HuagongsheHuagongshe Chemistry Print Report · For research reference only
Cesium carbonate → (8S)-9-[(5-chloro-1-benzothiophen-3-yl)methyl]-2-(morpholin-4-yl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Cesium carbonate | HCID 10796 | — |
| Reactant | 3-(Bromomethyl)-5-chloro-1-benzothiophene | HCID 2779857 | — |
| Reactant | (S)-8-(Morpholin-4-yl)-2-(trifluoromethyl)-1,2,3,4-tetrahydropyrimido[1,2-a]pyrimidin-6-one | HCID 136238743 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Product | (8S)-9-[(5-chloro-1-benzothiophen-3-yl)methyl]-2-(morpholin-4-yl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one | HCID 49854301 | — |
Reaction Steps
The product is prepared according to the procedure described in Example 22, using 100 mg of (8S)-2-morpholin-4-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one (Example 1e), 214 mg of caesium carbonate and 95 mg of 3-(bromomethyl)-5-chloro-1-benzothiophene in 2 ml of dimethylformamide. After purification by preparative HPLC/MS (Method C), 72 mg of (8S)-9-[(5-chloro-1-benzothiophen-3-yl)methyl]-2-(morpholin-4-yl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one are obtained in the form of an oil, the characteristics of which are the following:
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08846670B2 |
| Source dataset | uspto-grants-2014_09 |
| ORD ID | ord-db5b64d5cd5843a196ab5ef92c7d7025 |
| Source note | uspto-grants-2014_09 |