Reacción #11056

Ecuación de reacción

intermediate 1k

(6S)-[(4-{[(3-benzylamino-4-oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrimidine-6-carbonyl)-amino]-methyl}-phenyl)-imino-methyl]-carbamic acid tert-butyl ester

intermediate 1j

(S)-[(4-{[(3-amino-4-oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrimidine-6-carbonyl)-amino]-methyl}-phenyl)-imino-methyl]-carbamic acid tert-butyl ester

acetaldehyde

NaBH(OAc)3

→

intermediate 5a

Rendimiento 60.5%

(S)-[(4-{[(3-ethylamino-4-oxo-4,6,7,8-tetrahydro-pyrrolo[1,2-a]pyrimidine-6-carbonyl)-amino]-methyl}-phenyl)-imino-methyl]-carbamic acid tert-butyl ester

Rendimiento 60.5%

Condiciones de reacción

Procedimiento

Following a procedure similar to that for the preparation of intermediate 1k, intermediate 1j (101 mg, 0.24 mmol), acetaldehyde (21.1 mg, 0.48 mmol) and NaBH(OAc)3 (141.99 mg, 0.67 mmol) yielded 66 mg (60.5%) of intermediate 5a. MS (ESI) 455.1 (M+H+).

Fuente