LAUSR

N′‐alkyl benzohydrazides are classic organic compounds that have been widely utilized in organic chemistry. In this study, an efficient method was developed for the synthesis of N′‐alkyl benzohydrazides by hydrazine insertion catalyzed by lipase. Under the optimal conditions (Morita–Baylis–Hillman ketone [1 mmol], phenylhydrazine [1.3 mmol], N,N‐dimethylformamide [2 ml], lipase [20 mg], room temperature, 12 h), satisfactory yields (71–97%) and substrate tolerance were obtained when porcine pancreatic lipase was used as biocatalyst. These findings imply the great potential for the lipase‐catalyzed synthesis of N′‐alkyl benzohydrazides and extend the utilization of lipase in organic chemistry.