Process for the preparation of asenapine and intermediate...

Details Process for the preparation of asenapine and intermediate... Process for the preparation of asenapine and intermediate...

2011-06-21

2011-06-21

Shameem, Golam M (Department: 1626)

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

C548S416000, C548S420000

Reexamination Certificate

active

07964739

ABSTRACT:
The invention relates to a novel process for the preparation of asenapine, i.e. trans-5-chloro-2-methyl-2,3,3a,12b-tetrahydro-1H-dibenz[2,3:6,7]oxepino[4,5-c]pyrrole, as well as to novel intermediate products for use in said process.

REFERENCES:
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patent: WO 2007/046554 (2007-04-01), None
patent: WO 2008/003460 (2008-10-01), None
Vader, J., et. al. ; “The Syntheses of Radiolabelled Org 5222 and its main metabolite Org 30526”, Journal of Labelled Compounds and Radiopharmaceuticals, John Wiley, Chichester, GB, vol. 34, No. 9, 1994, pp. 845-869, XP008058294.
Padwa, A; Dent W.: “N-Benzyl-N-methoxymethyl-N-(trimethylsilyl) methylamine as an azomethine ylide equivalent: 2,6-dioxo-1-phenyl-4-benzyl-1,4-diazabicyclo[3.3.0]octane”, Organic Syntheses, vol. 67, 1989, pp. 133-137, XP003478138.
Wildenberg, V.D., et. al.; “Biotransformation of Trans-5-Choloro-2-Methyl-2,3,3a,12b-Tetrahydro- . . . ” Arzneimittel Forschung, Drug Research, ECV Editio Cantor Verlag, Aulendorf, DE, vol. 40, No. 5, 1990, pp. 540-544, XP008090109.
International Search Report for PCT/EP2008/068187; mailed Apr. 9, 2009; 4 pages.

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