氯化铵促进的5-亚氨基恶唑啉的三组分合成及其随后向大环缩肽的转化。

Ammonium chloride promoted three-component synthesis of 5-iminooxazoline and its subsequent transformation to macrocyclodepsipeptide.

作者信息

Pirali Tracey, Tron Gian Cesare, Masson Géraldine, Zhu Jieping

机构信息

Dipartimento di Scienze Chimiche, Alimentari, Farmaceutiche e Farmacologiche and Drug and Food Biotechnology Center, Università degli Studi del Piemonte Orientale A. Avogadro, Via Bovio 6, 28100 Novara, Italy.

出版信息

Org Lett. 2007 Dec 6;9(25):5275-8. doi: 10.1021/ol7024372. Epub 2007 Nov 9.

DOI:10.1021/ol7024372

PMID:17990892

Abstract

A three-component reaction of an alpha,alpha-disubstituted alpha-isocyanoacetamide, an aldehyde and an amino alcohol afforded the 5-iminooxazoline, which, upon saponification, cyclized under acidic conditions to provide the macrocyclodepsipeptide in good overall yield.

摘要

α,α-二取代的α-异氰基乙酰胺、醛和氨基醇的三组分反应生成了5-亚氨基恶唑啉，该产物经皂化后在酸性条件下环化，以良好的总收率得到大环缩肽。