تفاعل #159683

معادلة التفاعل

tert-butyl 4-(3-((1-(5-chloro-3-((1-(4-(methoxycarbonyl)phenyl)cyclopropyl)carbamoyl)pyridin-2-yl)azetidin-3-yl)oxy)phenyl)piperazine-1-carboxylate

trifluoroacetic acid dichloromethane

→

title compound ( D156 )

المردود 95.3%

methyl 4-(1-(5-chloro-2-(3-(3-(piperazin-1-yl)phenoxy)azetidin-1-yl)nicotinamido)cyclopropyl)benzoate

المردود 95.3%

المذيبات

dichloromethane

ظروف التفاعل

المعالجة

1. 1
   أخرىSolvents were evaporated in vacuo
2. 2
   أخرىto afford a residue that
3. 3
   أخرىAmmonia fractions after solvent evaporation

الإجراء التجريبي

To a cooled solution of tert-butyl 4-(3-((1-(5-chloro-3-((1-(4-(methoxycarbonyl)phenyl)cyclopropyl)carbamoyl)pyridin-2-yl)azetidin-3-yl)oxy)phenyl)piperazine-1-carboxylate (130 mg, 0.196 mmol) in dichloromethane (1 ml) a mixture trifluoroacetic acid/dichloromethane (3 ml/1 ml) was added and the resulting mixture stirred for 15 min. Solvents were evaporated in vacuo to afford a residue that was loaded on SPE-SCX (5 g) cartridge. Ammonia fractions after solvent evaporation afforded the title compound (D156) (105 mg)

المصدر