US 12,234,200 B2
Synthetic methods of preparing esketamine
Cheng Yi Chen, San Diego, CA (US)
Assigned to Janssen Pharmaceutica NV, Beerse (BE)
Appl. No. 17/603,603
Filed by JANSSEN PHARMACEUTICA NV, Beerse (BE)
PCT Filed Apr. 16, 2020, PCT No. PCT/EP2020/060737
§ 371(c)(1), (2) Date Oct. 14, 2021,
PCT Pub. No. WO2020/212510, PCT Pub. Date Oct. 22, 2020.
Claims priority of provisional application 62/834,636, filed on Apr. 16, 2019.
Prior Publication US 2022/0220062 A1, Jul. 14, 2022
Int. Cl. C07C 221/00 (2006.01); C07C 213/02 (2006.01); C07C 263/04 (2006.01); C07C 265/10 (2006.01); C07C 271/34 (2006.01)
CPC C07C 221/00 (2013.01) [C07C 213/02 (2013.01); C07C 263/04 (2013.01); C07C 265/10 (2013.01); C07C 271/34 (2013.01)] 9 Claims
 
1. An asymmetric synthesis of esketamine, D3-esketamine, or (S)-norketamine comprising
conversion of (S)-2′-chloro-2-methoxy-3,4,5,6-tetrahydro-[1,1′-biphenyl]-3-yl carbamate to (S)-2′-chloro-1-isocyanato-6-methoxy-1,2,3,4-tetrahydro-1,1′-biphenyl

OG Complex Work Unit Chemistry