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Title:
NEW VITAMIN D DERIVATIVE, THERAPEUTIC APPLICATION AND APPLICATION TO ASSAY OF METABOLITE OF VITAMIN D
Document Type and Number:
Japanese Patent JPH02262555
Kind Code:
A
Abstract:

NEW MATERIAL: Compd. of formula I [wherein R1 is a 1-15C substd. alkyl, in particular a side chain of vitamin D2 (20-28C) or vitamin D3 (20-27C); Y is H, OH, etc.; X is a 1-6C alkyl, an arom. or a heterocyclic ring, etc.; R2 and R3 are H, or methyl but they are not methyl at the same time or both CH2 together].

EXAMPLE: 11α-(2-hemisuccinoyloxyethyl)-1,25,(OH)2-vitamin D3.

USE: Being useful for therapy of diseases caused by shortage or excess of vitamin D. In addition, being useful for labelling of radioisotopes for assays of metabolites of vitamin D and formation of enzyme-labelled tracers.

PROCESS: A compd. of formula II or formula III is reacted with formula IV (wherein R6 is a protective group for hydroxyl) in the presence of n-butyl lithium and then, elimination of protection is performed to obtain a compd. of formula I.


Inventors:
ROJIE BUIYON
PIEERU JIYAN DOU KURERUKU
PIEERU ERIAARU
MOORI BANDOUWAARU
Application Number:
JP11400389A
Publication Date:
October 25, 1990
Filing Date:
May 06, 1989
Export Citation:
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Assignee:
I L EE MEDOJIENITSUKUSU SA
International Classes:
G01N33/50; A61K31/59; A61P3/02; C07B59/00; C07C49/733; C07C49/753; C07C401/00; G01N33/53; G01N33/82; (IPC1-7): C07C401/00; A61K31/59; C07C49/733; C07C49/753; G01N33/50; G01N33/53
Domestic Patent References:
JPS5387344A1978-08-01
JPS5388316A1978-08-03
JPS58193463A1983-11-11
JPH02274A1990-01-05
Attorney, Agent or Firm:
Kazuo Sato (2 outside)