反应详情

A solution of 4-{5-[2-amino-7-methyl-8-(3-trifluoromethyl-phenyl)-[1,2,4]triazolo[1,5-a]pyridin-6-yl]-pyrazol-1-yl}-benzonitrile (Ex. 1, 100 mg, 0.218 mmol) and ethyl chloroformate (104 μL, 1.089 mmol) in pyridine (2.5 mL) was heated at 120° C. for 20 mins using microwave irradiation. The reaction mixture was azeotroped with toluene in vacuo. The resultant residue was subjected to preparative C18 HPLC, eluting with a gradient of 40-80% MeCN in water (+0.1% formic acid) to give the title compound as a white solid (24 mg).

1. custommicrowave irradiation
2. customThe reaction mixture was azeotroped with toluene in vacuo
3. washeluting with a gradient of 40-80% MeCN in water (+0.1% formic acid)