Acetic Acid → (R)-methyl 4-(1-(1-(4-fluoro-3-methylbenzyl)piperidine-2-carboxamido)cyclopropyl)benzoate

Participants

Reaction Conditions

Reaction Steps

A mixture of (R)-methyl 4-(1-(piperidine-2-carboxamido)cyclopropyl)benzoate (D13) (40 mg, 0.13 mmol) and 4-fluoro-3-methyl benzaldehyde (0.02 ml, 0.16 mmol), NaBH(OAc)3 (84 mg, 0.4 mmol) and CH3COOH (0.076 ml, 1.3 mmol) in DCM (10 ml) was heated at 110° C. (2 cycles of 5 min each) under microwave irradiation. The resulting mixture was purified by SPE-Si (2 g) eluting with a mixture DCM/AcOEt from 100/0 to 80/20. Collected fractions after solvent evaporation afforded the title compound (D29) (33 mg).

Provenance & Evidence