3-{1-[6-(4-Amino-3-methyl-5-nitro-phenoxy)-pyrimidin-4-yl]-piperidin-4-yl}-7-methoxy-1,3,4,5-tetrahydro-benzo[d][1,3]diazepin-2-one → 3-{1-[6-(3,4-Diamino-5-methyl-phenoxy)-pyrimidin-4-yl]-piperidin-4-yl}-7-methoxy-1,3,4,5-tetrahydro-benzo[d][1,3]diazepin-2-one

Participants

Reaction Steps

830 mg (1.60 mmol) 3-{1-[6-(4-amino-3-methyl-5-nitro-phenoxy)-pyrimidin-4-yl]-piperidin-4-yl}-7-methoxy-1,3,4,5-tetrahydro-benzo[d][1,3]diazepin-2-one in 20 mL MeOH were combined with 100 mg palladium on charcoal (Pd/C 10%) and hydrogenated for 8 h under a hydrogen atmosphere of 50 psi. After the catalyst had been removed by suction filtering, the filtrate was evaporated down and the residue was reacted further as the crude product.

Provenance & Evidence