Hexahydropyrrolo¬1,2-c|pyrimidines as antiviral, antifungal...

Details Hexahydropyrrolo¬1,2-c|pyrimidines as antiviral, antifungal... Hexahydropyrrolo¬1,2-c|pyrimidines as antiviral, antifungal...

C - Chemistry, Metallurgy

07

D

C07D 491/22 (2006.01) A61K 31/505 (2006.01) A61P 31/10 (2006.01) A61P 31/12 (2006.01) A61P 35/00 (2006.01) C07D 209/00 (2006.01) C07D 239/00 (2006.01) C07D 311/00 (2006.01) C07D 313/00 (2006.01)

Patent

CA 2376758

Improved methods for convergent, total enantioselective synthesis of guanidinium alkaloid compounds including ones having <i>cis</i>- or - <i>trans</i>-1-oxo- and 1-iminohexahydropyrrolo[1,2-c]pyrimidine units including, 13,14,15-isocrambescidin 800, crambescidin 800 and ptilomycalin A, for use as therapeutic agents having antifungal and/or antiviral and/or antitumor activity are provided. Methods for preparing novel pentacyclic intermediates for the preparation of the crambescidin/ptilomycalin family of guanidinium alkaloids and congeners are also disclosed.

L'invention se rapporte à des procédés de synthèse convergente à énantiosélectivité totale de composés alcaloïdes de guanidinium comportant des "ones" possédant des unités cis- ou -trans-1-oxo-et 1-iminohexahydropyrrolo [1,2-c]pyrimidine, et notamment de composés du type 13,14,15-isocrambescidine 800, crambescidine 800 et ptilomycaline A, lesdits composés pouvant servir d'agents thérapeutiques dotés d'une activité antifongique et/ou antivirale et/ou antitumorale. L'invention se rapporte à des procédés de préparation de nouveaux intermédiaires pentacycliques utilisés pour la préparation de la famille crambescidine/ptilomycaline d'alcaloïdes de guanidinium et de congénères.

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