Weinreb酰胺是合成一些结构有意义或有生物活性的手性化合物的重要中间体,它可与有机金属试剂反应生成酮,又可被二异丁基铝氢(DIBAL-H),氢化铝锂(Li Al H4)等还原成醛,现已被普遍应用于全合成化学、药物化学以及生物有机化学等领域。因...Weinreb酰胺是合成一些结构有意义或有生物活性的手性化合物的重要中间体,它可与有机金属试剂反应生成酮,又可被二异丁基铝氢(DIBAL-H),氢化铝锂(Li Al H4)等还原成醛,现已被普遍应用于全合成化学、药物化学以及生物有机化学等领域。因此,研究Weinreb酰胺的合成具有重大意义。本文综述了以羧酸、羧酸衍生物等为原料制备Weinreb酰胺的方法并对制备Weinreb酰胺的方法进行了展望。展开更多
An unexpected decarboxamidation of a-arylsulfonyl Weinreb amides as a side reaction under the standardacylating conditions was found in Weirtreb amides chemistry. The control experiments for mechanism study disclosedt...An unexpected decarboxamidation of a-arylsulfonyl Weinreb amides as a side reaction under the standardacylating conditions was found in Weirtreb amides chemistry. The control experiments for mechanism study disclosedthat a-sulfo group was necessary, and a-quaternary carbon was the key factor for the reaction. Meanwhile, an effi-cient method was established for the preparation of secondary alkyl arylsulfones by this unexpected C--C bondcleavage reaction using excess Grignard reagent.展开更多
文摘Weinreb酰胺是合成一些结构有意义或有生物活性的手性化合物的重要中间体,它可与有机金属试剂反应生成酮,又可被二异丁基铝氢(DIBAL-H),氢化铝锂(Li Al H4)等还原成醛,现已被普遍应用于全合成化学、药物化学以及生物有机化学等领域。因此,研究Weinreb酰胺的合成具有重大意义。本文综述了以羧酸、羧酸衍生物等为原料制备Weinreb酰胺的方法并对制备Weinreb酰胺的方法进行了展望。
文摘An unexpected decarboxamidation of a-arylsulfonyl Weinreb amides as a side reaction under the standardacylating conditions was found in Weirtreb amides chemistry. The control experiments for mechanism study disclosedthat a-sulfo group was necessary, and a-quaternary carbon was the key factor for the reaction. Meanwhile, an effi-cient method was established for the preparation of secondary alkyl arylsulfones by this unexpected C--C bondcleavage reaction using excess Grignard reagent.
