KINETIC RESOLUTION OF PIPERAZINE-2-CARBOXAMIDE BY LEUCINE AMINOPEPTIDASE - AN APPLICATION IN THE SYNTHESIS OF THE NUCLEOSIDE TRANSPORT BLOCKER (-)DRAFLAZINE

被引：24

作者：

BRUCE, MA ^{[1
]}

LAURENT, DRS ^{[1
]}

POINDEXTER, GS ^{[1
]}

MONKOVIC, I ^{[1
]}

HUANG, S ^{[1
]}

BALASUBRAMANIAN, N ^{[1
]}

机构：

[1] BRISTOL MYERS SQUIBB CO,PHARMACEUT RES INST,WALLINGFORD,CT 06492

来源：

SYNTHETIC COMMUNICATIONS | 1995年 / 25卷 / 17期

关键词：

D O I：

10.1080/00397919508011814

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

The resolution of N-t-Boc-piperazine carboxamide 5 proceeded smoothly in the presence of leucine aminopeptidase to produce acid (S)-1 and amide (R)-5 with good optical purity. Sequential alkylation and functional group manipulation of carboxamide (S)-5 provided the known nucleoside transport blocker draflazine (-) 2.

引用

页码：2673 / 2684

页数：12

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