Chemo-enzymatic synthesis of (R)- and (S)-3,4-dichlorophenylbutanolide intermediate in the synthesis of sertraline
Chemo-enzymatic synthesis of (R)- and (S)-3,4-dichlorophenylbutanolide intermediate in the synthesis of sertraline
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DOI：
10.1016/s0957-4166(99)00402-4
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发表时间：
1999-10-15
影响因子：
--
通讯作者：
Servi, S
中科院分区：
文献类型：
--
作者：
Barbieri, C;Caruso, E;Servi, S
用全细胞生物催化剂还原3，4-二氯苯酰氯，得到(R)-或(S)-氯丙烷，产率高，对映体过量好到高。在疏水吸附树脂用量为4g/L的条件下，白地霉(CBS 233.76)菌体的产率和对映体纯度分别提高到95%和98%，后者转化为(R)-3，4-二氯苯基丁内酯，合成(+)-顺-1S，4S-舍曲林的中间体。(C)1999爱思唯尔科学有限公司。保留所有权利。
3,4-Dichlorophenacylchloride was reduced with whole cell biocatalysts to give the (R)- or (S)-chrorohydrine in high yields and good to high enantiomeric excess. Yields and enantiomeric purity of the (S)-enantiomer were increased to 95 and >98%, respectively, using growing cells from Geotrichum candidum (CBS 233.76) in the presence of hydrophobic adsorbing resins at 4 g/l. The latter compound was transformed into (R)-3,4-dichlorophenylbutanolide, intermediate in the synthesis of (+)-cis-1S,4S-sertraline. (C) 1999 Elsevier Science Ltd. All rights reserved.