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Title:
1BETA-HYDROXYVITAMIN D3 DERIVATIVE
Document Type and Number:
Japanese Patent JP3678446
Kind Code:
B2
Abstract:

PURPOSE: To obtain a new 1β-hydroxyvitamin D3 derivative useful as an agonist or an antagonist for vitamin D3.
CONSTITUTION: This 1β-hydroxyvitamin D3 derivative comprises a compound of the formula [R1 is a 3-10C straight-chain or branched-chain alkyl which may be substituted with one or more OHs or an OR3 (R3 is a 3-10C straight- chain or branched-chain alkyl which may be substituted with one or more OHs); R2 is H or a 1-6C alkyl which may be substituted with one or more OHs; with the proviso that in the case in which R1 is 4-methylpentyl or 4-hydroxy-4- methylpentyl, R2 is not H] or its optically active substance such as 1β,3β- dihydroxy-2β-(3-hydroxypropoxy)-9,10-secocholesta-5,7,10(19)-triene. The compound is obtained by selectively oxidizing OH at the 1-position as the allyl position of a corresponding 1α hydroxylated compound with a proper oxidizing agent (e.g. MnO2), reducing the resultant substance with NaBH4, etc., to selectively give a pre 1β derivative, then thermally isomerizing the derivative.


Inventors:
Kuboji Noboru
Yoshiyuki Ono
Application Number:
JP30416194A
Publication Date:
August 03, 2005
Filing Date:
November 01, 1994
Export Citation:
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Assignee:
Chugai Pharmaceutical Co., Ltd.
International Classes:
A61K31/59; A61P3/02; A61P3/14; A61P19/10; A61P37/00; A61P37/02; A61P43/00; C07C401/00; (IPC1-7): C07C401/00
Domestic Patent References:
JP2011563A
JP1238566A
JP62298572A
JP54063058A
JP54103855A
Attorney, Agent or Firm:
Hiroshi Kobayashi
Eiji Katayama
Junko Kobayashi