Department of Chemistry, Molecular Sciences Research Hub, Imperial College London, White City Campus, 82 Wood Lane, London W12 0BZ, U.K.
Org Lett. 2022 Feb 11;24(5):1175-1179. doi: 10.1021/acs.orglett.1c04265. Epub 2022 Jan 27.
Methyltrimethoxysilane [MTM, CHSi(OMe)] has been demonstrated to be an effective, inexpensive, and safe reagent for the direct amidation of carboxylic acids with amines. Two simple workup procedures that provide the pure amide product without the need for further purification have been developed. The first employs an aqueous base-mediated annihilation of MTM. The second involves simple product crystallization from the reaction mixture providing a low process mass intensity direct amidation protocol.
甲基三甲氧基硅烷(MTM,CHSi(OMe))已被证明是一种有效、廉价且安全的试剂,可用于羧酸与胺的直接酰胺化反应。已经开发出两种简单的后处理程序,可提供纯净的酰胺产物,而无需进一步纯化。第一种方法采用水基介导的 MTM 消除反应。第二种方法涉及从反应混合物中简单地进行产物结晶,提供了一种低过程质量强度的直接酰胺化方法。