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

1997-11-12

1999-09-14

Tsang, Cecilia J.

Organic compounds -- part of the class 532-570 series

Organic compounds

Nitrogen attached directly or indirectly to the purine ring...

544337, 514252, C07D41300

Patent

active

059525029

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 to 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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