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US 11,820,752 B2Granted
Process for the preparation of apalutamide
AssigneeOlon S.P.A.
InventorsValentina Grande, Gabriele Ferretti, Barbara Novo
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Abstract
The present invention relates to a process for the preparation of Apalutamide of formula (A) Apalutamide is a latest-generation androgen receptor inhibitor, used to treat non-metastatic castration-resistant prostate cancer.
Claims6
A process for the preparation of Apalutamide which comprises
- (a):
- alkylating in dioxane 4-amino-2-fluoro-N-methylbenzamide of formula I
- with an alkyl halide of formula II
- wherein X is bromine to give the compound of formula III
- (b):
- activating the carboxyl group of the compound of formula III, via the formation of the compounds of formula IV
- wherein Y is
- (c):
- condensating the activated product IV obtained in step (b) with the isothiocyanate of formula V
- to give crude Apalutamide;
- (d):
- purifying the crude Apalutamide obtained in step (c).
9 more elements
Esters of formula IVa, IVc or IVd
Dependencies are inferred from the claim text.