Method of producing 4'-epidaunomycin

专利摘要:
METHOD OF OBTAINING UNOMYCIN OF THE FORMULA ON IT ON IT OSH. О ОН Д ™ d-0 №; JH2-HC1 characterized in that, in order to simplify the process and increase the yield of the target product, the N-trifluoroacetyldaunomycin of the formula O but NHCOCF dissolved in anhydrous methylene chloride is subjected to oxidation at the C-4 hydroxyl group by dimethyl sulfoxide activated by trifluoroacetic anhydride, from -60 to -65 C, the reaction mixture is alkalinized with 1,5-diazo6cyclo
公开号:SU1181549A3
申请号:SU803213106
申请日:1980-11-21
公开日:1985-09-23
发明作者:Суарато Антонио；Пенсо Серджио；Аркамоне Федерико
申请人:Фармиталия Карло Эрба С.П.А.(Фирма)；
IPC主号:

专利说明:

to remove N-trifluoroacetyl hydrogen scrubbing in methanol to produce a subsequent α-treating base
4 Epidaunomycin chloride solution
1181549 ate of the corresponding hydrochloride ta.

权利要求:
Claims (1)
[1]
METHOD FOR PRODUCING 4'-EPIDA characterized in that, in order to simplify the process and increase the yield of the target product, N-trifluoroacetyldaunomycin of the formula dissolved in anhydrous methylene chloride is subjected to oxidation at the C-h-hydroxyl group with dimethyl sulfoxide activated by trifluoroacetic acid at temperature -60 to -65 ° C, the reaction mixture was basified with 1,5-diazabicyclo (4.3.0) non-5-ene to give April ¹ -keto-11-triftoratsetildaunomitsina formula is subjected to a selective recovery stereospecific borgid sodium idom at -10 ° C, and the resulting conformity 4'-hydroxy-derivative of for-
SU, 1181549 are subjected to alkaline hydrolysis with 0.1 N aqueous sodium hydroxide to remove the N-trifluoroacetyl protection followed by treating the 4-epidauiomycin base with a solution of hydrogen chloride in methanol to give the corresponding hydrochloride.

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法律状态:

优先权:

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申请号 | 申请日 | 专利标题

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GB7940457|1979-11-22|

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