Title:
22-OXACHOLECALCIFEROL DERIVATIVE AND ITS PRODUCTION
Document Type and Number:
Japanese Patent JP3493037
Kind Code:
B2
Abstract:
PURPOSE: To efficiently obtain the new derivative for antitumor agents, antilithium agents, etc., by reacting specific hydroxypregnenes with acrylamides and then successively subjecting the reactional product to treatment with an organic metal, introduction of double bond, irradiation of ultraviolet rays and thermal isomerization reaction.
CONSTITUTION: A compound of formula I (R4 is H or (protected) hydroxyl group; R5 is (protected) hydroxyl group; R6 and R7 are H or together form double bond) is made to react with acrylic amides of formula II (R8 is 1-5C dialkylamino) in an organic solvent or a water-organic solvent system to afford a compound of formula III and the compound of formula III is made to react with an organometallic compound of the formula R9X (R9 is 1-5C alkyl; X is alkali metal, alkaline earth metal halide, etc.) to give a compound of formula IV (R2 and R3 are 1-5C alkyl). Then the compound of formula IV wherein R6 and R7 are H is subjected to halogenation at allyl position and dehydrohalogenation reaction to introduce a double bond thereto and then subjected to irradiation with ultraviolet rays in an organic solvent and successively subjected to thermal isomerization to provide the objective 22- oxacholecalciferol derivative expressed by formula V (R1 is H or OH).
Inventors:
Masahiro Kato
Tetsuhiro Mikami
Hiroyoshi Watanabe
Noboru Kubodera
Kiyonari Ochi
Tetsuhiro Mikami
Hiroyoshi Watanabe
Noboru Kubodera
Kiyonari Ochi
Application Number:
JP35436292A
Publication Date:
February 03, 2004
Filing Date:
November 27, 1992
Export Citation:
Assignee:
Chugai Pharmaceutical Co., Ltd.
International Classes:
A61P3/02; A61P5/12; A61K31/59; A61P29/00; A61P35/00; C07C401/00; C07J7/00; C07J51/00; C07J71/00; (IPC1-7): C07C401/00; A61K31/59
Domestic Patent References:
| JP3188061A | ||||
| JP61267550A |
Attorney, Agent or Firm:
Kazuo Shamoto (4 outside)