Back to results
US 10,208,054 B2Granted
Method of preparing buprenorphine
AssigneeJohnson Matthey Public Limited Company
InventorsNicolas Archer, David August, Michael Bease, Barbara Jamieson, Robert S. Marmor
Life of this patent
Estimating the term…
Abstract
An improved process for preparing buprenorphine and a method for increasing the yield of buprenorphine or a derivative thereof.
Claims7
A process for the preparation of a compound of formula (Ib),
- wherein:
- R10 is a straight-chain, branched or cyclic C1-C20 alkyl;
- R11 is C(R13)(R14)(OH) or a protected C(═O)(R15);
- R12 is H or CN;
- R13 is a straight-chain, branched or cyclic C1-C20-alkyl;
- R14 is a straight-chain, branched or cyclic C1-C20-alkyl;
- and
- R15 is a straight-chain, branched or cyclic C1-C20-alkyl
- is a double bond or a single bond;
- the process comprising:
- i. reacting a compound of formula (Ia) with a thiolate in a suitable polar aprotic solvent, wherein the thiolate is selected from the group consisting of an optionally substituted C1-C20-alkylthiolate, an optionally substituted C6-C20-arylthiolate or an optionally substituted C7-C30-arylalkylthiolate;
- and
- ii. treating the reaction mixture of step (i) with a protonating agent to give the compound of formula (Ib).
10 more elements
Dependencies are inferred from the claim text.