반응 #2175376

반응 방정식

1-phenyl-8-azabicyclo[3.2.1]octan-6-carboxylic acid trifluoroacetate

(1R*,2R*,5S*,6R*)-2-{[3,5-Bis(trifluoromethyl)phenyl]methoxy}-1-phenyl-8-azabicyclo[3.2.1]octan-6-carboxylic acid trifluoroacetate

N-benzylpiperazine

triethylamine

1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride

→

title compound

수율 85.0%

(1R*,2R*,5S*,6R*)-6-[(4-Benzylpiperazin-1-yl)carbonyl]-2-{[3,5-bis(trifluoromethyl)phenyl]methoxy}-1-phenyl-8-azabicyclo[3.2.1]octane

수율 85.0%

반응 조건

후처리

1. 1
   기타was prepared
2. 2
   기타purified by chromatography on silica gel (dichloromethane:methanol)

실험 절차

A mixture of (1R*,2R*,5S*,6R*)-2-[3,5-bis(trifluoromethyl)phenyl]methoxy)-1-phenyl-8-azabicyclo[3.2.1]octan-6-carboxylic acid trifluoroacetate (Example 122; 100 mg, 0.19 mmol), N-benzylpiperazine (0.1 ml), triethylamine (0.1 ml, 0.7 mmol), 1-(3-dimethylaminopropyl)-3-ethylcarbodiimide hydrochloride (44 mg, 0.23 mmol) and 4-N,N-dimethylaminopyridine (12 mg, 0.1 mmol)was prepared. The mixture was stirred at room temperature for 20 hours and purified by chromatography on silica gel (dichloromethane:methanol) to give the title compound (102 mg, 85%).

출처