Hydrochloric Acid → N-Cyclopropyl-2-(4-piperidin-4-yl-phenyl)-propionamide
Reaction equation
C(OC([N:8]1[CH2:13][CH2:12][CH:11]([C:14]2[CH:19]=[CH:18][C:17]([CH:20]([C:22](=[O:27])[NH:23][CH:24]3[CH2:26][CH2:25]3)[CH3:21])=[CH:16][CH:15]=2)[CH2:10][CH2:9]1)=O)(C)(C)C.Cl>CO>[CH:24]1([NH:23][C:22](=[O:27])[CH:20]([C:17]2[CH:18]=[CH:19][C:14]([CH:11]3[CH2:10][CH2:9][NH:8][CH2:13][CH2:12]3)=[CH:15][CH:16]=2)[CH3:21])[CH2:25][CH2:26]1Participants
4
Procedure
To 3.40 g (9.13 mmol) 4-[4-(1-cyclopropylcarbamoyl-ethyl)-phenyl]-piperidine-1-carboxylic acid tert-butyl ester (X.1) in 20 mL methanol are added 10.9 mL (13.7 mmol) 1.25 M HCl in methanol. The mixture is stirred for 12 h at rt. After that time, 2.0 mL 1.25 M HCl in methanol are added and the mixture is stirred for 2 d at 40° C. After that time, the solvent is evaporated, the residue taken up in 1N NaOH and extracted with EtOAc. After drying over sodium sulphate, the solvent is removed in vacuo to yield the desired product.