Ammonia → HCID 86670413, compound

Participants

Reaction Conditions

Reaction Steps

A 5-mL microwave vial was charged with N-(((2R)-4-((6-chloro-3-pyridinyl)sulfonyl)-1-(5-(2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl)-2-pyrimidinyl)-2-piperazinyl)methyl)-N-phenylmethanesulfonamide (0.134 g, 0.194 mmol, step 1) and 2M NH3 in MeOH (2 mL). The reaction mixture was heated in an Initiator microwave reactor (Biotage AB, Inc., Uppsala, Sweden) at 140° C. for 3 h. Then the mixture was then heated at 130° C. (thermal) for 12 h. The solvent was removed and the crude product was purified by column chromatography (25 g of silica gel, 10 to 90% EtOAc in hexanes) to afford N-(((2R)-4-((6-amino-3-pyridinyl)sulfonyl)-1-(5-(2,2,2-trifluoro-1-hydroxy-1-(trifluoromethyl)ethyl)-2-pyrimidinyl)-2-piperazinyl)methyl)-N-phenylmethanesulfonamide (0.0385 g) as a white solid.

Provenance & Evidence