| 摘要 |
<p>PURPOSE: A method for preparing retiferol derivatives in high yield is provided, which derivatives are useful for the treatment or prevention of hyperproliferative skin diseases and for reversing the conditions associated with photodamage. CONSTITUTION: The method comprises the step of coupling the ketones of the formula(2) with the compounds of formula(3), or coupling the phosphine oxides of the formula(4) with the aldehydes of the formula(5), wherein A is -C=C- or -CH=CH-; R1 and R2 are independent each other and are a lower alkyl group or a lower perfluoroalkyl group; X1 and X2 are a protecting group of hydroxy group; and Y is a protection group of hydroxy group. Preferably X1 and X2 are independent each other and are a monoalkyl dimethylsilyl group of C1-C4 alkyl or an acyl group R3CO- (wherein R3 is a lower alkyl group or a monochlorinated lower alkyl group), and Y is a trialkylsilyl group of C1-C4 alkyl.</p> |
