公开(公告)号：US20210070755A1

公开(公告)日：2021-03-11

申请号：US16767057

申请日：2018-11-27

申请人： EGIS GYOGYSZERGYAR ZRT.

发明人： Gábor BERECZ ,  Bálint NYULASI ,  Mátyás MILEN ,  Gyula SIMIG ,  András MRAVIK ,  Gábor NÉMETH ,  Adrienn KESZTHELYI ,  Beatrix BALI ,  Balázs VOLK ,  László SZLÁVIK ,  Zoltán VARGA ,  Daniel ULEJ

IPC分类号： C07D471/16 ,  C07B57/00 ,  C07C309/35 ,  C07C309/30 ,  C07C235/74

摘要： 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.

公开(公告)号：US20230331727A1

公开(公告)日：2023-10-19

申请号：US18110570

申请日：2023-02-16

申请人： EGIS GYOGYSZERGYAR ZRT.

发明人： Gábor BERECZ ,  Bálint NYULASI ,  Mátyás MILEN ,  Gyula SIMIG ,  András MRAVIK ,  Gábor NÉMETH ,  Adrienn KESZTHELYI ,  Beatrix BALI ,  Balázs VOLK ,  László SZLÁVIK ,  Zoltán VARGA ,  Daniel ULEJ

IPC分类号： C07D471/16 ,  C07B57/00 ,  C07C235/74 ,  C07C309/30 ,  C07C309/35

CPC分类号： C07D471/16 ,  C07B57/00 ,  C07C235/74 ,  C07C309/30 ,  C07C309/35 ,  C07B2200/07 ,  C07B2200/13

摘要： 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.