| 摘要 |
<p>PURPOSE: To obtain an eosinophilic leukocyte function inhibitor containing a specific benzophenone derivative, capable of inhibiting at low levels eosinophilic leukocyte degranulation in allergic or inflammatory reactions, and excellent in e.g. the inhibitory activity on eosinophilic leukocyte wandering. CONSTITUTION: This eosinophilic leukocyte function inhibitor contains a compound (or a salt thereof) of formula I[R<1> is H or a 1-10C alkyl; R<2> is a (halogen- substituted) 1-12C alkyl; R<3> and R<4> are each H or a halogen; R<5> is the same as R<1> or a 1-10C alkoxyl; R<6> -R<8> are each the same as R<1> , a 1-6C alkylcarbonyl, etc.; R<9> is H, a 1-10C alkoxyl, etc.] [e.g. 2-(2,6-dihydroxy-4-methylbenzoyl)-5 hydroxy-3-methoxybenzoic acid methyl ester]. Of the compounds of formula I, a sulochrin (analogue) of formula II is obtained by the following process: a compound of formula III (Pa, Pb and Pc are each a protecting group) is used as the starting material to form a compound of formula IV (Bn is benzyl), which is, in turn, reacted with the lithiated product of 1,3-bis (methoxy)-5 methylbenzene followed by a compound of formula R<2> -OH and the resultant product is debenzylated.</p> |
