Demonstrates efficient N-ethylation and N-acetylation methods in secondary amines, suggesting practical applications in drug synthesis.
We herein describe an efficient and highly selective N-ethylation and N-acetylation of secondary amines using sodium triacetoxyborohydride [NaBH(OAc)3] as alkyl and acetyl sources, which were controlled by the solvent. High isolated yields were obtained for a series of N-substituted amine substrates with flash column chromatographic purification. The practicability of the methodology was demonstrated by synthesizing an approved drug, and the mechanism was proposed based on experiments.
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Wang et al. (2026) studied this question.
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