Synthesis of P1 aspartate-based peptide acyloxymethyl and fluoromethyl ketones as inhibitors of interleukin-1β-converting enzyme |
| |
Authors: | Laszlo Revesz Chantal Briswalter Richard Heng Albert Leutwiler Rudolf Mueller and Hans-Juerg Wuethrich |
| |
Institution: | Sandoz Research Institute Berne Ltd., CH-3001 Berne, Switzerland |
| |
Abstract: | 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. |
| |
Keywords: | |
本文献已被 ScienceDirect 等数据库收录! |