反应详情

To a solution of the crude 2-cyano-4-(methylspiro[2.5]oct-6-ylmethylamino)pyrimidine-5-carboxylic acid (82 mg, step 73.4) in DMF (1.5 mL) are added (R)-2-phenyl-1-pyrrolidin-1-ylmethylethylamine (0.3 mmol), EDCI-HCl (0.4 mmol), and HOAt (0.4 mmol) at room temperature. The reaction mixture is stirred for 24 h and the reaction is quenched by the addition of water. The mixture is extracted with AcOEt and the organic extracts are dried over Na2SO4, filtered, concentrated in vacuo. The resulting residue is purified by RP-HPLC to give the title compound; MS (M+1)+ 488, Rf (solvent) 0.13 (CH2Cl2:MeOH=10:1).

1. customthe reaction is quenched by the addition of water
2. extractionThe mixture is extracted with AcOEt
3. dry with materialthe organic extracts are dried over Na2SO4
4. filtrationfiltered
5. concentrationconcentrated in vacuo
6. customThe resulting residue is purified by RP-HPLC