Trifluoroacetic acid → 2-{5H,6H,7H,8H-[1,2,4]triazolo[4,3-a]pyrazin-3-yl}pyridine
反応式
[N:1]1[CH:6]=[CH:5][CH:4]=[CH:3][C:2]=1[C:7]1[N:11]2[CH2:12][CH2:13][N:14](C(OC(C)(C)C)=O)[CH2:15][C:10]2=[N:9][N:8]=1.C(O)(C(F)(F)F)=O>ClCCl>[N:1]1[CH:6]=[CH:5][CH:4]=[CH:3][C:2]=1[C:7]1[N:11]2[CH2:12][CH2:13][NH:14][CH2:15][C:10]2=[N:9][N:8]=1参加物
4
実験手順
To a solution of 1,1-dimethylethyl 3-(2-pyridinyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazine-7(8H)-carboxylate (I100)(115 mg, 0.382 mmol) in dichloromethane (DCM) (1 mL), TFA (0.588 mL, 7.63 mmol) was added and mixture was stirred at RT for 3 h. Volatiles removed under reduced pressure and residue purified by SCX cartridge eluting first with MeOH and then with 2.0N NH3 in MeOH. Ammonia fractions were concentrated under reduced pressure yielding desired product as a pale yellow solid.60 mg.