Process for making asenapine

Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...

Reexamination Certificate

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C549S354000

Reexamination Certificate

active

07875729

ABSTRACT:
Asenapine and related trans-isomer bicyclic compounds can be obtained by reducing a compound of formula (C) to preferentially form a trans-isomer compound of formula (D), followed by subsequent ring closure to form a compound of formula (B) such as asenapine.

REFERENCES:
patent: 4145434 (1979-03-01), van der Burg
patent: 1 710 241 (2006-10-01), None
patent: WO 95/23600 (1995-09-01), None
patent: WO 99/32108 (1999-07-01), None
Th. de Boer et al., “Antipsychotic Dopamine D2 Receptor Antagonist 5-HT2 Receptor Antagonist” Drugs of the Future 1993, 18(12): 1117-1123.
C. W. Funke et al., “Physico-chemical Properties and Stability of trans-5-Chloro-2-methyl-2,3,3a,12b-tetra . . . ” Arzneim-Forsch/Drug Res., 40(1) Nr. 5 (1990) pp. 536-539.

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