반응 #2365675

반응 방정식

sodium (5-fluoro-4-morpholin-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)acetate

(−)-2-methyl-4,5-difluoro-2,3-dihydro-1H-indole

→

2-[2-((+)-4,5-difluoro-2-methyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-5-fluoro-6-morpholin-4-yl-3H-pyrimidin-4-one

수율 57.1%

반응 조건

후처리

1. 1
   기타The product is prepared
2. 2
   기타After silica column purification

실험 절차

The product is prepared by following the procedure described in example 1a (step 5a) using 140 mg of sodium (5-fluoro-4-morpholin-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)acetate obtained in step 2a of example 6a and 93 mg of (−)-2-methyl-4,5-difluoro-2,3-dihydro-1H-indole (reference example 2a). After silica column purification: eluent 98/02 dichloromethane/methanol, 117 mg of 2-[2-((+)-4,5-difluoro-2-methyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-5-fluoro-6-morpholin-4-yl-3H-pyrimidin-4-one are obtained in the form of a solid, the characteristics of which are the following:

출처