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US 8,710,226 B2Granted
Process for the preparation of morphinane analogues
AssigneeSun Pharmaceutical Industries Limited
InventorsNileshkumar Sureshbhai Patel, Srinivasu Kilaru, Rajamannar Thennati
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Abstract
The present invention relates to an improved process for preparing morphinane analogues of formula 1 wherein the substituents R1, R2, R2a, R3, R4, R5 and Y have the meanings as defined in the specifications.
Claims12
A process for preparation of buprenorphine, represented by formula 1c
- wherein the process comprises the steps of
- (a) reacting a compound of formula 2c
- with ethylchloroformate in presence of an alkali iodide and Lithium carbonate to yield a compound of formula 3c:
- (b) subjecting the compound of formula 3c to hydrolysis in presence of potassium hydroxide to obtain a compound of formula 4c
- (c) reacting the compound of formula 4c with a compound of formula 5c
- in presence of methanesulfonyl chloride and LiBr, to obtain a compound of formula 6c,
- d) converting the compound of formula 6c to a compound of formula 1c or salt thereof by reacting with potassium tert-butoxide in presence of an C1-4alkyl or an arylthiol and optionally reacting with a mineral acid.
4 more elements
Dependencies are inferred from the claim text.