Title:
4,10β-ジアセトキシ-2α-ベンゾイルオキシ-5β,20-エポキシ-1,13α-ジヒドロキシ-9-オキソ-19-ノルシクロプロパ[g]タキサ-11-エンの製造方法
Document Type and Number:
Japanese Patent JP4664903
Kind Code:
B2
Abstract:
Preparation of taxoid compounds (I) comprises reacting an optionally protected taxene compound (II) with a molecular sieve base in sulfolane, condensing with a side chain, and removing protecting groups. Preparation of taxoid compounds of formula (I) comprises reacting an optionally protected taxene compound of formula (II) with a basic molecular sieve in sulfolane to cyclize the 7 beta -trifluoromethyl sulfonyloxy group, condensing with a side chain, and removing protecting groups. [Image] Ar : aryl; R : H, acetyl, alkoxyacetyl or alkyl; R 1benzoyl or R 2-O-CO; R 21-8C alkyl; R' : a protecting group when R in (I) is H, or R. An independent claim is also included for the preparation of intermediate compounds of formula (III) which comprises reacting (II) with a molecular sieve base in sulfolane. [Image] ACTIVITY : None given. MECHANISM OF ACTION : None given.
Inventors:
Eric Didier
Guy Amour
Guy Amour
Application Number:
JP2006505793A
Publication Date:
April 06, 2011
Filing Date:
April 13, 2004
Export Citation:
Assignee:
Aventis Pharma Societe Anonym
International Classes:
C07D305/14
Domestic Patent References:
| JP11503443A | ||||
| JP10508015A | ||||
| JP10500979A |
Foreign References:
| US5814658 |
Other References:
CHEN,S.H. et al,Serendipitous synthesis of a cyclopropane-containing taxol analog via anchimeric participation of an unactivated angular methyl group,Journal of Organic Chemistry,1993年,Vol.58, No.17,p.4520-4521
ROTH,G.P. et al,Reaction of paclitaxel and 10-desacetyl baccatin III with diethylamino sulfurtrifluoride,Tetrahedron Letters,1995年,Vol.36, No.10,p.1609-1612
ROTH,G.P. et al,Reaction of paclitaxel and 10-desacetyl baccatin III with diethylamino sulfurtrifluoride,Tetrahedron Letters,1995年,Vol.36, No.10,p.1609-1612
Attorney, Agent or Firm:
Chika Takagi
Junji Yuda
Shoji Miwa
Junji Yuda
Shoji Miwa