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Title:
GLUCOPYRANOSIDE BENZOTHIOPHENE
Document Type and Number:
Japanese Patent JPH07316180
Kind Code:
A
Abstract:

PURPOSE: To obtain the subject new compound useful for decrease in serum cholesterol concentration and suppression of bone resorption and decrease in bone mass.

CONSTITUTION: This new compound is 6-raloxifene-β-D-glucopyranoside of formula I or 4-raloxifene-β-D-glucopyranoside of formula II or their salts or solvates thereof. This compound is obtained e.g. by reacting raloxifene with t- butyldimethylsilyl chloride in the presence of a dimethylaminopyridine to yield a compound of formula III, reacting the resultant compound with 1,2,3,4-O- tetraacetyl-D-glucopyranuric acid methyl ester in the presence of boron trifluoride etherate in anhydrous CH2Cl2 to yield uronic acid.methyl-1-(6-t- butyldimethylsilyl-4'-hydroxy-raloxifene)-2,3,4-tri-O-acetyl-β-D-glucopyranoside, finally reacting the resultant product with LiOH hydrate in dioxane followed by reaction with tetrabutylammonium fluoride.


Inventors:
JIEFURII ARAN DOTSUJI
CHIYAARUZU ARAN FURORITSUKU
TERII DONARUDO RINDOSUTOROMU
CHIYAARUZU UIRISU RAGAA ZA SAA
GIRUBAATO SUTANRII SUTEITON
Application Number:
JP11833895A
Publication Date:
December 05, 1995
Filing Date:
May 17, 1995
Export Citation:
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Assignee:
LILLY CO ELI
International Classes:
A61K31/38; A61K31/70; A61K31/7028; A61K31/7042; A61P3/00; A61P3/06; A61P43/00; C07H15/26; C07H17/00; (IPC1-7): C07H15/26; A61K31/70; C07H17/00
Attorney, Agent or Firm:
Aoyama Ryo (1 person outside)