1-Methylpiperazine → HCID 44611001, compound

Participants

Reaction Conditions

Reaction Steps

(S)-2-(1-(4-Bromophenyl)ethylamino)-9-cyclopentyl-5,7,7-trimethyl-8,9-dihydro-5H-pyrimido[4,5-b][1,4]diazepin-6(7H)-one (100 mg, 0.2117 mmol), 1-methylpiperazine (84.82 mg, 93.93 μL, 0.8468 mmol), di-tert-butyl-(2-phenylphenyl)phosphane (6.317 mg, 0.02117 mmol) and K3PO4 (89.87 mg, 0.4234 mmol) were taken in up DME (2 mL) and degassed using cycles of vacuum and nitrogen. Pd2DBA3 (19.39 mg, 0.02117 mmol) was added and the reaction mixture was further degassed and then heated at 100° C. in a sealed tube for 4 hours and then allowed to cool to the ambient temperature. The reaction mixture was then diluted with ethyl acetate (5 mL) and filtered. The filtrate was concentrated in vacuo and the residue purified by mass directed HPLC and the combined product fractions passed through a bicarbonate cartridge and lypholized to give the title compound as a white solid (9.9 mg, 10% yield).

Provenance & Evidence