HCID 86723483, compound → HCID 77107224, compound

Participants

Reaction Steps

A mixture of 10-(4-Chlorothiazol-2-yl)-5-(3-fluorophenyl)-8-(hydroxymethyl)-1,3-dimethyl-7,8-dihydropyrimido[4,5-a]indolizine-2,4(1H,3H)-dione (310 mg, 0.66 mmol) and 10% platinum on carbon (310 mg) in ethanol (22 mL) and tetrahydrofuran (22 mL) was stirred under an atmosphere of hydrogen for 3 days. The reaction mixture was filtered and the filtrates concentrated under vacuum. The residue was dissolved in ethanol (22 mL) and tetrahydrofuran (22 mL), fresh 10% platinum on carbon (310 mg) was added and the mixture further stirred under an atmosphere of hydrogen for 5 days. The reaction mixture was filtered and the filtrates evaporated under vacuum. The residue was dissolved in 10 mL of 5% MeOH/DCM and the solution was treated with silica-TMT (trimercaptotriazine functionalized silica, ˜1 g) for 5 minutes, then filtered. The residue was washed with 5% MeOH/DCM and the filtrates evaporated under vacuum.

Provenance & Evidence