Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Hydrochloric Acid | HCID 313 | — |
| Reactant | Succinic anhydride | HCID 7922 | — |
| Reactant | HCID 11668552 | HCID 11668552 | — |
| Solvent | Pyridine | HCID 1049 | — |
| Product | HCID 57557947 | HCID 57557947 | 76% |
Reaction Steps
The 7-((R)-5-hydroxymethyl-2-oxooxazolidin-3-yl)-3-(2-trifluoromethylphenyl)-2H-isoquinolin-1-one (50 mg, 0.12 mmol) obtained in step B of Example 1-14 was dissolved in pyridine (3 ml). Thereafter, succinic anhydride (14 mg, 0.14 mmol) was added to the solution, and the obtained mixture was then stirred at 50° C. for 6 hours. Thereafter, succinic anhydride (24 mg, 0.25 mmol) was further added to the reaction solution, and the obtained mixture was then stirred at 50° C. for 15 hours. Thereafter, 1 N hydrochloric acid was added to the reaction mixture, and precipitated powders were collected by filtration. The obtained filtrate was washed with water. The resultant was subjected to air-drying, and was then dried under reduced pressure, so as to obtain 3-{(R)-2-oxo-3-[1-oxo-3-(2-trifluoromethylphenyl)-1,2-dihydroisoquinolin-7-yl]oxazolidin-5-ylmethoxycarbonyl}propionic acid (46 mg, 74%) in the form of white powders.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US07820693B2 |
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| Source dataset | uspto-grants-2010_10 |
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| ORD ID | ord-bb3b3af81e6a4c3ca892d054077a3e2c |
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| Source note | uspto-grants-2010_10 |
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