反应详情

A solution of 3-trifluoromethyl-1H-pyrazole-4-carboxylic acid (adamantan-1-ylmethyl)-amide (100 mg, 0.306 mmol), 2-chloro-5-fluoro-pyrimidin-4-ylamine (52 mg, 0.35 mmol) and Cs2CO3 (130 mg, 0.4 mmol) in NMP (1.0 mL) is heated in a microwave reactor at 150° C. for 1 h. The mixture is poured into H2O. The crude product is filtered out, dissolved in 10% MeOH in DCM, and dried over anhydrous Na2SO4. The title compound is purified by PTLC (eluted with 5% MeOH in DCM). 1H NMR (CD3OD): 8.96 (s, 1H), 8.11 (s, 1H), 3.0 (s, 2H), 1.98 (m, 3H), 1.78-1.68 (m, 6H), 1.58 (s, 611). MS (M+1)=439.29; RT=1.34 min. *IC50.

1. filtrationThe crude product is filtered out
2. dissolutiondissolved in 10% MeOH in DCM
3. dry with materialdried over anhydrous Na2SO4
4. customThe title compound is purified by PTLC (eluted with 5% MeOH in DCM)