تفاعل #78351

معادلة التفاعل

4-amino-4-phenylpiperidine dibenzenesulfonate

compound

1-Benzoyl-3-(3,4-dichlorophenyl)-3-[3-[4-(pyrrolidin-1-ylcarbonyl)piperid-1-yl]propyl]piperidine Hydrochloride

K2CO3

→

expected product

المردود 74.6%

3-[3-(4-Amino-4-phenylpiperid-1-yl)propyl]-1-benzoyl-3-(3,4-dichlorophenyl)-piperidine

المردود 74.6%

المذيبات

DMF acetonitrile

ظروف التفاعل

المعالجة

1. 1
   تركيزIt is concentrated under vacuum
2. 2
   استخلاصextracted with AcOEt
3. 3
   غسيلthe organic phase is washed with water and with saturated NaCl solution
4. 4
   تجفيفdried over MgSO4
5. 5
   أخرىthe solvent is evaporated off under vacuum
6. 6
   أخرىThe residue is chromatographed on silica H

الإجراء التجريبي

A mixture of 6.81 g of 4-amino-4-phenylpiperidine dibenzenesulfonate, 5.2 g of the compound obtained in step B of EXAMPLE 1 and 6.1 g of K2CO3 in 30 ml of a DMF/acetonitrile mixture (50/50; v/v) is heated at 100° C. for 5 hours. It is concentrated under vacuum, the residue is taken up with water and extracted with AcOEt, the organic phase is washed with water and with saturated NaCl solution and dried over MgSO4 and the solvent is evaporated off under vacuum. The residue is chromatographed on silica H using a DCM/MeOH mixture (from 99/1; v/v to 85/15; v/v) as the eluent to give 3.6 g of the expected product.

المصدر