Synthesis of both enantiomers of baclofen using (R)- and (S)-N-phenylpantolactam as chiral auxiliaries

被引：43

作者：

Camps, P ^{[1
]}

Muñoz-Torrero, D ^{[1
]}

Sánchez, L ^{[1
]}

机构：

[1] Univ Barcelona, Fac Farm, Quim Farmaceut Lab, Unitat Associada CSIC, E-08028 Barcelona, Spain

来源：

TETRAHEDRON-ASYMMETRY | 2004年 / 15卷 / 13期

关键词：

D O I：

10.1016/j.tetasy.2004.05.021

中图分类号：

O61 [无机化学];

学科分类号：

070301 ; 081704 ;

摘要：

Esterification of racemic 4-nitro-3-(4-chlorophenyl)butanoic acid with (R)- or (S)-N-phenylpantolactam as the chiral auxiliary allowed us to obtain the (3R,3'R)- or (3S,3'S)-nitro esters with > 98:2 dr after column chromatography. Hydrolysis of the resulting diastereopure nitro esters gave the corresponding enantiopure nitro acids, which were readily converted in high yields into either (R)- or (S)-baclofen hydrochloride. (C) 2004 Elsevier Ltd. All rights reserved.

引用

页码：2039 / 2044

页数：6

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