تفاعل #157978

معادلة التفاعل

11-chloro-2,3-dihydro-1H-cyclopenta[4,5]pyrido[1,2-a]benzimidazole-4-carboxamide

DIPEA

NMP

3-azabicyclo[4.1.0]hept-6-ylmethanol hydrochloride

→

11-[6-(hydroxymethyl)-3-azabicyclo[4.1.0]hept-3-yl]-2,3-dihydro-1H-cyclopenta[4,5]pyrido[1,2-a]benzimidazole-4-carboxamide

المردود 74.8%

المذيبات

water

ظروف التفاعل

المعالجة

1. 1
   أخرىwas performed at 220° C. for 60 minutes under microwave irradiation
2. 2
   أخرىThe reaction liquid
3. 3
   ترشيحthe precipitate was collected by filtration
4. 4
   أخرىThe resulting solid was purified by silica gel column chromatography (MeOH/chloroform)

الإجراء التجريبي

11-chloro-2,3-dihydro-1H-cyclopenta[4,5]pyrido[1,2-a]benzimidazole-4-carboxamide (800 mg) and DIPEA (1.95 ml) were added to an NMP suspension of 3-azabicyclo[4.1.0]hept-6-ylmethanol hydrochloride (1.01 g), and stirring was performed at 220° C. for 60 minutes under microwave irradiation. The reaction liquid was added to water and the precipitate was collected by filtration. The resulting solid was purified by silica gel column chromatography (MeOH/chloroform) to obtain 11-[6-(hydroxymethyl)-3-azabicyclo[4.1.0]hept-3-yl]-2,3-dihydro-1H-cyclopenta[4,5]pyrido[1,2-a]benzimidazole-4-carboxamide (788 mg).

المصدر