Title:
【発明の名称】バッカチン▲III▼及び10-デアセチルバッカチン▲III▼のエステル化のための新規な方法
Document Type and Number:
Japanese Patent JP3064419
Kind Code:
B2
Abstract:
PCT No. PCT/FR93/00965 Sec. 371 Date Apr. 5, 1995 Sec. 102(e) Date Apr. 5, 1995 PCT Filed Oct. 4, 1993 PCT Pub. No. WO94/07876 PCT Pub. Date Apr. 14, 1994This invention relates to a method of preparing esters of baccatine III or 10-deacetylbaccatine III of formula (I) by esterification of protected baccatine III or 10-deacetylbaccatine III of formula (II) by means of an activated acid of formula (III). The esters of formula (I) can be used to prepare taxane derivatives having remarkable antileucemia and antitumor properties. In formulae (I), (II) and (III) Ar is an aryl radical, R1 is a hydrogen atom or an aryl radical or an R4-O-CO- radical (R4=alkenyl, alkynyl, optionally substituted alkyl, cycloalkyl, cycloalkynyl, bicycloalkyl, phenyl, heterocyclyle) and R2 is a hydrogen atom, and R3 stands for a hydroxy function protection grouping, or R1 is defined as above and R2 and R3 together form a 5 or 6 membered, saturated heterocyclic ring, G1 is an acetyl radical or a hydroxy function protection grouping, G2 is a hydroxy function protection grouping, and X is an acyl radical, aryl, radical or halogen atom. (I) (II) (III)
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Inventors:
Deni, Jean-Noel
Green,andreux
Ma, Jean-Manuel
Green,andreux
Ma, Jean-Manuel
Application Number:
JP50878594A
Publication Date:
July 12, 2000
Filing Date:
October 04, 1993
Export Citation:
Assignee:
Loan-Poulin L'Oré Societe Anonym
International Classes:
C07C271/22; C07D263/04; C07D263/06; C07D305/14; C07D413/12; (IPC1-7): C07D305/14
Domestic Patent References:
| JP383956A | ||||
| JP8501788A | ||||
| JP8501789A | ||||
| JP6501790A | ||||
| JP7503477A | ||||
| JP7503721A | ||||
| JP6504771A |
Other References:
Ｔｅｔｒａｈｅｄｒｏｎ Ｌｅｔｔ．，Ｖｏｌ．３３，Ｎｏ．３６，ｐ．５１８５−５１８８（１９９２）
Attorney, Agent or Firm:
Heikichi Odashima