Synthesis of N-sulfonylamidines via three-component reaction of proline, aldehydes, and sulfonyl azides under metal-free conditions

摘要

Synthesis of N-sulfonylamidines was performed by three-component coupling reaction of proline, aldehydes, and sulfonyl azides under mild conditions. In this reaction, using acetophenone as a representative ketone instead of aldehydes gave the desired product albeit in low yield. During our mechanistic studies, we trapped the nitrene as the key intermediate using PPh3. This simple and practical approach could be applied for the synthesis of biologically active molecules having N-sulfonylamidine moiety. [GRAPHICS]