VITAMIN D3 DERIVATIVE AND ITS PRODUCTION

Japanese Patent JP3595025

B2

PURPOSE: To obtain a new 1α-hydroxyvitamin D3 derivative useful as a medicine such as a bone formation promoter, an immunosuppressor, a tumor cell proliferation suppressor or an agent for hypercalcemia agent.
CONSTITUTION: This vitamin D3 derivative is expressed by formula I, e.g. 1α hydroxy-22-[(1-hydroxy-1-methyl)-2-cyclopentene-4-yl]-23, 24, 25, 26, 27-pentanoyl- vitamin D3. This vitamin D3 derivative of formula I is obtained by reacting a new cyclopentene derivative of formula II with a compound of formula III [R2 and R3 are each H, a tri(1-7C hydrocarbon)silyl, a 2-7C acyl or a group forming an acetal bond together with O of OH] in the presence of Pd catalyst to afford a vitamin D3 derivative of formula IV and subjecting the resultant derivative to deprotecting reaction except when R1, R2 and R3 are simultaneously H. Cyclopentene derivative) of formula V (R12 is same as R2 and R3) and formula VI (R12 is same as R2 and R3) are new substances.

Tabe Masayasu
Kenji Manabe
Atsuo Hari
Yuko Tanaka
Seiichi Ishizuka

JP13782195A

December 02, 2004

June 05, 1995

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Teijin Limited

A61K31/59; A61P3/02; A61P3/14; A61P7/00; A61P19/10; A61P35/00; A61P37/06; A61P43/00; C07C29/44; C07C35/21; C07C35/52; C07C43/30; C07C49/737; C07C69/145; C07C401/00; C07F7/18; (IPC1-7): C07C401/00; A61K31/59; A61P3/14; A61P19/10; A61P35/00; A61P37/06

JP60185715A
JP58210011A
JP58118516A
JP5271183A
JP5239018A

WO1993016022A1

Journal of Medicinal Chemistry,1991年,34(8),p.2452-2463

Hideko Mihara

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