Facile hydrolysis and formation of amide bonds by N-hydroxyethylation of α-amino acids
摘要:
The C-terminal amides of alpha-amino acids are readily hydrolyzed at 25 degrees and pH 7 when the N-terminus is N-hydroxyethylated, with one or two hydroxyethyl groups. The reaction proceeds via cyclization to a morpholinolactone (2) which is rapidly hydrolyzed by water. In the presence of equimolar amounts of amines or amino acid derivatives, 2 reacts in H2O without condensing agents to form a new peptide bond. (C) 1997 Elsevier Science Ltd.
Facile hydrolysis and formation of amide bonds by N-hydroxyethylation of α-amino acids
作者:J.William Suggs、Richard M. Pires
DOI:10.1016/s0040-4039(97)00330-4
日期:1997.3
The C-terminal amides of alpha-amino acids are readily hydrolyzed at 25 degrees and pH 7 when the N-terminus is N-hydroxyethylated, with one or two hydroxyethyl groups. The reaction proceeds via cyclization to a morpholinolactone (2) which is rapidly hydrolyzed by water. In the presence of equimolar amounts of amines or amino acid derivatives, 2 reacts in H2O without condensing agents to form a new peptide bond. (C) 1997 Elsevier Science Ltd.
Preparation of Derivatives of Nitrogen Mustard having Structure of α-Amino Acid Amide
作者:Yoshio Sakurai、Eiichi Matsui
DOI:10.1248/cpb.13.594
日期:——
A number of new amide derivatives of bis(2-chloroethyl)-DL-glycine and bis(2-chloroethyl)-DL-alanine were prepared and tested for their in vivo and in vitro antitumor activity against Yoshida Sarcoma, and chemical properties.