Invention Grant
- Patent Title: Method for the production of lumateperone and its salts
-
Application No.: US16767057Application Date: 2018-11-27
-
Publication No.: US11655251B2Publication Date: 2023-05-23
- Inventor: Gábor Berecz , Bálint Nyulasi , Mátyás Milen , Gyula Simig , András Mravik , Gábor Németh , Adrienn Keszthelyi , Beatrix Bali , Balázs Volk , László Szlávik , Zoltán Varga , Daniel Ulej
- Applicant: EGIS GYOGYSZERGYAR ZRT.
- Applicant Address: HU Budapest
- Assignee: EGIS GYOGYSZERGYAR ZRT.
- Current Assignee: EGIS GYOGYSZERGYAR ZRT.
- Current Assignee Address: HU Budapest
- Agency: Millen White Zelano and Branigan, PC
- Agent Csaba Henter
- Priority: HU 700491 2017.11.27 HU 700492 2017.11.27 HU 700493 2017.11.27 HU 800126 2018.04.16
- International Application: PCT/HU2018/050050 2018.11.27
- International Announcement: WO2019/102240A 2019.05.31
- Date entered country: 2020-05-26
- Main IPC: C07D471/16
- IPC: C07D471/16 ; C07B57/00 ; C07C235/74 ; C07C309/30 ; C07C309/35

Abstract:
Method for the production of formula (I) lumateperone or its acid addition salts so that the enantiomer compound with stereochemistry 6bR,10aS
is separated form the cis racemate using resolution and the formula (II) stereoisomer is alkylated with 4-halo-4′-fluoro butyrophenone (X=I, Br, Cl) to produce the formula (I) lumateperone, or optionally its acid addition salt. The object of the invention also relates to the amorphous form of the morphologically uniform p-toluenesulfonic acid salt of lumateperone and to the naphthalene-2-sulfonic acid salt of lumateperone, to the 1:2 stoichiometry salt of lumateperone formed with naphthalene-2-sulfonic acid.
is separated form the cis racemate using resolution and the formula (II) stereoisomer is alkylated with 4-halo-4′-fluoro butyrophenone (X=I, Br, Cl) to produce the formula (I) lumateperone, or optionally its acid addition salt. The object of the invention also relates to the amorphous form of the morphologically uniform p-toluenesulfonic acid salt of lumateperone and to the naphthalene-2-sulfonic acid salt of lumateperone, to the 1:2 stoichiometry salt of lumateperone formed with naphthalene-2-sulfonic acid.
Public/Granted literature
- US20210070755A1 METHOD FOR THE PRODUCTION OF LUMATEPERONE AND ITS SALTS Public/Granted day:2021-03-11
Information query