A sequential addition-cyclization reaction between carboxylic acids, crotonate sulfonium salts, and amines has been developed for the construction of 1,2,3-trisubstituted pyrroles. The reaction involves regioselective addition of crotonate sulfonium salts directly to in situ-activated carboxylic acids to construct the first C-C bond, followed by cyclization with a primary amine to create the two C-N bonds in one pot. The new transformation appears to have a general substrate scope, uses readily accessible starting materials, and proceeds rapidly at room temperature. The reaction is versatile and scalable, making it suitable for applications in process and medicinal chemistry.
Chavan et al. (Mon,) studied this question.
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