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US 6,541,242 B1Granted
Enzymatic processes for the resolution of enantiomeric mixtures of compounds useful as intermediates in the preparation of taxanes
AssigneeBristol-Myers Squibb Company
InventorRamesh N. Patel
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Abstract
Methods for the enzymatic resolution of mixtures of enantiomers, such as β-lactam compounds, which may be employed as intermediates in the preparation of taxanes bearing a C-13 sidechain containing a heterocyclic or cycloalkyl group, the latter useful in the pharmaceutical field.
Claims4
A method for the resolution of a mixture IV comprising the enantiomers IVa and IVb:
- R2—Ta—COOH (IVa)
- and
- R2—Tb—COOH (IVb)
- wherein
- wherein
- R1 is in the erythro position relative to the group W in both IVa and IVb, or R1 is in the threo position relative to the group W in both IVa and IVb;
- W is NH2;
- R1 is hydroxyl;
- and
- R2 is heterocyclo;
- comprising the steps of (a) contracting said mixture IV with an esterase, lipase or protease enzyme or a microorganism containing an esterase, lipase or protease enzyme capable of catalyzing the stereoselective conversion of one of said compounds IVa or IVb to a non-enantiomeric compound in the presence of an acylating agent, (b) effecting said conversion, and (c) recovering said non-enantiomeric compound.
8 more elements
Dependencies are inferred from the claim text.