HCID 59733723, compound → HCID 59733718, compound

Participants

Reaction Conditions

Reaction Steps

To a sealed tube was added a solution of 5-(3-tert-butyl-phenyl)-2-(toluene-4-sulfonyl)-4,5,6,7-tetrahydro-2H-indazol-5-ylamine (0.41 g, 1.0 mmol) in isopropyl alcohol followed by 2-[2-(3,5-difluoro-phenyl)-ethyl]-oxirane (0.18 g, 1.0 mmol). The reaction was heated at 50° C. overnight and no product was formed. After heating at 100° C. for an additional 3.5 h the reaction was complete. The reaction mixture was concentrated and the crude product was purified by flash chromatography, eluting with 3% methanol in CHCl3 to afford 0.25 g (0.41 mmol, 42%) of 1-[5-(3-tert-butyl-phenyl)-2-(toluene-4-sulfonyl)-4,5,6,7-tetrahydro-2H-indazol-5-ylamino]-4-(3,5-difluoro-phenyl)-butan-2-ol: retention time (min)=2.15, method [1]. MS (ESI) 608.4 (M+H).

Provenance & Evidence