Process for the synthesis of substituted chloromethyl dialkylphosphates
US12071421B2 · kind B2 · utility
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3Claims
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Key dates
| Filing date | Mar 21, 2022 |
| Grant date | Aug 27, 2024 |
| Priority date | — |
| Expiry date | Mar 21, 2042 |
Classification
- Technology area (CPC C)Chemistry; Metallurgy
- CPC primaryC07F9/650952
- WIPO fieldPharmaceuticals
- WIPO sectorChemistry
Abstract
Disclosed are compounds including phosphate and N-oxide prodrugs of the NK1 antagonist netupitant, useful in the prevention and/or treatment of diseases including emesis induced by chemotherapy. Also disclosed are methods of making a di-tert-butyl (chloromethyl) phosphate useful in the manufacture of such prodrugs by reacting a dialkylphosphate salt with an acid to obtain the corresponding ester of phosphoric acid, reacting the ester with a quaternary ammonium hydroxide base to form a monobasic salt, and reacting the monobasic salt with chloroiodomethane to form the corresponding chloromethyl dialkyl phosphate.
Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.