Title:
【発明の名称】アントラサイクリノンの製造方法
Document Type and Number:
Japanese Patent JP2717023
Kind Code:
B2
Abstract:
Process for preparing anthracyclinones of general formula (I): wherein R represents a hydrogen atom or a COOR1 group in which R1 may be a hydrogen atom or an optionally substituted C1-C10 alkyl group, which are intermediates in the preparation of antitumor anthracycline glycosides, are prepared by: (i)(a) reacting a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V): wherein R min represents an alkyl group having from 1 to 10 carbon atoms optionally substituted by one or more halogen atoms or an aryl group optionally substituted by halogen, alkyl, alkoxy or nitro, in a reducing environment with a catalytic amount of a compound of formula (VIII): MLnL min m wherein M represents a transition metal atom, L and L min , which may be the same or different, each represent an anion or a neutral molecule and n and m may vary from 0 to 4, such as to obtain a compound of formula (VII): wherein R represents hydrogen; or (b) carbonylating a 4-demethyl-4-sulfonyl-7-deoxy-13-dioxolanyl daunomycinone of formula (V) as defined above, with carbon monoxide in the presence of a nucleophile R1OH wherein R1 is as defined above, an organic or inorganic base and as catalyst a compound of formula (VIII) as defined above, such as to obtain a compound of formula (VII) as shown above wherein R represents a COOR1 group; and (ii) introducing an alpha -hydroxy group at the 7-position and removing the 13-oxo protecting group by acid hydrolysis from the resultant compound of formula (VII). r
Inventors:
Cabri, Bartel
Candeani, Ilaria
De Bernardinis, Sylvia
Franca Ranch, Franco
Candeani, Ilaria
De Bernardinis, Sylvia
Franca Ranch, Franco
Application Number:
JP50416390A
Publication Date:
February 18, 1998
Filing Date:
February 28, 1990
Export Citation:
Assignee:
Farmacia e Appzyon Esset Pear
International Classes:
B01J31/12; C07B61/00; C07C46/00; C07C49/423; C07C49/727; B01J27/128; C07C50/36; C07C50/38; (IPC1-7): C07C50/38; C07C46/00
Domestic Patent References:
| JP4500956A | ||||
| JP1308243A | ||||
| JP63313796A |
Attorney, Agent or Firm:
Yoshio Kawaguchi (5 outside)