Lithium borohydride → HCID 67327561, compound

Participants

Reaction Steps

To a stirred solution of (3SR,4RS)-4-(3,4-dichloro-phenyl)-1-(4-methanesulfonyl-piperazine-1-carbonyl)-pyrrolidine-3-carboxylic acid ethyl ester (2.39 g, 5.00 mmol) in MeOH (80 mL) at RT was added LiBH4 (434 mg, 19.9 mmol). After 2 hours a second portion of LiBH4 (1.30 g, 59.7 mmol) was added and stirring was continued for 2 days. The reaction mixture was poured on H2O, extracted with EtOAc and the combined organic phases were dried over Na2SO4. Flash chromatography (SiO2, EtOAc, then EtOAc/MeOH 9:1) yielded the title product (1.76 g, 81%) as a white solid. ES-MS m/e: 436.1 (M+H+).

Provenance & Evidence