- Novel method for the synthesis of lenvatinib using 4-nitrophenyl cyclopropylcarbamate and their pharmaceutical salts
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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
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p. 1475 - 1483
(2020/11/05)
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- Preparation method of lenvatinib mesylate
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The invention relates to a preparation method of lenvatinib mesylate, in particular to a method for efficiently synthesizing lenvatinib mesylate by taking 4-chloro-6-cyano-7-methoxy quinoline and 2-chloro-4-hydroxy aniline formic acid cyclopropanamide as raw materials through two steps of substitution reaction and hydrolysis reaction. The preparation method of lenvatinib mesylate provided by the invention is a preparation method which is short in steps, high in yield, low in cost, less in three wastes, good in product purity and suitable for industrialization.
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Paragraph 0016-0018
(2021/01/15)
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- Method for refining Lenvatinib mesylate
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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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- Synthesis method of lenvatinib and new intermediate
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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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- Preparation method of high-purity lenvatinib mesylate crystal form C
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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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- NOVEL POLYMORPHS OF 4-[3-CHLORO-4-(N'-CYCLOPROPYL UREIDO)PHENOXY]-7-METHOXYQUINOLINE-6-CARBOXAMIDE, ITS SALTS AND PROCESS FOR THE PREPARATION THEREOF
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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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- PROCESS FOR THE PREPARATION OF LENVATINIB OR ITS SALTS THEREOF
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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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- AN IMPROVED PROCESS FOR THE PREPARATION OF LENVATINIB
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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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- Preparation method of lenvatinib and its salts
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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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- Preparation method of lenvatinib mesylate crystal form B
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The present invention relates to a preparation method of a lenvatinib mesylate crystal form B. The method includes: reacting 4-(3-chloro-4-(cyclopropyl amino carbonyl)aminophenoxy)-7-methoxy-6-quinoline carboxamide with methanesulfonic acid in a specific
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Page/Page column 0016-0025
(2019/10/01)
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- Lenvatinib mesilatee polymorph and preparation method thereof
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The invention relates to a lenvatinib mesilatee polymorph and a preparation method thereof. In particular, the present invention provides a novel crystalline form of a lenvatinib mesilatee dimethyl sulfoxide solvate and a preparation method of the novel c
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Paragraph 0102-0105; 0110; 0111
(2019/07/10)
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- NEW CRYSTAL FORM OF LENVATINIB METHANESULFONATE SALT AND PREPARATION METHOD THEREOF
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The present disclosure relates to a novel crystalline form of lenvatinib mesylate and the preparation method thereof. The novel crystalline form of mesylate of the present disclosure can be used for treating invasive and differentiated thyroid cancer. The
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Paragraph 0052; 0053; 0054; 0059; 0060
(2018/06/15)
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- SOLID STATE FORMS OF LENVATINIB MESYLATE
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The present invention provides a crystalline form of Lenvatinib Mesylate, processes for the preparation of crystalline form of lenvatinib Mesylate and pharmaceutical compositions thereof. The crystalline form of lenvatinib Mesylate designated as Form VN1
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Page/Page column 11
(2018/07/29)
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- CRYSTALLINE FORMS OF SALTS OF LENVATINIB
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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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- HIGH-PURITY QUINOLINE DERIVATIVE AND METHOD FOR MANUFACTURING SAME
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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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- Amorphous salt of 4-(3-chiloro-4-(cycloproplylaminocarbonyl)aminophenoxy)-7-method-6-quinolinecarboxamide and process for preparing the same
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An amorphous form of a salt of 4-(3-chloro-4-(cyclopropylaminocarbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide.
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Page/Page column 6
(2008/06/13)
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- CRYSTAL OF SALT OF 4-(3-CHLORO-4-(CYCLOPROPYLAMINOCARBONYL)AMINO-PHENOXY)-7-METHOXY-6-QUINOLINECARBOXAMIDE OR OF SOLVATE THEREOF AND PROCESSES FOR PRODUCING THESE
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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 17
(2008/06/13)
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- AMORPHOUS SALT OF 4-(3-CHLORO-4-(CYCLOPROPYLAMINOCARBONYL)-AMINOPHENOXY)-7-METHOXY-6-QUINOLINECARBOXAMIDE AND PROCESS FOR PRODUCING THE SAME
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An amorphous salt of 4-(3-chloro-4-(cyclopropylaminocarbonyl)-aminophenoxy)-7-methoxy-6-quinolinecarboxamide.
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Page/Page column 15
(2008/06/13)
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- c-Kit kinase inhibitor
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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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