	US 12,258,348 B2
	Method for the production of lumateperone and its salts
Gábor Berecz, Budapest (HU); Bálint Nyulasi, Budapest (HU); Mátyás Milen, Budapest (HU); Gyula Simig, Budapest (HU); András Mravik, Budapest (HU); Gábor Németh, Budapest (HU); Adrienn Keszthelyi, Budapest (HU); Beatrix Bali, Budapest (HU); Balázs Volk, Budapest (HU); László Szlávik, Budapest (HU); Zoltán Varga, Budapest (HU); and Daniel Ulej, Budapest (HU)
Assigned to EGIS GYOGYSZERGYAR ZRT., Budapest (HU)
Filed by EGIS GYOGYSZERGYAR ZRT., Budapest (HU)
Filed on Feb. 16, 2023, as Appl. No. 18/110,570.
Application 18/110,570 is a division of application No. 16/767,057, granted, now 11,655,251, previously published as PCT/HU2018/050050, filed on Nov. 27, 2018.
Claims priority of application No. P1700491 (HU), filed on Nov. 27, 2017; application No. P1700492 (HU), filed on Nov. 27, 2017; application No. P1700493 (HU), filed on Nov. 27, 2017; and application No. P1800126 (HU), filed on Apr. 16, 2018.
Prior Publication US 2023/0331727 A1, Oct. 19, 2023
Int. Cl. C07D 471/16 (2006.01); C07B 57/00 (2006.01); C07C 235/74 (2006.01); C07C 309/30 (2006.01); C07C 309/35 (2006.01)

CPC C07D 471/16 (2013.01) [C07B 57/00 (2013.01); C07C 235/74 (2013.01); C07C 309/30 (2013.01); C07C 309/35 (2013.01); C07B 2200/07 (2013.01); C07B 2200/13 (2013.01)]

20 Claims

1. A

salt of formula (VI)

(6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3′,4′: 4,5]pyrrolo[1,2,3-de]quinoxaline formed with (+)-dibenzoyl-D-tartaric acid mono(dimethylamide),

a salt of formula (II)

(6bR,10aS)-3-methyl-2,3,6b,9,10,10a-hexahydro-1H-pyrido[3′,4′: 4,5]pyrrolo[1,2,3-de]quinoxaline formed with hydrochloric acid,

the salt of formula (I) lumateperone formed with naphthalene-2-sulfonic acid,

the amorphous form of formula (III) lumateperone salt

in which salt the molar ratio of lumateperone and the p-toluenesulfonic acid is 1:1.