申请人:NIPPON SODA CO., LTD.
公开号:EP1142857A1
公开(公告)日:2001-10-10
Processes for producing a compound (1) represented by formula (1), which includes an acrylic acid derivative and is useful as an agricultural chemical or medicine. One of the processes comprises the step of formylating a compound (3) (step (1)) and the step of converting the OH of the resultant compound (2) into OR" (step (2)). The step (1) comprises reacting a formic or orthoformic ester in the presence of a Lewis acid and a base. The step (2) comprises [1] reacting the compound (2) with R" OH or with R" OH and CH(OR")3 under acidic conditions or [2] using a phase-transfer catalyst in a two-phase system and regulating the base and the concentration thereof to stereoselectively synthesize the target compound. In another process, the compound (1) is efficiently produced without isolating the compound (2). In still another process, the compound (1) is directly produced without via the compound (2).
生产由式(1)表示的化合物(1)的工艺,该化合物包括丙烯酸衍生物,可用作农用化学品或药物。其中一种工艺包括将化合物(3)甲酰化的步骤(步骤(1))和将所得化合物(2)的 OH 转化为 OR 的步骤(步骤(2))。步骤(1)包括在路易斯酸和碱存在下使甲酸酯或原甲酸酯发生反应。步骤(2)包括[1] 在酸性条件下,使化合物(2)与 R" OH 或与 R" OH 和 CH(OR")3 反应,或[2] 在两相体系中使用相转移催化剂,调节碱及其浓度,立体选择性地合成目标化合物。在另一种工艺中,无需分离化合物(2)即可高效生产化合物(1)。在另一种工艺中,不通过化合物(2)直接生产化合物(1)。