Process and intermediates for the preparation of 4-aryl...

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

Reexamination Certificate

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C546S326000, C546S233000, C546S230000, C546S226000

Reexamination Certificate

active

06998488

ABSTRACT:
A novel process is provided for the preparation of 4-aryl piperidines, and the useful intermediates obtained therein. These compounds are intermediates for the synthesis of melanocortin-4 receptor (MC-4R), which are useful for the treatment of disorders such as obesity, diabetes, male sexual dysfunction, and female sexual dysfunction.

REFERENCES:
patent: 0 831 087 (1997-09-01), None
patent: WO 02/068387 (2002-09-01), None
patent: WO 02/068388 (2002-09-01), None
Ca 83:206332, “Benzoguanamine derivatives”, Murai et al.
Ca 133:350205, “Contraceptive compositions containing antiprogestinic and progestinic dihydro-2H-3,1-benzoxazin-2-ones”, Gary et al.
Ca 2002:224612, “Combination regimens using progesterone receptor modulators”, Grubb et al.
Billotte, Synlett (1998), pp. 379-380, “Synthesis of C-Substituted cyclic amines using azacycloalkyl organozinc reagents”.
Comins et al., J. Org. Chem. (1982), vol. 47, pp. 4315-4319, “Regioselective addition of Grignard reagents to 1-acylpyridinium salts”.

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