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US 12,459,948 B2Granted
Processes and intermediates for preparing a Btk inhibitor
AssigneeJanssen Pharmaceutica NV
InventorsPhilip James Pye, Andras Horvath, Laurent Lefort, Bernardus Kaptein, Gerardus Karel Maria Verzijl, Yuanyuan Yuan, Jinxiong Su
Life of this patent
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Abstract
Disclosed is a process for the preparation of certain intermediates, e.g. process for preparing a compound of formula (I) or a pharmaceutically acceptable salt thereof, in an enantioenriched form, which intermediate and processes are useful in the preparation of a BTK inhibitor, such as ibrutinib.
Claims9
A process for preparing a compound of formula (I):
- or a pharmaceutically acceptable salt thereof, in an enantioenriched form, wherein:
- R1 is hydrogen or a nitrogen protecting group;
- * is a chiral centre of an (R) configuration;
- and the process comprises reductive hydrazination of a compound of formula (II):
- or a salt thereof, with a compound of formula (III):
- H2N—N(H)—R2 (III)
- or a salt thereof, wherein R2 is hydrogen or a nitrogen protecting group to form a compound of formula (IV):
- or a salt thereof, followed by, in any order at least one of:
- optionally deprotecting R2 (when R2 is a nitrogen protecting group),
- optionally introducing R1 at the NH moiety of the piperidinyl ring (when R1 is a nitrogen protecting group) to form a product, and
- optionally resolving the product.
8 more elements
Dependencies are inferred from the claim text.