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    • 4. 发明申请
    • PROCESS FOR PRODUCING 1,4-BENZODIOXANE DERIVATIVES
    • 生产1,4-苯二酮衍生物的方法
    • WO1996030360A1
    • 1996-10-03
    • PCT/JP1996000727
    • 1996-03-21
    • DAISO CO., LTD.FURUKAWA, YoshiroKITAORI, KazuhiroTAKENAKA, Keishi
    • DAISO CO., LTD.
    • C07D319/20
    • C07D319/20Y02P20/55
    • A novel process for producing 1,4-benzodioxane derivatives represented by general formula (1), which are useful as intermediates in the production of remedies for circulatory diseases and psychoneurotic diseases, comprising sulfonating a phenoxypropanediol compound by reacting with a sulfonyl halide compound, eliminating the protecting group, treating with a base to thereby subject to a ring closure reaction followed by, if required, further sulfonation. In said formula R represents H or RSO2 (wherein R represents alkyl or optionally alkyl-substituted phenyl); and R , R and R represent each H, halogeno, OH, NO2, CN, formyl, COOH, alkoxycarbonyloxy, alkyl, alkoxy, haloalkyl, N,N-dialkylamino, alkylcarbonyl, alkoxycarbonyl, optionally alkyl-substituted phenyl, etc.
    • 一种用于生产由通式(1)表示的1,4-苯并二恶烷衍生物的新方法,其可用作生产循环系统疾病和精神神经病疾病的药物的中间体,包括通过与磺酰卤化合物反应来磺化苯氧基丙二醇化合物,消除 保护基团,用碱处理,从而进行闭环反应,随后如果需要,进一步磺化。 在所述式中,R 1表示H或RSO 2(其中R表示烷基或任选被烷基取代的苯基); R 2,R 3和R 4分别表示H,卤代,OH,NO 2,CN,甲酰基,COOH,烷氧基羰基氧基,烷基,烷氧基,卤代烷基,N,N-二烷基氨基,烷基羰基, 烷基取代的苯基等
    • 7. 发明申请
    • PROCESS FOR PREPARING 1,3-DIOXOLANE-4-METHANOL COMPOUNDS
    • 制备1,3-二氧杂环戊烷-4-甲醇化合物的方法
    • WO1998011088A1
    • 1998-03-19
    • PCT/JP1997003166
    • 1997-09-09
    • DAISO CO., LTD.HINOUE, KazumasaFURUKAWA, Yoshiro
    • DAISO CO., LTD.
    • C07D317/22
    • C07D317/20
    • A process for preparing 1,3-dioxolane-4-methanol compounds in a racemic modification form and an optically active form having a high purity in a high yield in a simple and cost-effective manner. The process comprises reacting a 3-halogeno-1,2-propanediol (1a) (wherein X represents a halogen atom) or a glycidol with an alcohol in the presence of a base, acetalating the resultant 3-alkoxy-1,2-propanediol in the presence of an acid catalyst, and further conducting hydrogenation in the presence of a reduction catalyst to prepare a 1,3-dioxolane-4-methanol compound (5) (wherein R and R represent each hydrogen, an alkyl group having 1 to 4 carbon atoms, or a phenyl group, or R and R together with the adjacent carbon atom may form a three- to six-membered ring).
    • 以简单且成本有效的方式以高产率制备外消旋体形式的1,3-二氧戊环-4-甲醇化合物和具有高纯度的光学活性形式的方法。 该方法包括在碱的存在下使3-卤代-1,2-丙二醇(1a)(其中X表示卤素原子)或缩水甘油与醇反应,缩合所得3-烷氧基-1,2-丙二醇 在酸催化剂的存在下,在还原催化剂的存在下进一步进行氢化以制备1,3-二氧戊环-4-甲醇化合物(5)(其中R 1和R 2各自代表氢, 具有1至4个碳原子的烷基或苯基,或R 1和R 2与相邻碳原子一起可以形成三至六元环)。