반응 #596904

반응 방정식

Dimebon

mCPBA

→

product

수율 41.9%

2,8-dimethyl-5-(2-(6-methylpyridin-3-yl)ethyl)-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole 2-oxide

수율 41.9%

용매

dichloromethane

dichloromethane

반응 조건

후처리

1. 1
   기타The solvent was removed under reduced pressure (below 30 deg C.)
2. 2
   기타the residue was purified by column chromatography on neutral alumina eluting with methanol-dichloromethane gradient

실험 절차

Dimebon (500 mg) was dissolved in 10 mL dichloromethane. To this was added a solution of mCPBA (65%, 536 mg) in 5 mL dichloromethane drop wise at 25 deg C. The reaction mixture was stirred at 25 deg C. for 24 h at which point it was found complete (by TLC and LCMS). The solvent was removed under reduced pressure (below 30 deg C.) and the residue was purified by column chromatography on neutral alumina eluting with methanol-dichloromethane gradient to obtain 220 mg of product as light brown oil. TLC Rf 0.5 in 5% MeOH-DCM. This compound also exhibited the following inhibition profile:

출처