反应详情

Cis-4-Benzyloxycarbonylamino-3-[4-(2-oxo-2H-pyridin-1-yl)-benzoylamino]-piperidine-1-carboxylic acid tert-butyl ester (22.2 mg, 0.041 mmol) was dissolved in 2 mL of anhydrous CH2Cl2 To this solution was added 2 mL of trifluoroacetic acid (TFA). The mixture was stirred for one hour at rt. The solvent was removed in vacuo to yield cis-{3-[4-(2-Oxo-2H-pyridin-1-yl)-benzoylamino]-piperidin-4-yl}-carbamic acid benzyl ester, CF3COOH salt (42.7 mg) as a viscous oil, which was used without any further purification. Anal. LC/MS (ESI) Shimadzu Phenomenex C18; 4.6×50 mm Luna; flow rate 4 mL/mn; detection at 220 nM; Gradient elution 0% to 100% B over 4 min; (A=10% MeOH, 90% H2O, 0.1% TFA & B=90% MeOH, 10% H2O, 0.1% TFA); 447.24 (M+H)+, tR=2.15 min.

1. customThe solvent was removed in vacuo