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US 12,358,917 B2Granted
Processes and intermediates for preparing a Btk inhibitor
AssigneeJanssen Pharmaceutica NV
InventorsCyril Ben Haim, Thomas Joost Martti Michiels, Florian Damien Medina, Simon Albert Wagschal, Dominique Paul M. Depré
Life of this patent
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Abstract
Disclosed is a process for the preparation of certain intermediates, e.g. the following compound: which intermediate and processes are useful in the preparation of a BTK inhibitor, such as ibrutinib.
Claims18
A process for preparing a compound of formula (I):
- in an enantio enriched form, wherein:
- R1 is hydrogen,
- R2 is tert-butyloxycarbonyl (BOC);
- * is a chiral centre of an(S) configuration;
- the process comprising Savinase enzymatic kinetic resolution of a compound of formula (II):
- in the presence of (i) an acyl donor that is vinyl butyrate or o-cresol methoxy acetate, (ii) a solvent that is toluene, methyl-tetrahydrofuran, or tert-amyl alcohol, and (ii) an inorganic base that is sodium carbonate (Na2CO3), triethylamine (Et3N), or N,N-diisopropylethylamine (DIPEA).
3 more elements
Dependencies are inferred from the claim text.