	US 12,404,256 B2
	Process for preparing ozanimod
Lenka Chalupova, Blansko (CZ); and Marian Buchlovic, Blansko (CZ)
Assigned to Synthon B.V., Nijmegen (NL)
Appl. No. 17/627,386
Filed by Synthon B.V., Nijmegen (NL)
PCT Filed Jul. 16, 2020, PCT No. PCT/EP2020/070188 § 371(c)(1), (2) Date Jan. 14, 2022, PCT Pub. No. WO2021/009306, PCT Pub. Date Jan. 21, 2021.
Claims priority of application No. 19186630 (EP), filed on Jul. 16, 2019.
Prior Publication US 2022/0259163 A1, Aug. 18, 2022
Int. Cl. C07D 271/06 (2006.01)

CPC C07D 271/06 (2013.01)

20 Claims

1. A process for preparation of a compound of formula (1) or a salt thereof,

comprising:

i) reacting a compound of formula (7) in a presence of a compound of formula (R)₃SiOM, where R is selected from C₁-C₅alkyl or aryl and M is selected from Na or K or Li, in a solvent at a temperature between 50° C. and reflux temperature of the solvent to provide the compound of formula (1) in a reaction mixture;

ii) adding an acid or silicagel to said reaction mixture;

iii) isolating a solid form of the compound of formula (1) from alkyl acetate or an alcohol or a mixture thereof; and

iv) optionally salifying the compound of formula (1).