申请人:ISHIHARA SANGYO KAISHA, LTD.
公开号:EP2338335A1
公开(公告)日:2011-06-29
A process for producing a benzoylpyridine derivative represented by the following formula (I) or its salt:
(wherein X is a halogen atom, a nitro group, a substitutable hydrocarbon group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group, a hydroxyl group, a substitutable alkylthio group, a cyano group, a carboxyl group which may be esterified or amidated, or a substitutable amino group; n is 1, 2, 3 or 4; R' is a substitutable alkyl group; R2' is a substitutable alkyl group, a substitutable alkoxy group, a substitutable aryloxy group, a substitutable cycloalkoxy group or a hydroxyl group; p is 1, 2 or 3; and R2" is a substitutable alkoxy group or a hydroxyl group; wherein at least two of R2' and R2" may form a condensed ring containing an oxygen atom);
characterized by reacting a compound represented by the formula (XIII):
(wherein X and n are as defined above) with a compound represented by the formula (XIV):
(wherein R1, R2', R2" and p are as defined above) in the presence of a Lewis acid or a dehydrating agent.
一种生产下式 (I) 所代表的苯甲酰吡啶衍生物或其盐的工艺:
(其中 X 是卤原子、硝基、可被取代的烃基、可被取代的烷氧基、可被取代的芳氧基、可被取代的环烷氧基、羟基、可被取代的烷硫基、氰基、可被酯化或酰胺化的羧基或可被取代的氨基;n 是 1、2、3 或 4;R'是可被取代的烷基;R2'是可被取代的烷基、可被取代的烷氧基、可被取代的芳氧基、可被取代的环烷氧基或羟基;p 是 1、2 或 3;R2 "是可被取代的烷氧基或羟基;其中至少两个 R2'和 R2 "可形成含有一个氧原子的缩合环);
其特征是使式 (XIII) 所代表的化合物发生反应:
式(XIII)代表的化合物(其中X和n如上定义)与式(XIV)代表的化合物反应:
(其中 R1、R2'、R2 "和 p 如上定义)的化合物在路易斯酸或脱水剂存在下反应。