SYNTHESIS OF P1 ASPARTATE-BASED PEPTIDE ACYLOXYMETHYL AND FLUOROMETHYL KETONES AS INHIBITORS OF INTERLEUKIN-1-BETA-CONVERTING ENZYME

被引：44

作者：

REVESZ, L

BRISWALTER, C

HENG, R

LEUTWILER, A

MUELLER, R

WUETHRICH, HJ

机构：

[1] Sandoz Research Institute Berne Ltd.

来源：

TETRAHEDRON LETTERS | 1994年 / 35卷 / 52期

关键词：

D O I：

10.1016/0040-4039(94)88361-0

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

Improved procedures have been developed for the synthesis of P1 aspartate-based 2,6-dichlorobenzoyloxymethyl ketone 1 and fluoromethyl ketone 2, the prodrugs of two potent ICE-inhibitors. 1 was prepared from (R)-trans-4,5-O-isopropylidene-4,5-dihydroxy-2-pentenecarboxylic acid ethyl ester; 2 was obtained via a nitro-aldol condensation as key step from in situ generated fluoroacetaldehyde.

引用

页码：9693 / 9696

页数：4

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