Title:
【発明の名称】半合成のジアステレオマー的に純粋なN-グリシジルアントラサイクリンの立体選択的な製造方法
Document Type and Number:
Japanese Patent JP3299293
Kind Code:
B2
Abstract:
The invention relates to anthracyclines with cytostatic activity and the formula I, which are optionally in the form of a salt of an inorganic or organic acid, in which R<1> is hydrogen or a hydroxyl group, R<2> is hydrogen, a hydroxyl group or an alkyloxy group (C1-C4), R<3> is hydrogen, a hydroxyl group or a structure of the formula II, R<4> is CH2CH3, COCH3, COCH2OH, CHOHCH3 or CHOHCH2OH, R<5> is hydrogen, a hydroxyl group, a methoxycarbonyl group or a structure of the formula II, R<6> is hydrogen, an alkyl group (C1-C4), an allyl group, a benzyl group or mono- or dimethyloxy-substituted benzyl group, a tetrahydropyranyl group, R<7> is hydrogen, an alkyl group (C1-C4), an allyl group, a benzyl group or mono- or dimethyloxy-substituted benzyl group, and R<8> is a structure of the formula III or IV, and to a process for the preparation of these compounds, characterised in that an anthracycline derivative of the structure I in which R<1>, R<2> and R<4> are as defined above, and R<3> is hydrogen, a hydroxyl group or a structure of the formula V, R<5> is hydrogen, a hydroxyl group, a methoxycarbonyl group or a structure of the formula V and R<6> and R<7> are as defined above, is reacted with (R)- or (S)-glycidyl sulphonate.
Inventors:
Manfred Gelken
Monica Grimm
Ernst Rhap
Dieter Hoffman
Liner Shoutrop
Monica Grimm
Ernst Rhap
Dieter Hoffman
Liner Shoutrop
Application Number:
JP32404891A
Publication Date:
July 08, 2002
Filing Date:
November 13, 1991
Export Citation:
Assignee:
HOECHST AKTIENGESELLSCHAFT
International Classes:
A61K31/70; A61K31/704; A61P35/00; C07B53/00; C07C15/62; A61K31/65; C07C50/36; C07H15/252; C07H15/26; (IPC1-7): C07H15/252; C07B53/00
Domestic Patent References:
| JP225497A | ||||
| JP1279887A | ||||
| JP52133983A |
Other References:
Ｔｅｔｒａｈｅｄｒｏｎ，１９８８，Ｖｏｌ．４４，Ｎｏ．１１，Ｐ３２８９−３２９４
Attorney, Agent or Firm:
Chika Takagi (2 outside)