HuagongsheHuagongshe Chemistry Print Report · For research reference only
5-fluoro-2-[2-(4-fluoro-2,3-dihydroindol-1-yl)-2-oxoethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one → 5-fluoro-2-[2-(5-fluoro-2-methyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 5-fluoro-2-[2-(4-fluoro-2,3-dihydroindol-1-yl)-2-oxoethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one | HCID 136069565 | — |
| Reactant | Sodium (5-fluoro-4-morpholin-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)acetate | HCID 136069585 | — |
| Product | 4-Hydroxypyrimidine | HCID 20695 | — |
| Product | 5-fluoro-2-[2-(5-fluoro-2-methyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one | HCID 136378663 | 66.8% |
Reaction Steps
5-Fluoro-2-[2-(5-fluoro-2-methyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-6-morpholin-4-yl)-3H-pyrimidin-4-one is prepared by following the procedure described in example 1a (step 5a) using 182 mg of sodium (5-fluoro-4-morpholin-4-yl-6-oxo-1,6-dihydropyrimidin-2-yl)acetate (obtained in step 2a) and 197 mg of 5-fluoro-2-methyl-2,3-dihydro-1H-indole (reference example 1a). After silica column purification, eluent: 98/02 dichloromethane/methanol, 85 mg of 5-fluoro-2-[2-(5-fluoro-2-methyl-2,3-dihydroindol-1-yl)-2-oxoethyl]-6-morpholin-4-yl-3H-pyrimidin-4-one are obtained in the form of a white 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-e73767702ba8412da970c37cdbf6df69 |
| Source note | uspto-grants-2015_09 |