PROCESS FOR THE PREPARATION OF ARYLOXYPROPYLAMINES
    3.
    发明申请
    PROCESS FOR THE PREPARATION OF ARYLOXYPROPYLAMINES 审中-公开
    制备芳基丙烯酰胺的方法

    公开(公告)号:US20070270483A1

    公开(公告)日:2007-11-22

    申请号:US11749977

    申请日:2007-05-17

    IPC分类号: A61K31/381 C07D333/22

    CPC分类号: C07C213/08 Y02P20/55

    摘要: A process for preparation of a compound of formula (I), or a salt thereof, both as individual isomer and as mixtures thereof, wherein each of A and B is independently aryl or heteroaryl optionally substituted with 1 to 4 substituents; and R and R1, which can be the same or different, are hydrogen, C1-C6 alkyl or an amino-protecting group; comprising the reaction of a compound (II) wherein A and B are as defined above, with a compound (III) wherein each of R and R1 is independently C1-C6 alkyl or an amino-protecting group; and X is a leaving group; in the presence of a basic agent; and, if desired the conversion of a compound (I) to another compound (I); and/or, if desired, the separation of an isomeric mixture of a compound (I) into the individual isomers; and/or, if desired, the conversion of a compound (I) to a salt thereof.

    摘要翻译: 制备式(I)化合物或其盐作为单独异构体及其混合物的方法,其中A和B各自独立地为任选被1至4个取代基取代的芳基或杂芳基; R 1和R 2可以相同或不同,为氢,C 1 -C 6烷基或氨基保护基 ; 包括其中A和B如上定义的化合物(II)与化合物(III)的反应,其中R和R 1各自独立地为C 1〜 C 6烷基或氨基保护基; X为离去群; 在一个基本代理人的面前; 并且如果需要,化合物(I)转化为另一化合物(I); 和/或如果需要,将化合物(I)的异构体混合物分离成单独的异构体; 和/或如果需要,化合物(I)转化为其盐。

    PROCESS FOR THE PREPARATION OF PYRIDINE COMPOUNDS
    4.
    发明申请
    PROCESS FOR THE PREPARATION OF PYRIDINE COMPOUNDS 失效
    制备吡啶化合物的方法

    公开(公告)号:US20070249662A1

    公开(公告)日:2007-10-25

    申请号:US11737852

    申请日:2007-04-20

    CPC分类号: C07D471/04 C07D401/12

    摘要: A process for preparation of a compound of formula (I), both as the isomeric mixture and individual isomers, wherein Q is ═CR8— or ═N—; each R1, R2, R3, R4 is independently selected from hydrogen, halogen, hydroxy; nitro; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen or C1-C6 alkoxy; phenyl-C1-C6 alkyl; phenyl-C1-C6 alkoxy; and —N(RaRb) wherein each Ra and Rb is independently hydrogen or C1-C6 alkyl or Ra and Rb, taken together with the nitrogen atom they are linked to, form a saturated heterocyclic ring; andeach R5, R6, R7, R8 is independently selected from hydrogen, halogen, hydroxy; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen; C1-C6 alkyl-carbonyl, C1-C6 alkoxy-carbonyl, and oxazol-2-yl; comprising converting a compound of formula (IV), to said compound of formula (I), in the presence of a catalyst, if necessary in an organic solvent.

    摘要翻译: 制备式(I)化合物的方法,均为异构体混合物和各异构体,其中Q为-CR 8 - 或-N-; 每个R 1,R 2,R 3,R 4,R 4独立地选自氢,卤素,羟基; 硝基 任选被羟基取代的C 1 -C 6烷基; 烷硫基C 1 -C 6烷基; 任选被卤素或C 1 -C 6烷氧基取代的C 1 -C 6烷氧基; 苯基-C 1 -C 6烷基; 苯基-C 1 -C 6烷氧基; 和-N(RaRb),其中每个R a和R b独立地是氢或C 1 -C 6烷基或R a和R b与它们所连接的氮原子一起 形成饱和杂环; 并且每个R 5,R 6,R 7,R 8和R 8独立地选自氢,卤素,羟基 ; 任选被羟基取代的C 1 -C 6烷基; 烷硫基C 1 -C 6烷基; 任选被卤素取代的C 1 -C 6烷氧基; C 1 -C 6烷基 - 羰基,C 1 -C 6烷氧基 - 羰基和恶唑-2(C 1 -C 6) - 基; 包括在催化剂存在下,如果需要在有机溶剂中将式(Ⅳ)化合物转化为所述式(Ⅳ)化合物。

    PROCESS FOR THE PREPARATION OF ENTACAPONE
    5.
    发明申请
    PROCESS FOR THE PREPARATION OF ENTACAPONE 失效
    制备ENTACAPONE的方法

    公开(公告)号:US20080146829A1

    公开(公告)日:2008-06-19

    申请号:US11958778

    申请日:2007-12-18

    IPC分类号: C07C255/23

    CPC分类号: C07C253/30 C07C255/41

    摘要: A process for the preparation of entacapone, in particular as the polymorphic form A, comprising the preparation of a compound of formula (V), as herein defined, by condensation of N,N-diethyl-cyano-acetamide with a compound of formula (IV), as herein defined, in the presence of a strong basic agent; the dealkylation of said compound of formula (V) to obtain entacapone and the crystallization thereof to the polymorphic form A.

    摘要翻译: 恩替卡朋的制备方法,特别是多晶型A,其包括通过N,N-二乙基 - 氰基 - 乙酰胺与式(III)化合物的缩合制备如本文定义的式(Ⅴ)化合物 IV),如本文所定义的,在强碱性剂的存在下; 所述式(V)化合物的脱烷基化以获得恩他卡朋,并将其结晶化为多晶型A.

    PROCESS FOR THE PREPARATION OF NITRILE COMPOUNDS
    8.
    发明申请
    PROCESS FOR THE PREPARATION OF NITRILE COMPOUNDS 审中-公开
    制备NITRILE化合物的方法

    公开(公告)号:US20080039640A1

    公开(公告)日:2008-02-14

    申请号:US11835784

    申请日:2007-08-08

    IPC分类号: C07D311/02 C07D405/04

    摘要: A process for the preparation of a compound of formula (I) or a salt thereof wherein R is an amino, nitro or —NHCOR1 group, wherein R1 is C1-C6 alkyl or phenyl optionally substituted by a —O—(CH2)n-phenyl group, wherein n is an integer of 1 to 6; comprising reacting a compound of formula (II) or a salt thereof, both as the individual isomer and as an isomeric mixture, wherein R is as defined above; with a dehydrating agent, if necessary in the presence of an organic solvent, and optionally in the presence of a basic agent; and, if desired, converting a compound of formula (I) to another compound of formula (I) or a salt thereof.

    摘要翻译: 一种制备式(I)化合物或其盐的方法,其中R是氨基,硝基或-NHCOR 1个基团,其中R 1是C < 任选被-O-(CH 2)n - 亚苯基取代的C 1 -C 6烷基或苯基, 其中n为1至6的整数; 包括使式(II)化合物或其盐作为单独的异构体和异构体混合物反应,其中R如上定义; 如果需要,在有机溶剂的存在下,任选地在碱性试剂的存在下,使用脱水剂; 如果需要,将式(I)化合物转化为另一种式(I)化合物或其盐。