Sodium borohydride → Paliperidone

To a solution of 3-[2-[4-(6-fluoro-1,2-benzisoxazol-3-yl)piperidin-1-yl]ethyl]-9-oxo-2-methyl-6,7,8,9-tetrahydro-4H-pyrido-[1,2-a]pyrimidin-4-one (formula-10) (0.3 grams) taken in a mixture of methanol (1.5 ml) and dichloromethane (3 ml) added sodium borohydride (0.008 grams) and stirred for 1 hour at 30° C. The solvent was distilled off under reduced pressure. Methanol (1.5 ml) was added to it and heated to reflux for 30 min. the reaction mixture was cooled to 20° C. and stirred for 1 hour. Filtered the solid, washed with methanol and dried.

1. distillationThe solvent was distilled off under reduced pressure
2. additionMethanol (1.5 ml) was added to it
3. temperatureheated
4. temperatureto reflux for 30 min. the reaction mixture
5. temperaturewas cooled to 20° C.
6. stirringstirred for 1 hour
7. filtrationFiltered the solid
8. washwashed with methanol
9. customdried

ORDレコード

ord-31fcfda66c1e45ac94a75421d21bf066

出典データセット

uspto-grants-2013_07

DOI

10.6084/m9.figshare.5104873.v1

特許番号

US08481729B2