HuagongsheHuagongshe Chemistry Print Report · For research reference only
(+)-2-methyl-5,6-difluoro-2,3-dihydro-1H-indole → 5-fluoro-2-[2-((+)-5,6-difluoro-2-methyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-3-methyl-6-morpholin-4-yl-3H-pyrimidin-4-one
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | (+)-2-methyl-5,6-difluoro-2,3-dihydro-1H-indole | HCID 57388227 | — |
| Reactant | Sodium (5-fluoro-1-methyl-4-morpholin-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)acetate | HCID 57388477 | — |
| Product | 5-fluoro-2-[2-((+)-5,6-difluoro-2-methyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-3-methyl-6-morpholin-4-yl-3H-pyrimidin-4-one | HCID 68281749 | 40.9% |
Reaction Steps
The product is prepared by following the procedure described in example 1a (step 5a) using 80 mg of sodium (5-fluoro-1-methyl-4-morpholin-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)acetate obtained in step 2a of example 8a and 46 mg of (−)-2-methyl-5,6-difluoro-2,3-dihydro-1H-indole (reference example 3a). After silica column purification: eluent 98/02 dichloromethane/methanol, 47 mg of 5-fluoro-2-[2-((+)-5,6-difluoro-2-methyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-3-methyl-6-morpholin-4-yl-3H-pyrimidin-4-one are obtained in the form of a solid, the characteristics of which are the following:
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US09133168B2 |
| Source dataset | uspto-grants-2015_09 |
| ORD ID | ord-4389b2c30bd941dda798f4bee47928c3 |
| Source note | uspto-grants-2015_09 |