Abstract Peptide chloromethyl esters are important compounds in prodrug synthesis. A simple, mild and efficient method for the synthesis of chloromethyl esters of N-blocked amino acids and dipeptides using exclusively bromochloromethane is reported. These N-blocked amino acid and dipeptide chloromethyl esters react readily with the carboxylic acid group of aspirin and with the sulfonamido group of
摘要 肽氯甲酯是前药合成中的重要化合物。报道了一种仅使用溴氯甲烷合成 N 封闭氨基酸和二肽的氯甲酯的简单、温和且有效的方法。这些 N 封闭的氨基酸和二肽氯甲酯很容易与阿司匹林的羧酸基团和抗疟药磺胺二甲嘧啶的磺胺基反应,得到相应的前药。
Kinetically Controlled Peptide Synthesis Mediated by Papain Using the Carbamoylmethyl Ester as an Acyl Donor
carbamoylmethyl (Cam) esters as acyldonors in the presence of a cysteine protease, papain, immobilized on Celite. Several segment condensations were also achieved generally in high yields without danger of racemization and formation of the secondary-hydrolysis product. Moreover, partial sequences of some bioactive peptides were prepared through segment condensations, and aimed-at peptides were obtained generally