[EN] NOVEL SYNTHETIC OPTIONS TOWARDS THE MANUFACTURE OF (6R,10S)-10- {4-[5-CHLORO-2-(4-CHLORO-1H-1,2,3-TRIAZOL-1-YL)PHENYL]-6-OXO-1(6H)- PYRIMIDINYL}- 1-(DIFLUOROMETHYL)-6-METHYL-1,4,7,8,9,10-HEXAHYDRO-11,15 -(METHENO)PYRAZOLO [4,3-B] [1,7] DIAZACYCLOTETRADECIN-5(6H)-ONE<br/>[FR] NOUVELLES OPTIONS SYNTHÉTIQUES POUR LA FABRICATION DE (6R,10S)-10-{4-[5-CHLORO-2-(4-CHLORO-1H-1,2,3-TRIAZOL-1-YL) PHÉNYL]-6-OXO-1(6H)-PYRIMIDINYL}1-(DIFLUOROMÉTHYL)-6-MÉTHYL-1,4,7,8,9,10-HEXAHYDRO-11,15- (METHENO)PYRAZOLO [4,3-B] [1,7] DIAZACYCLOTÉTRADECIN-5 (6H)-ONE
申请人:BRISTOL MYERS SQUIBB CO
公开号:WO2020210613A1
公开(公告)日:2020-10-15
Highly efficient methods are provided for preparing key intermediates in the synthesis of Compound (I), which are broadly applicable and can provide selected components having a variety of substituents groups.
Activation of benzylic amines towards regioselective metallation by borane complex formation
作者:Mark R. Ebden、Nigel S. Simpkins、David N.A. Fox
DOI:10.1016/0040-4039(95)01797-l
日期:1995.11
Formation of borane complexes of N, N-dimethylbenzylamine 4 and N methyltetrahydroisoquinoline 1 facilitates regioselective metallation of these systems using BuLi, giving benzylic anions which react with a range of electrophiles.
PROCESS FOR PREPARATION OF ERIBULIN AND INTERMEDIATES THEREOF
申请人:DR. REDDY'S LABORATORIES LIMITED
公开号:US20190276470A1
公开(公告)日:2019-09-12
The present application relate to process for preparation of tetrahydrofuran compound of formula II, 4-Methylene tetrahydrofuran compound of formula V and tetrahydropyran compound of formula IX which are useful as intermediates for the preparation of halichondrin B analogues such as Eribulin or its pharmaceutically acceptable salts.
Process for preparation of eribulin and intermediates thereof
申请人:DR. REDDY'S LABORATORIES LIMITED
公开号:US10836776B2
公开(公告)日:2020-11-17
The present application relate to process for preparation of tetrahydrofuran compound of formula II, 4-Methylene tetrahydrofuran compound of formula V and tetrahydropyran compound of formula IX which are useful as intermediates for the preparation of halichondrin B analogues such as Eribulin or its pharmaceutically acceptable salts.
本申请涉及制备式 II 的四氢呋喃化合物、式 V 的 4-亚甲基四氢呋喃化合物和式 IX 的四氢吡喃化合物的工艺,这些化合物可用作制备卤化菊酯 B 类似物(如 Eribulin 或其药学上可接受的盐)的中间体。
Masui, Masaichiro; Kamada, Yoshiyuki; Sasaki, Etuko, Chemical and pharmaceutical bulletin, 1982, vol. 30, # 4, p. 1234 - 1243