorine-4-(carbobenzoxy)aminophenoxy]-7-methoxyquinoline-6-formamide and cyclopropylamine are subjected to amidation reaction, and the finished product lenvatinib is obtained.The method is short in process route step, operation is simplified, cost is low, and the method is environmentally friendly and suitable for industrial production.
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Paragraph 0031; 0038; 0039; 0040

(2016/10/09)

ANTI-TUMOR AGENT
A combination therapy for tumor is provided. Disclosed is a method of treating tumor, the method comprises administering to a patient, a compound or pharmaceutically acceptable salt thereof represented by Formula (I) and everolimus represented by Formula (II): wherein R1 is C1-6 alkyl or C3-8 cycloalkyl; R2 is a hydrogen atom or C1-6 alkoxy; and R3 is a hydrogen atom or a halogen atom.
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(2012/04/05)

METHOD FOR ASSAY ON THE EFFECT OF VASCULARIZATION INHIBITOR
The present invention provides a method of predicting the antitumor effect of an angiogenesis inhibitor. It is possible to predict the antitumor effect of an angiogenesis inhibitor by evaluating the EGF dependency of a tumor cell for proliferation and/or survival and using the EGF dependency as an indicator. Since the antitumor effect of an angiogenesis inhibitor correlates with the EGF dependency of a tumor cell for proliferation and/or survival, the angiogenesis inhibitors is capable of producing excellent antitumor effect when combined with a substance having EGF inhibitory activity.
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(2010/04/30)

Amorphous salt of 4-(3-chiloro-4-(cycloproplylaminocarbonyl)aminophenoxy)-7-method-6-quinolinecarboxamide and process for preparing the same
An amorphous form of a salt of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide.
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Page/Page column 4

(2008/06/13)

MEDICINAL COMPOSITION
A pharmaceutical composition comprising: an active ingredient consisting of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide, salt thereof, or solvate of the foregoing; and (i) a compound, a 5% (w/w) aqueous solution
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Page/Page column 12

(2008/06/13)

Polymorph of 4-[3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy]-7-methoxy-6- quinolinecarboxamide and a process for the preparation of the same
A polymorph (A) of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide, having a diffraction peak at a diffraction angle (2θ±0.2°) of 15.75° in a powder X-ray diffraction; and a polymorph (B) of 4-[3-chloro-4-(cyclopropy
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Page/Page column 7

(2008/06/13)

CRYSTAL OF SALT OF 4-(3-CHLORO-4-(CYCLOPROPYLAMINOCARBONYL)AMINO-PHENOXY)-7-METHOXY-6-QUINOLINECARBOXAMIDE OR OF SOLVATE THEREOF AND PROCESSES FOR PRODUCING THESE
A crystal of a 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide hydrochloride, hydrobromide, p-toluenesulfonate, sulfate, methanesulfonate or ethanesulfonate, or a solvate thereof.
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Page/Page column 15

(2008/06/13)

AMORPHOUS SALT OF 4-(3-CHLORO-4-(CYCLOPROPYLAMINOCARBONYL)-AMINOPHENOXY)-7-METHOXY-6-QUINOLINECARBOXAMIDE AND PROCESS FOR PRODUCING THE SAME
An amorphous salt of 4-(3-chloro-4-(cyclopropylaminocarbonyl)-aminophenoxy)-7-methoxy-6-quinolinecarboxamide.
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Page/Page column 10

(2008/06/13)

UREA DERIVATIVE AND PROCESS FOR PRODUCING THE SAME
A process for preparing a compound (C) represented by the following formula: wherein R1 represents hydrogen, C1-6 alkyl or C3-8 cycloalkyl, and R2 represents hydrogen or methoxy,characterized by reacting a compo
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Page/Page column 8

(2008/06/13)

c-Kit kinase inhibitor
It was discovered that a compound represented by the general formula (I) shows strong c-Kit kinase inhibitory activity, and it inhibits proliferation of c-Kit kinase activated-cancer cells in vitro and in vivo. A novel anticancer agent showing c-Kit kinas
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(2008/06/13)

Nitrogen-containing aromatic derivatives
Compounds represented by the following general formula: [wherein Ag is an optionally substituted 5- to 14-membered heterocyclic group, etc.; Xg is —O—, —S—, etc.; Yg is an optionally substituted C6-14 aryl group, an optionally substituted 5- to 14-membered heterocyclic group, etc.; and Tg1 is a group represented by the following general formula: (wherein Eg is a single bond or —N(Rg2)—, Rg1 and Rg2 each independently represent a hydrogen atom, an optionally substituted C1-6 alkyl group, etc. and Zg represents a C1-8 alkyl group, a C3-8 alicyclic hydrocarbon group, a C6-14 aryl group, etc.)], salts thereof or hydrates of the foregoing.
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(2008/06/13)