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Priority claimed from YU01154/88Aexternal-prioritypatent/YU115488A/en
Publication of SI8811154ApublicationCriticalpatent/SI8811154A/en
Publication of SI8811154BpublicationCriticalpatent/SI8811154B/en
Pharmaceuticals Containing Other Organic And Inorganic Compounds
(AREA)
Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems
(AREA)
Acyclic And Carbocyclic Compounds In Medicinal Compositions
(AREA)
Claims (1)
67 patentni zahtevek Postopek za pripravo N-substituiranih derivatov stavrosporina s splošno formulo (n, • /Stau/-N(CH3)-R kjer /Stau/ predstavlja ostanek z delno formulo HA process for the preparation of N-substituted staurosporine derivatives of general formula (n, • (Stau) -N (CH3) -R wherein / Stau / represents a residue of partial formula H[Stau] in je R aciklični, karbociklični ali karbociklično-aciklični ogljikovodikov ostanek R°, ki ima skupno največ 30 atomov ogljika, in ki je lahko nasičen ali nenasičen in nesubstituiran ali substituiran, pri čemer lahko namesto enega, dveh ali večih atomov ogljika nastopajo enaki ali različni heteroatomi, izbrani izmed kisika, žvepla in dušika; ali acil Ac, ki ima največ 30 atomov ogljika; kot tudi soli spojin s formulo I s solotvornimi lastnostmi, označen s tem, da stavrosporin s formulo (Stauj-NH-CH^ (II), kjer ima (Stau) zgoraj navedeni pomen, ali njegovo kislinsko adicijsko sol, presnovimo z reagentom s formulo R-Y (III) - 68 - kjer ima R zgoraj navedene pomene in Y pomeni reakcije sposobno aktivirano hidroksilno skupino ali dodatno enojno vez, katere drugi konec nadomešča vodik v ostanku R, ter po želji dobljeno spojino s formulo I pretvorimo v neko drugo spojino s formulo I in/ali v prosti obliki dobljeno spojino s formulo I pretvorimo v njeno sol; in/ali spojino s formulo I, dobljeno kot sol, prevedemo v njeno prosto obliko ali neko drugo sol. Za CIBA-GEIGY AG:[Stau] and R is an acyclic, carbocyclic or carbocyclic-acyclic hydrocarbon residue R 0 having a total of not more than 30 carbon atoms and which may be saturated or unsaturated and unsubstituted or substituted, with one, two or more carbon atoms in place. the same or different heteroatoms selected from oxygen, sulfur and nitrogen; or acyl Ac having a maximum of 30 carbon atoms; as well as salts of the compounds of formula I with salting properties, characterized in that the staurosporine of formula (Stauj-NH-CH2 (II), wherein (Stau) has the above meaning, or its acid addition salt, is reacted with a reagent of formula RY (III) - 68 - wherein R has the meanings given above and Y represents a reactive hydroxyl group or an additional single bond, the other end of which is replaced by hydrogen in the residue R, and optionally the resulting compound of formula I is converted into another compound of formula I and / or in free form the compound of formula I obtained is converted into its salt, and / or the compound of formula I obtained as salt is converted into its free form or some other salt For CIBA-GEIGY AG:66
SI8811154A1987-06-151988-06-14Process for the preparation of staurosporine derivatives substituted on methylamine nitrogen
SI8811154B
(en)
Desazapulin-nucleoside derivatives, methods for their preparation, pharmaceutical compositions containing them, their use for hexane configuration and their use as antiviral agents