Sodium triacetoxyborohydride → HCID 16048762, compound

Participants

Reaction Steps

To a solution of 1-[4-(5,6,7,8-tetrahydropyrazolo[3,4-d]azepin-2(4H)-yl)phenyl]-2-pyrrolidinone (may be prepared as described in Description 22) (55 mg, 0.10 mmol) in dichloromethane (5 ml) was added cyclopropylacetaldehyde (26 mg, 0.30 mmol) and acetic acid (3 drops). The resulting mixture was stirred at room temperature, under argon, for 20 minutes. Sodium triacetoxyborohydride (64 mg, 0.30 mmol) was added and stirring continued for 18 hours. The resulting crude mixture was diluted with methanol and then purified by SCX, eluting with methanol and then with 2M ammonia/methanol. The basic fractions were collected and solvent evaporated in vacuo. Crude product was triturated with ethyl acetate to afford the title compound (E19). MS (ES+) m/e 351 [M+H]+.

Provenance & Evidence