반응 #11055

반응 방정식

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

acetone

NaBH(OAc)3

→

intermediate 4a

수율 65.0%

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

수율 65.0%

반응 조건

실험 절차

Following a procedure similar to that for the preparation of intermediate 1k, intermediate 1j (60 mg, 0.14 mmol), acetone (97.6 mg, 1.68 mmol) and NaBH(OAc)3 (385.7 mg, 1.82 mmol) yielded 43 mg (65%) of intermediate 4a. MS (ESI) 469.1 (M+H+).

출처