Verfahren zur Herstellung von Mitosan-Derivaten

Antibiotic derivatives of mitosene having the formula wherein X is -OR, -NH2, -NHR, or -NR2R3, Z is H or R5 and each of R, R1, R2, R3, R4 and R5 are lower alkyl radicals having 1 to 6 carbon atoms are prepared by heating a compound having the formula with an acid anhydride having the formula Alka...

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Hauptverfasser: MATSUI,MASANAO, UZU,KEIZO, WAKAKI,SHIGETOSHI
Format: Patent
Sprache:ger
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Zusammenfassung:Antibiotic derivatives of mitosene having the formula wherein X is -OR, -NH2, -NHR, or -NR2R3, Z is H or R5 and each of R, R1, R2, R3, R4 and R5 are lower alkyl radicals having 1 to 6 carbon atoms are prepared by heating a compound having the formula with an acid anhydride having the formula Alkaline hydrolysis with, for example ammonia, sodium carbonate or triethylamine of compounds having Formula (I) above gives compounds of formula Examples relate to the preparation of 1 - acetoxy - 2 - acetamino - 7 - amino mitosene and 1 - acetoxy - 2 - acetamino - 7 - methoxy mitosene from acetic anhydride and Mitomycin C and Mitomycin A respectively and the subsequent hydrolysis with methanolic ammonia to 1-hydroxy-2-acetoamino-7-amino mitosene and 1 - hydroxy - 2 - acetamino - 7 - methoxy mitosene respectively.