- Intermediate for preparing pexidartinib, and preparation method and application thereof
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The invention discloses an intermediate for preparing pexidartinib, a preparation method and application thereof. According to the invention, raw materials and reagents used in the method are cheap and easily available, the ultralow-temperature reaction and corrosive trifluoroacetic acid are successfully avoided, the method has low requirements on equipment and is beneficial to energy conservationand emission reduction, the preparation process of pexidartinib and related intermediates is simple to operate, post-treatment and purification are convenient, column chromatography is not needed, and the total yield is up to 48%; according to the method, a compound (IV) is prepared from a compound (II), a compound (V) is prepared from a compound (IV), and pexidartinib is prepared, so that the defects and deficiencies of preparation methods reported in literatures are overcome; and the intermediate for preparing pexidartinib is a compound with a structure represented by a formula (A1), a compound with a structure represented by a formula (II) or a compound with a structure represented by a formula (IV).
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Paragraph 0069-0072; 0077-0080
(2020/07/12)
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- Halogen–metal exchange on bromoheterocyclics with substituents containing an acidic proton via formation of a magnesium intermediate
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A selective and practical bromine–metal exchange on bromoheterocyclics bearing substituents with an acidic proton under non-cryogenic conditions was developed by a simple modification of an existing protocol. Our protocol of using a combination of i-PrMgCl and n-BuLi has not only solved the problem of intermolecular quenching that often occurred when using alkyl lithium alone as the reagent for halogen–lithium exchange, but also offered a highly selective method for performing bromo–metal exchange on dibrominated arene compounds through chelation effect.
- Tian, Qingqiang,Shang, Suqin,Wang, Huajun,Shi, Guoqiang,Li, Zhiyao,Yuan, Jianyong
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supporting information
(2017/12/05)
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- SPIROCYCLIC HAT INHIBITORS AND METHODS FOR THEIR USE
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Compounds having a structure of Formula (IX) or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, wherein R1, R2a, R2b, R3a, R3b, R4a, R4b, Q1----Q2, R6, R7, A, B, W, x, and y are as defined herein and are provided. Pharmaceutical compositions comprising such compounds and methods for treating various HAT-related conditions or diseases, including cancer, by administration of such compounds are also provided.
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Page/Page column 747
(2016/04/10)
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- Process for the preparation of 3-(6-amino-pyridin-3yl)-2-acrylic acid derivatives
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The present invention relates to a process for the preparation of a compound of the formula I, which comprises reacting a compound of the formula IV with the compound of formula VII R15-A2-CHO and to novel intermediate compounds used therein.
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Paragraph 0283; 0284
(2013/09/26)
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- Process for the preparation of 3-(6-amino-pyridin-3yl)-2-acrylic acid derivatives
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Process for the preparation of 3-(6-amino-pyridin-3yl)-2-acrylic acid derivatives The present invention relates to a process for the preparation of a compound of the formula (I), which comprises reacting a compound of the formula IV, (IV) with the compound of formula VII R15-A2-CHO and to novel intermediate compounds used therein.
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Page/Page column 22
(2012/05/31)
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- OXADIAZOLIDINEDIONE COMPOUND
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A pharmaceutical agent having GPR40 receptor agonistic action, particularly a compound which is useful as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus. The present inventors have examined a compound having GPR40 receptor agonistic action, confirmed that an oxadiazolidinedione compound which has a substituent such as a benzyl group, etc. linked with a substituent such as a phenyl group, etc. through a linker at the 2-position of an oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof has an excellent GPR40 agonistic activity, and thus completed the invention. The oxadiazolidinedione compound has excellent insulin secretagogue action and anti-hyperglycemic action, and therefore can be used as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus.
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Page/Page column 24
(2010/08/18)
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- Imidazole acetic acid TAFIa inhibitors: SAR studies centered around the basic P′1 group
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Structural modifications of the aminopyridine P1 ′ group of imidazole acetic acid based TAFIa inhibitors led to the discovery of the aminocyclopentyl analog 28, a 1nM TAFIa inhibitor with CLT50 functional activity of 14nM but without selectivity against CPB. While not as active, aminobutyl derivative 27 provided an improved 6.7-fold selectivity for TAFIa versus CPB.
- Nantermet, Philippe G.,Barrow, James C.,Lindsley, Stacey R.,Young, Marybeth,Mao, Shi-Shan,Carroll, Steven,Bailey, Carolyn,Bosserman, Michele,Colussi, Dennis,McMasters, Daniel R.,Vacca, Joseph P.,Selnick, Harold G.
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p. 2141 - 2145
(2007/10/03)
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- PYRAZINONE THROMBIN INHIBITORS
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Compounds of the invention are useful in inhibiting thrombin and associated thrombotic occlusions having the following structure: STR1 for example: STR2
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