发明名称 Asymmetric catalytic reduction of oxcarbazepine
摘要 A process for preparing (S)-(+)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide or (R)-(-)-10,11-dihydro-10-hydroxy-5H-dibenz/b,f/azepine-5-carboxamide, by reduction of oxcarbazepine in the presence of a catalyst and a hydride source is disclosed. The catalyst is prepared from a combination of [RuX 2 (L)] 2 wherein X is chlorine, bromine or iodine, and L is an aryl or aryl-aliphatic ligand, with a ligand of formula (A) or formula (B): wherein R 1 is chosen from C 1-6 alkoxy and C 1-6 alkyl, n is a number from 0 to 5, and when n is a number from 2 to 5, R 1 can be the same or different, and R 2 is alkyl, substituted alkyl, aryl, substituted aryl, alkaryl or substituted alkaryl. The hydride source is either NR 3 R 4 R 5 and formic acid, [R 3 R 4 R 5 NH][OOCH] and optionally formic acid, or [M][OOCH] x and formic acid, wherein R 3 , R 4 and R 5 are C 1-6 alkyl, M is an alkali metal or alkaline earth metal and x is 1 or 2. A pH from 6.5 to 8 is maintained during the process.
申请公布号 ZA200800986(B) 申请公布日期 2010.02.24
申请号 ZA20080000986 申请日期 2006.04.21
申请人 PORTELA & C.A., S.A. 发明人 LEARMONTH, DAVID ALEXANDER;GRASA, GRABRIELA ALEXANDRA;ZANOTTI-GEROSA, ANTONIO
分类号 C07D;C07D223/22 主分类号 C07D
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