Methods for the synthesis of milnacipran and congeners thereof

Organic compounds -- part of the class 532-570 series – Organic compounds – Amino nitrogen containing

Reexamination Certificate

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C564S461000

Reexamination Certificate

active

11097466

ABSTRACT:
One aspect of the present invention relates to methods for synthesizing milnacipran or congeners thereof. Another aspect of the present invention relates to asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof. The present invention also relates to methods for synthesizing intermediates useful in the non-asymmetric or asymmetric methods for synthesizing enantiomerically enriched milnacipran or congeners thereof.

REFERENCES:
Casadio et al., Bollettino Chimico Farmaceutico (1978), 117(6), 331-42, CAS online citation on STN, Columbus OH, USA.
Wang et al., Zhongguo Yiyao Gongye Zazhi (2004), 35(5), 259-260, CAS online citation on STN, Columbus OH, USA.
Bonnaud, B, et al., “1-Aryl-2-(aminoethyl)cyclopropanecarboxylic Acid Derivatives. A New Series of Potential Antidepressants”,J. Med. Chem., 30:318-325 (1987).
Bonnaud, B., et al., “Synthesis of Novel Indolizine Derivatives”,J. Heterocyclic Chem., 28:1927-1932 (1991).
Ronsisvalle, G. et al., “Substituted 1-Phenyl-2-cyclopropylmethylamines with High Affinity and Selectivity for Sigma Sites”,Bioorg.&Med. Chem., 8:1503-1513 (2000).
Shuto, S. et al., “Synthesis of (+)- and (−)-Milnaciprans and Their Conformationally Restricted Analogs”,Tetrahedron Letters, 37(5):641-644 (1996).
Partial International Search Report issued for corresponding PCT application No. PCT/US2005/011365.
International Search Report issued for corresponding PCT application No. PCT/US2005/011365 dated Feb. 2, 2006.

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