Rhodium(II) acetate-catalysed decomposition of 2-diazo-3-oxobutanamides derived from L-phenylalanine
摘要:
In order to developed a practical method for alkylating alpha-amino acids at the alpha- or beta-carbon atom by intramolecular carbene C-H insertion, a series of diazoamides 3a-e was synthesized and subjected to rhodium(II) acetate-catalysed decomposition. The N-benzyl derivative 3a gave mainly the azetidinones 4a and 5a, resulting from a carbene C-H insertion into the N-benzyl group. The N-diphenylmethyl derivative 3c yielded, upon treatment with rhodium(II) acetate, the azetidinone 5c, the imine 6c, the cycloheptapyrrolidinone 7c as well as the desired pyrrolidinone 8c (22% yield) the latter resulting from an alkylation of the L-phenylalanine framework at the beta-carbon atom.
Facile synthesis of pyrazino[2,3-e][1,4]diazepine derivatives via the intramolecular aza-Wittig reaction
作者:Tomohiro Okawa、Shoji Eguchi
DOI:10.1016/0040-4039(95)02107-8
日期:1996.1
Pyrazino[2,3-e][1,4]diazepine derivatives were synthesized from 3-aminopyrazine-2-carboxylic acid 1 and α-amino acid esters via the intramolecular aza-Wittig reaction.
通过分子内的氮杂-Wittig反应,由3-氨基吡嗪-2-羧酸1和α-氨基酸酯合成吡嗪并[2,3- e ] [1,4]二氮杂derivatives衍生物。
Hydantoin derivative as metalloprotease inhibitor
申请人:FUJIREBIO INC.
公开号:EP0640594A1
公开(公告)日:1995-03-01
A hydantoin derivative represented by formula (I):
wherein the all symbols are defined in the disclosure. The hydantoin derivative has an inhibitory activity on metalloprotease and hence is useful as analgesic and cardiovascular drug.