Enantioselective Synthesis of (R)-Homoboroproline from (S)-Proline Using a Borylation Approach

[摘要]：(S)-Proline was converted through a five-step sequence into (R)-homoboroproline hydrochloride in 29?% overall yield with 97?%?ee The key step was the conversion of N-Boc iodomethylpyrrolidine into the corresponding pinacol boronate ester by an efficient copper(I)-catalyzed borylation reaction by using bispinacolatodiboron.

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