تفاعل #215778

معادلة التفاعل

1-(2-Methoxy-4-(1-ethenylsulfonyl-4-piperidyloxy)phenylacetyl)-4-(2-methylphenyl)piperazine-2-carboxamide

cyclopropylamine

cyclopropylamine

→

1-(2-methoxy-4-(1-(2-(N-cyclopropylamino)ethylsulfonyl)-4-piperidyloxy)phenylacetyl)-4-(2-methylphenyl)piperazine-2-carboxamide

المذيبات

methanol

ظروف التفاعل

المعالجة

1. 1
   workup.STIRRINGthe mixture stirred another 72 hours at ambient temperature
2. 2
   تركيزThe reaction was concentrated in vacuo
3. 3
   أخرىthe residue was chromatographed on silica gel
4. 4
   غسيلeluted with 4% methanol in methylene chloride
5. 5
   أخرىThe combined product fractions were evaporated to dryness in vacuo

الإجراء التجريبي

1-(2-Methoxy-4-(1-ethenylsulfonyl-4-piperidyloxy)phenylacetyl)-4-(2-methylphenyl)piperazine-2-carboxamide (69 mg, 0.12 mmol) was dissolved in methanol (4 ml), treated with cyclopropylamine (0.0072 ml, 10 mg, 0.18 mmol), and stirred at ambient temperature under nitrogen for 18 hours. An additional 0.014 ml of cyclopropylamine was added and the mixture stirred another 72 hours at ambient temperature. The reaction was concentrated in vacuo and the residue was chromatographed on silica gel eluted with 4% methanol in methylene chloride. The combined product fractions were evaporated to dryness in vacuo. The residue was reconcentrated from ether to give 1-(2-methoxy-4-(1-(2-(N-cyclopropylamino)ethylsulfonyl)-4-piperidyloxy)phenylacetyl)-4-(2-methylphenyl)piperazine-2-carboxamide: mp 69°-110° C.

المصدر