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Title:
VITAMIN D DERIVATIVE
Document Type and Number:
Japanese Patent JP2000219630
Kind Code:
A
Abstract:

To obtain a new derivative having an oxetane ring on a side chain, and having excellent pharmacological activity as an osteogenesis stimulating agent, a bone resorption suppressing agent or the like.

A derivative of formula I [R1 and R2 are each H or a protective group for OH; R3 is H, F, Cl or a (substituted) 1-2C alkyl; R4 is H, F, Cl or a (substituted)methyl; X1 is F or Cl; X2 is H, F or Cl; and n=1-3] or its prodrug, for example, (5Z,5E)-23S,25-epoxy-26,26,26,27,27,27-hexafluoro-9,10- secocholesta-5,7,10(19)-triene-1α,3β-diol. Further, the compound is obtained by reacting a compound of formula II with a halide of a corresponding sulfonyl compound in an aprotic solvent such as dichloromethane at a temperature from 0°C to the boiling point of the solvent in the presence of a base such as pyridine, and treating the obtained compound with an alkali.


Inventors:
IKEDA MASAHIKO
TANAKA TOMOYUKI
NOGUCHI TOSHIHIRO
MATSUMURA HARUKI
Application Number:
JP1931599A
Publication Date:
August 08, 2000
Filing Date:
January 28, 1999
Export Citation:
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Assignee:
SUMITOMO PHARMA
International Classes:
C07D305/06; A61K31/00; A61K31/59; A61K31/593; A61P3/00; A61P3/02; C07C401/00; C07F7/18; (IPC1-7): A61K31/593; A61P3/02; C07F7/18
Attorney, Agent or Firm:
Toshio Nakamura