四川师范大学学报（自然科学版）2013，Vol.36Issue(2)：275-279,5.DOI:10.3969/j.issn.1001-8395.2013.02.025
N-甲基二肽N-Ns-N(Me)-L-Ala-N(Me)-L-Ile-OtBu的合成研究
Study on the Synthesis of N-methyldipeptide N-Ns-N (Me)-L-Ala-N (Me)-L-Ile-OtBu
摘要
Abstract
A N-methylated peptide amide bond often exhibits higher resistance to proteolysis and thus results in improved oral activity and enhanced duration of action. However, few N-methyl amino acids are commercially available and their synthesis is tedious. The formation of hindered amide bond with high yield and minimal racemization is often troublesome. Herein the hindered N-methyl-dipeptide ( N-Ns-N( Me) -L-Ala-N( Me) -L-Ile-O'Bu) , a segment of the new cyclodepsipeptide Apratoxin A, which exhibits cytotoxycity against human tumor cell lines, was synthesized from L-Alanine and L-iso-Leucine through ten steps. The coupling reaction needs not any catalyst and proceeds effectively, so the workup procedure is quite simple.关键词
邻硝基苯磺酰氯/L-丙氨酸/L-异亮氨酸/N-甲基二肽Key words
2-nitrobenzenesulfonyl chloride/ L-alanine/ L-iso-leucine/ N-methyldipeptide分类
化学化工引用本文复制引用
王晓季,唐琳钧,吕常山,陈世鹏,冯俊敏..N-甲基二肽N-Ns-N(Me)-L-Ala-N(Me)-L-Ile-OtBu的合成研究[J].四川师范大学学报（自然科学版）,2013,36(2):275-279,5.基金项目
江西省自然科学基金(2010GZH0042)资助项目 （2010GZH0042）
