IPROVED PROCESS FOR PREPARING 4'-EPI-DOXORUBICIN

The known cpd., 4'-epidoxorubicine hydrochloride of formula (I), is made from N-trifluoroacetyl daunorubicin by (a) oxidising in 4'-position to obtain 4'-keto N-trifluoroacetyl daunorubicin, (b) stereo-specific redn. of the 4'-keto gp. and hydrolysis of the N-protecting gp. to ob...

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Hauptverfasser: ARCAMONE,FEDERICO,IT, PENCO,SERGIO,IT, SUARATO,ANTONIO,IT
Format: Patent
Sprache:eng
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Zusammenfassung:The known cpd., 4'-epidoxorubicine hydrochloride of formula (I), is made from N-trifluoroacetyl daunorubicin by (a) oxidising in 4'-position to obtain 4'-keto N-trifluoroacetyl daunorubicin, (b) stereo-specific redn. of the 4'-keto gp. and hydrolysis of the N-protecting gp. to obtain 4'-epidaunorubicin, (c) reacting with bromine to the 14'-bromo deriv., and (d) hydrolysis with aq. sodium formate soln. and isolation as hydrochloride