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US 9,102,963 B2Granted
Biocatalytic process for preparing eslicarbazepine and analogs thereof
AssigneeCodexis, Inc.
InventorsAnupam Gohel, Derek Smith, Brian Wong, Joly Sukumaran, Wan Lin Yeo, Steven J. Collier, Scott Novick
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Abstract
The present disclosure relates to biocatalysts and its uses for the efficient preparation of eslicarbazepine, eslicarbazepine acetate, and analogs thereof.
Claims11
A process for preparing a compound of structural formula (1) in enantiomeric excess,
- wherein
- each ring A and B is independently an optionally substituted monocyclic aryl or heteroaryl,
- R1 is selected from hydrogen, hydroxy, halo, cyano, carboxy, and an optionally substituted alkyl, aminoalkyl, cycloalkyl, heterocycloalkyl, alkyloxycarbonyl, aminocarbonyl, aminothiocarbonyl, aminosulfonyl, and sulfonyl;
- the process comprising contacting the compound of structural formula (2),
- wherein A and B, and R1 are defined above, with a ketoreductase polypeptide comprising an amino acid sequence that has at least 80% sequence identity to the reference polypeptide of SEQ ID NO:
- 10, wherein the amino acid sequence comprises X80 is T;
- X96 is V or R;
- X145 is L;
- X153 is T;
- X190 is P;
- X196 is L or M;
- and X226 is V, wherein the ketoreductase is capable of converting compound (2) to compound (1) in enantiomeric excess, in presence of NADH or NADPH under suitable reaction conditions.
9 more elements
Dependencies are inferred from the claim text.