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.
WO/2023/200893 | SMALL MOLECULE ENHANCERS OF ANTISENSE OLIGO ACTIVITY |
JPH06247850 | 12-LIPOXYGENASE INHIBITOR |
CHIYAARUZU ARAN FURORITSUKU
TERII DONARUDO RINDOSUTOROMU
CHIYAARUZU UIRISU RAGAA ZA SAA
GIRUBAATO SUTANRII SUTEITON