2R, 4S, R, S- and 2S, 4R, R, S-hydroxyitraconazole

Details 2R, 4S, R, S- and 2S, 4R, R, S-hydroxyitraconazole 2R, 4S, R, S- and 2S, 4R, R, S-hydroxyitraconazole

1999-06-14

2000-12-26

Shah, Mukund J.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

544367, 544337, A61K 31495, C07D41300, C07D40514

Patent

active

061660183

ABSTRACT:
A method of preparation of optically pure isomers of hydroxyitraconazole, in particular the two cis dioxolane diastereomers of the sec-butyl (R,S)-isomer, and to phosphate and sulfate derivatives thereof is disclosed. Pharmaceutical compositions containing these compounds and their use for the treatment of fungal infection are also disclosed.

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Saksena et al., "Concise Asymmetric Routes to 2,2,4-Trisubstituted Tetrahydrofurans Via Chiral Titanium Imide Enolates: Key Intermediates Towards Synthesis of Highly Active Azole Antifungals SCH 51048 and SCH 56592", Tetrahedron Letters, 37, No. 32, 5657-5660, 1996.

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