反应详情

6.4 1 g of {4-[2-(4,5-dihydro-3H-pyrrol-2-yl)ethyl]naphthalen-1-yl)morpholin-4-ylmethanone is dissolved in 50 ml of methanol, and 0.26 g of sodium cyano borohydride is added. A pH of 2 inset at 0° C. using methanolic HCl. The mixture is subsequently allowed to left to stir at RT for a further 6 h and then subjected to aqueous work-up. A pH of 9 is set using aqueous NaOH, and the mixture is extracted with ethyl acetate. The dried and evaporated organic phase is purified by chromatography, giving 460 mg of morpholin-4-yl-[4-(2-pyrrolidin-2-ylethyl)naphthalen-1-yl]methanone; Rt.: 1.420 min; [M+H]+339.2.

1. custominset at 0° C.
2. waitto left
3. extractionthe mixture is extracted with ethyl acetate
4. customThe dried
5. customevaporated organic phase
6. customis purified by chromatography