Title:
2'-DEOXY-2'-FLUOROCOFORMYCIN AND STEREOISOMERS THEREOF
Document Type and Number:
WIPO Patent Application WO/1993/010137
Kind Code:
A1
Abstract:
2'-Deoxy-2'-fluorocoformycin and 2'-deoxy-8-epi-2'-fluorocoformycin have now been synthesized by a multistage reaction via 3,5-di-O-benzoyl-2-deoxy-2-fluoro-alpha- and -beta-D-ribofuranosyl bromide. Also 2'-deoxy-2'-epi-2'-fluorocoformycin and 2'-deoxy-8,2'-diepi-2'-fluorocoformycin have been synthesized from 3,5-di-O-benzoyl-2-deoxy-2-fluoro-alpha-D-arabinofuranosyl bromide by a multistage reaction. These four 2'-fluorocoformycin derivatives are novel compounds and have a potent enzyme inhibiting activity against adenosine deaminase. In particular, they are useful for treating acute lymphocytic leukemia in virtue of the above activity. Other novel compounds also obtained include various intermediates useful for the synthesis of the above derivatives.
Inventors:
TAKEUCHI TOMIO (JP)
UMEZAWA SUMIO (JP)
TSUCHIYA TSUTOMU (JP)
TAKAHASHI YOSHIAKI (JP)
UMEZAWA SUMIO (JP)
TSUCHIYA TSUTOMU (JP)
TAKAHASHI YOSHIAKI (JP)
Application Number:
PCT/JP1992/001489
Publication Date:
May 27, 1993
Filing Date:
November 13, 1992
Export Citation:
Assignee:
ZAIDAN HOJIN BISEIBUTSU (JP)
International Classes:
C07H5/02; C07H5/06; C07H11/00; C07H19/04; C07H19/052; C07H19/23; F01K23/10; A61K31/7056; A61P31/04; A61P35/00; A61P43/00; (IPC1-7): C07H5/02; C07H5/04; C07H19/052; C07H19/23
Foreign References:
| JPS61199797A | 1986-09-04 | |||
| JPS60209598A | 1985-10-22 | |||
| JPS60116697A | 1985-06-24 | |||
| JPS63275596A | 1988-11-14 |
Other References:
CHEMICAL ABSTRACT, Vol. 92, No. 21, p. 691 (1980), Abstract No. 181528w, The Abstract for (ALENIN V.V. et al., Zh. Cbshch Khim 1979 49(12), 2755-6).
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