Febrifugine, isofebrifugine and method for producing the same

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C544S287000

Reexamination Certificate

active

06844350

ABSTRACT:
A febrifugine represented by Formula (A):and an isofebrifugine represented by Formula (B):which exhibit extremely strong activities against tropical malarial protozoan are provided, together with a total synthesis route which enables efficient large scale synthesis of the same.

REFERENCES:
patent: 4762838 (1988-08-01), Glazer
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Burgess, L.E., et al. “The Preparation of α-Substituted, β-Hydroxy Piperidines and pyrrolidines: The Total Synthesis of Febrifugine.”, Tetrahedron Letters, vol. 37, No. 19 (1996), pp. 3255-3258.
Kobayashi, S., et al. “Catalytic Asymmetric Synthesis of Antimalarial Alkaloids Febrifugine and Isofebrifugine and Their Biological Activity”, J. Org. Chem., vol. 64 (1999), pp. 6833-6841.
Kobayashi, S., et al. “Catalytic Asymmetric Synthesis of Febrifugine and Isofebrifugine”, Tetrahedron Letters, vol. 40 (1999) pp. 2175-2178.

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