DERIVADOS DO EPOTILONE SUA PREPARACAO E UTILIZACAO

Epothilone derivatives of formula (I)-(III) are new. R = H or 1-4C alkyl; Y Z = H, halo, pseudohalogen, OH, 1-6C acyloxy, 1-6C alkoxy or benzoyloxy; or Y+Z = bond or O; (a) R' = Q; A = H; B = OR1; and R" = R2; or R"+B = C(O)O, C(S)O, S(O)O, Si(R")2O or C(R")(R"')O;...

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Bibliographische Detailangaben
Hauptverfasser:	GERHARD HOFLE, DR, MICHAEL KIFFE
Format:	Patent
Sprache:	por
Schlagworte:	ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM AGRICULTURE ANIMAL HUSBANDRY BIOCIDES, e.g. AS DISINFECTANTS, AS PESTICIDES, AS HERBICIDES CHEMISTRY FISHING FORESTRY HETEROCYCLIC COMPOUNDS HUMAN NECESSITIES HUNTING HYGIENE MEDICAL OR VETERINARY SCIENCE METALLURGY ORGANIC CHEMISTRY PEST REPELLANTS OR ATTRACTANTS PLANT GROWTH REGULATORS PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES PRESERVATION OF BODIES OF HUMANS OR ANIMALS OR PLANTS OR PARTSTHEREOF SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS TRAPPING
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Beschreibung
Zusammenfassung:	Epothilone derivatives of formula (I)-(III) are new. R = H or 1-4C alkyl; Y Z = H, halo, pseudohalogen, OH, 1-6C acyloxy, 1-6C alkoxy or benzoyloxy; or Y+Z = bond or O; (a) R' = Q; A = H; B = OR1; and R" = R2; or R"+B = C(O)O, C(S)O, S(O)O, Si(R")2O or C(R")(R"')O; (b) R' = C(=X)Me or CH(OX')Me; A = H; B = OR1; and R" = R2; (c) R' = Q; and A+B = bond; X = O, NOR4, N-NR4R5 or N-NHCONR4R5; X' = H, 1-18C alkyl, 1-18C acyl, benzyl, benzoyl or cinnamoyl; Q = a group of formula (i); and R1-R5 = H, 1-6C alkyl, 1-6C acyl, benzoyl, 1-4C trialkylsilyl, or benzyl or phenyl (both optionally substituted by 1-6C alkoxy, 6C alkyl, OH and halo); or R4+R5 = 2-6C alkylene. Epothilone A and B are excluded. Also claimed is the production of epothilone A or B and/or their 12,13-bis-epi derivatives comprising the epoxidation of epothilone C (for A or derivatives) or D (for B or derivatives) especially using dimethyldioxirane or a peracid.