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    • 1. 发明申请
    • PROCESS AND INTERMEDIATES FOR PRODUCTION OF DONEPEZIL AND RELATED COMPOUNDS
    • 二苯醚及其相关化合物的生产过程和中间体
    • WO0009483A3
    • 2001-06-21
    • PCT/IL9900436
    • 1999-08-11
    • FINETECH LTDGUTMAN L ARIESHKOLNIK ELEONORATISHIN BORISNISNEVICH GENADYZALTZMAN IGOR
    • GUTMAN L ARIESHKOLNIK ELEONORATISHIN BORISNISNEVICH GENADYZALTZMAN IGOR
    • C07B53/00C07B61/00C07D211/32C07D211/34
    • C07D211/32C07D211/34
    • The present invention relates to a new process for the preparation of acetylcholinesterase inhibitors of formula (I) or a salt thereof, wherein: R is N-acyl-4-piperidyl; N-alkoxycarbonyl-4-piperidyl; 4-piperidyl; N-alkyl-4-piperidyl; N-benzyl-4-piperidyl; N-( omega -aralkyl)-4-piperidyl; 4-pyridyl; R , R , R and R are identical or different and each represents hydrogen, straight-chain or branched alkyl, aryl, hydroxy, alkoxy, aryloxy, benzyloxy, acyloxy, alkylthio, arylthio, benzylthio, acylamino, phthalimido or halogen; n is 1, 2 or 3; m is 1, 2, 3, 4 or 5. This process comprises cyclisation of a compound of formula (II) or salts thereof, wherein R , R , R , R and R , m and n are as defined above; R is selected from a derivatised or non-derivatised carboxyl, cyano, N-substituted aminocarbonyl groups or hydrogen; R is selected from a derivatised or non-derivatised carboxyl, cyano or N-substituted aminocarbonyl groups, optionally in the presence of acids and/or solvents. One of the most potent acetylcholinesterase inhibitors of the class of compounds prepared according to the present invention is donepezil.
    • 本发明涉及制备式(I)的乙酰胆碱酯酶抑制剂或其盐的新方法,其中:R 1是N-酰基-4-哌啶基; N-烷氧羰基-4-哌啶基; 4-哌啶基; N-烷基-4-哌啶基; N-苄基-4-哌啶基; N-(ω-芳烷基)-4-哌啶基; 4-吡啶基; R 4,R 5,R 6和R 7相同或不同,各自表示氢,直链或支链烷基,芳基,羟基,烷氧基,芳氧基,苄氧基,酰氧基,烷硫基,芳硫基 ,苄硫基,酰氨基,苯二甲酰亚氨基或卤素; n为1,2或3; m为1,2,3,4或5.该方法包括式(II)化合物或其盐的环化,其中R 1,R 4,R 5,R 6和R 7,m和n如上所定义; R 2选自衍生或未衍生的羧基,氰基,N-取代的氨基羰基或氢; R 3选自衍生化或非衍生的羧基,氰基或N-取代的氨基羰基,任选在酸和/或溶剂的存在下。 根据本发明制备的化合物类别中最有效的乙酰胆碱酯酶抑制剂之一是多奈哌齐。
    • 3. 发明申请
    • PROCESS FOR THE PREPARATION OF ZAFIRLUKAST
    • 制备ZAFIRLUKAST的方法
    • WO0246153A2
    • 2002-06-13
    • PCT/IB0102268
    • 2001-11-30
    • ISP FINETECH LTDGUTMAN ARIENISNEVICH GENNADYZALTZMAN IGORPONOMAREV VICTORSOTRIHIN MAXIM
    • GUTMAN ARIENISNEVICH GENNADYZALTZMAN IGORPONOMAREV VICTORSOTRIHIN MAXIM
    • C07D209/18C07D209/24C07D209/00
    • C07D209/18C07D209/24Y02P20/582
    • The present invention provides a novel process for the preparation of alkyl (1-alkylindol-3-ylmethyl)benzoate derivatives which process comprises the steps of: (a) reacting of an alkyl (halomethyl)benzoate with excess of an indole, said indole being unsubstituted at positions 1-, 2- and 3-, under conditions promoting alkylation at the 3-position of the indole to yield a mixture comprising alkyl (indol-3-ylmethyl)benzoate and unreacted starting indole,(b) treating the mixture obtained in step (a) with base to yield a mixture, comprising the salt of (indol-3-ylmethyl)benzoic acid and the unreacted indole, (c) recovering the unreacted indole from the mixture obtained in step (b), and recycling the indole as starting material to step (a),(d) isolating the salt of (indol-3-ylmethyl)benzoic acid and/or acidifying the salt to form (indol-3-ylmethyl)benzoic acid, (e) reacting the (indol-3-ylmethyl)benzoic acid or it's salt with alkylating agent in the presence of base to form the desired alkyl (1-alkylindol-3-ylmethyl)benzoate. The above process affords also the preparation of the anti-asthmatic leukotriene antagonist zafirlukast. In such case, methyl 3-methoxy-4-(1-methyl-5-nitroindol-3-ylmethyl)benzoate [1a] is formed in step (e) of the process and this compound is subsequently converted into zafirlukast by known methods.
    • 本发明提供了一种制备烷基(1-烷基吲哚-3-基甲基)苯甲酸酯衍生物的新方法,该方法包括以下步骤:(a)使(卤代甲基)烷基烷基酯与过量的吲哚反应,所述吲哚为 在吲哚的3位上促进烷基化的条件下,在位置1-,2-和3-未被取代,得到包含烷基(吲哚-3-基甲基)苯甲酸酯和未反应的起始吲哚的混合物,(b)处理得到的混合物 在步骤(a)中与碱反应以产生包含(吲哚-3-基甲基)苯甲酸的盐和未反应的吲哚的混合物,(c)从步骤(b)中获得的混合物中回收未反应的吲哚,并将 吲哚作为步骤(a)的起始原料,(d)分离(吲哚-3-基甲基)苯甲酸的盐和/或酸化盐以形成(吲哚-3-基甲基)苯甲酸,(e)使 吲哚-3-基甲基)苯甲酸或其与烷基化剂的盐在碱的存在下形成所需的烷基 (1-alkylindol -3-基甲基)苯甲酸甲酯。 上述方法还提供了抗哮喘白三烯拮抗剂扎非司酮的制备。 在这种情况下,在该方法的步骤(e)中形成3-甲氧基-4-(1-甲基-5-硝基吲哚-3-基甲基)苯甲酸甲酯[1a],该化合物随后通过已知方法转化成扎非司酮。