反应详情

N-Chlorosuccinimide (239 mg, 1.77 mmol) was added to a solution of 1-methyl-3-(2-methylsulfanyl-pyrimidin-4-yl)-1H-indazole (413 mg, 1.6 mmol) in NMP, and the resulting mixture was stirred at 85° C. for 15 min. trans-Aminocyclohexanol was then added, the reaction mixture stirred for 1 h, then poured into water and extracted twice with EtOAc. The combined organic extracts were dried over Na2SO4, filtered, and evaporated under reduced pressure. The crude residue was purified by preparative TLC to give trans-4-[4-(1-methyl-1H-indazol-3-yl)-pyrimidin-2-ylamino]-cyclohexanol. MS=324 [M+H]+; MP=180-183.3° C. (Compound 77).

1. additionwas then added
2. extractionextracted twice with EtOAc
3. dry with materialThe combined organic extracts were dried over Na2SO4
4. filtrationfiltered
5. customevaporated under reduced pressure
6. customThe crude residue was purified by preparative TLC