Laboratoire de Glycochimie et de Synthèse Asymétrique, Swiss Federal Institute of Technology (EPFL) , Batochime, CH 1015 Lausanne, Switzerland.
Org Lett. 2014 Jan 17;16(2):604-7. doi: 10.1021/ol403508j. Epub 2014 Jan 3.
An efficient method has been developed for the direct amidification of carboxylic acids via sulfinylamides preformed in situ by the reaction of pure amines with prop-2-ene-1-sulfinyl chloride. The method can be applied to aliphatic acids, including pivalic acid, aromatic acids, and primary and secondary amines. It is compatible with acids bearing unprotected alcohol, phenol, and ketone moieties and applicable to the synthesis of peptides. It does not induce their α-epimerization.
已经开发出一种有效的方法，通过纯胺与丙烯-2-磺酰氯反应原位形成的亚磺酰胺，直接将羧酸进行酰胺化。该方法适用于包括特戊酸在内的脂肪族酸、芳香族酸以及伯胺和仲胺。它与未保护的醇、酚和酮部分的酸兼容，适用于肽的合成。它不会诱导它们的α-差向异构化。
