1-(2-methanesulfonyl-pyrimidin-4-yl)-3-methoxy-1H-indazole → HCID 178494301, compound

Participants

Reaction Conditions

Reaction Steps

trans-4-Aminocyclohexanol (870 mg, 8 mmol) was added to 1-(2-methanesulfonyl-pyrimidin-4-yl)-3-methoxy-1H-indazole (440 mg, 1 mmol) in NMP (15 mL), and the resulting mixture heated to 120° C. for 3 h. The reaction mixture was cooled and partitioned between EtOAc and water. The organic layer was separated, washed with water, dried over Na2SO4, filtered, and concentrated under reduced pressure to give a crude yellow solid. This crude material was purified by flash chromatography (MeOH/DCM, 5:95) and recrystallized from DCM/hexanes to give trans-4-[4-(3-methoxy-indazol-1-yl)-pyrimidin-2-ylamino]-cyclohexanol (181 mg (37% yield) as a white solid. MS=340 [M+H]+; MP=202.3-205.1° C.

Provenance & Evidence