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US 12,606,539 B2Granted
Process for preparation of apalutamide
AssigneeSynthon BV
InventorsOndrej Hylse, David Chalupa, Bohumil Dymacek, Marian Buchlovic
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Abstract
The presented invention relates to a process for preparation of Apalutamide, compound (1) or a salt or a solvate thereof: The presented invention further relates to solid forms of Apalutamide, solvates of Apalutamide and to processes for preparation thereof. The presented invention also relates to solid forms of intermediates used in the process for preparing Compound (1).
Claims14
A process for preparation of Compound (1) or a salt thereof,
- which comprises:
- a) reacting Compound (2) with Compound (3) in the presence of a non-nucleophilic base to obtain Compound (4), wherein the pKa value of conjugated acid formed from the non-nucleophilic base is higher than 25
- wherein R1 is selected from C1-C6 alkyl or substituted C1-C6 alkyl or aryl or substituted aryl,
- R2 is selected from alkyl or substituted alkyl or aryl or substituted aryl or C(O)R3 or C(O)OR3, and
- R3 is selected from C1-C6 alkyl or substituted C1-C6 alkyl or aryl or substituted aryl;
- and
- b) transforming Compound (4) into Compound (1) or a salt thereof.
4 more elements
Dependencies are inferred from the claim text.