Optically active 3-amino-2,5-dioxopyrrolidine-3-carboxylate,...

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

Reexamination Certificate

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Reexamination Certificate

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08058456

ABSTRACT:
The present invention provides a compound of the formula (III):wherein R is a C1-6alkyl group,as a novel optically active intermediate for preparing tetrahydropyrrolo[1,2-a]pyrazin-4-spiro-3′-pyrrolidine derivatives such as Ranirestat being a promising therapeutic agent for diabetic complications in a short process, in an economically advantageous manner and in high yields, and the process for preparing the same.

REFERENCES:
patent: 5258382 (1993-11-01), Negoro et al.
patent: 4-164066 (1992-06-01), None
patent: 5-186472 (1993-07-01), None
patent: 6-192222 (1994-07-01), None
Jordan, V. C. Nature Reviews: Drug Discovery, 2, 2003, 205.
Dörwald, F. Zaragoza. Side Reactions in Organic Synthesis: A Guide to Successful Synthesis Design, Weinheim: Wiley-VCH Verlag GmbH & Co. KGaA, 2005, Preface.
English translation of PCT Written Opinion dated Jan. 29, 2009 in the International (PCT) Application PCT/JP2007/061888 of which the present application is the U.S. National Stage.
Toshiyuki Negoro et al., “Novel, Highly Potent Aldose Reductase Inhibitors: (R)-(−)-2-(4-Bromo-2-fluorobenzyl)-1,2,3,4-tetrahydropyrrolo[1,2-a]pyrazine-4-spiro-3′-pyrrolidine-1,2′,3,5′-tetrone (AS-3201) and its Congeners”, Journal of Medicinal Chemistry, vol. 41, pp. 4118-4129, 1998.
International Search Report dated Jul. 31, 2007 in the International (PCT) Application PCT/JP2007/061888 of which the present application is the U.S. National Stage.

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