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    PROCESS FOR THE MONONITRATION OF ALKANEDIOLS
    6.
    发明申请
    PROCESS FOR THE MONONITRATION OF ALKANEDIOLS 失效
    阿尔卡尼溶液的制备方法

    公开(公告)号：US20080146830A1

    公开(公告)日：2008-06-19

    申请号：US12036555

    申请日：2008-02-25

    申请人： Nevio FRANCESCUTTI ,  Tiziano SCUBLA ,  Fausto GORASSINI ,  Graziano CASTALDI

    发明人： Nevio FRANCESCUTTI ,  Tiziano SCUBLA ,  Fausto GORASSINI ,  Graziano CASTALDI

    IPC分类号： C07C201/00

    CPC分类号： C01B21/46 ,  C07C201/02 ,  C07C203/04

    摘要： A process for the preparation of compounds of formula HO-A-ONO2   (I) wherein A is a C2-C6 alkylene chain by nitration of the corresponding alkanediols with “stabilised” nitric acid is herein disclosed. The process is safer to operators and allows to obtain advantageous yields on an industrial scale.

    摘要翻译： 一种制备式<β的化合物的方法在线式描述=“在线式”中=“铅”→HO-A-ONO 2（I）<α -line-formula description =“In-line Formulas”end =“tail”？>其中A是C 2 -C 6 -C 6亚烷基链，硝化相应的链烷二醇 本文公开了“稳定”硝酸。 该过程对操作员更安全，并允许在工业规模上获得有利的产量。

    Process for the preparation of adapalene
    7.
    发明授权
    Process for the preparation of adapalene 失效
    阿达帕林制备方法

    公开(公告)号：US07345189B2

    公开(公告)日：2008-03-18

    申请号：US11392909

    申请日：2006-03-30

    申请人： Graziano Castaldi ,  Pietro Allegrini ,  Gabriele Razzetti ,  Mauro Ercoli

    发明人： Graziano Castaldi ,  Pietro Allegrini ,  Gabriele Razzetti ,  Mauro Ercoli

    IPC分类号： C07C69/76

    CPC分类号： C07C51/412 ,  C07C51/02 ,  C07C67/343 ,  C07C2603/74 ,  C07C65/26 ,  C07C69/94

    摘要： A process for the preparation of a compound of formula (I), or a salt thereof wherein R is H, C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; comprising the reaction between a compound of formula (II) wherein R1 and R2 are independently hydrogen, C1-C8 alkyl, aryl, aryl-C1-C8 alkyl, or R1 and R2, taken together, form a —(CH2)m—V—(CH2)n— group, in which V is NR3 or C(R3)2 wherein R3 is hydrogen, C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; and m and n, which can be the same or different, are 1 or 2; with a compound of formula (III) in which R4 and R5 are independently C1-C8 alkyl, aryl or aryl-C1-C8 alkyl; in the presence of a Ni (II) salt, an organic ligand and a basic agent, to obtain a compound of formula (I) wherein R is C1-C8 alkyl, aryl or aryl-C1-C8 alkyl and, if desired, its conversion to a compound of formula (I) wherein R is hydrogen or to a salt thereof.

    摘要翻译： 制备式（I）化合物或其盐的方法，其中R为H，C 1 -C 8烷基，芳基或芳基-C C 1 -C 8烷基; 包括其中R 1和R 2独立地是氢，C 1 -C 8的式（II）化合物之间的反应 烷基，芳基，芳基-C 1 -C 8烷基或R 1和R 2

    Process for the preparation of tolterodine
    8.
    发明授权
    Process for the preparation of tolterodine 失效
    制备托特罗定的方法

    公开(公告)号：US07335793B2

    公开(公告)日：2008-02-26

    申请号：US11356953

    申请日：2006-02-21

    申请人： Gabriele Razzetti ,  Simone Mantegazza ,  Roberto Rossi ,  Pietro Allegrini

    发明人： Gabriele Razzetti ,  Simone Mantegazza ,  Roberto Rossi ,  Pietro Allegrini

    IPC分类号： C07C211/00 ,  C09B11/02

    CPC分类号： C07C215/54 ,  C07C69/736 ,  C07C217/18 ,  C07C233/18

    摘要： A novel process prepares tolterodine, i.e. (R)-N,N-diisopropyl-3-(2-hydroxy-5-methylphenyl)-3-phenylpropanamine, in the racemic form, as well as intermediates useful for its preparation. Tolterodine free base may be prepared by reacting diisopropyl-(3-phenyl-3-p-tolyloxy-propyl)-amine and 60% aqueous sulfuric acid for three hours under stirring at room temperature. The reaction mixture is then poured over ice/water and then alkalized with 50% NaOH.

    摘要翻译： 一种新颖的方法制备托特罗定，即外消旋形式的（R）-N，N-二异丙基-3-（2-羟基-5-甲基苯基）-3-苯基丙胺，以及可用于其制备的中间体。 通过二异丙基 - （3-苯基-3-对甲氧基 - 丙基） - 胺和60％硫酸水溶液在室温搅拌下反应3小时可以制备托特罗定游离碱。 然后将反应混合物倒入冰/水中，然后用50％NaOH碱化。

    Process for the mononitration of alkanediols
    9.
    发明授权
    Process for the mononitration of alkanediols 失效
    链烷二醇单硝化方法

    公开(公告)号：US07335789B2

    公开(公告)日：2008-02-26

    申请号：US10534868

    申请日：2003-11-06

    申请人： Nevio Francescutti ,  Tiziano Scubla ,  Fausto Gorassini ,  Graziano Castaldi

    发明人： Nevio Francescutti ,  Tiziano Scubla ,  Fausto Gorassini ,  Graziano Castaldi

    IPC分类号： C07C201/02 ,  C07C203/04

    CPC分类号： C01B21/46 ,  C07C201/02 ,  C07C203/04

    摘要： A process for the preparation of compounds of formula (I): HO-A-ONO2  (I) wherein A is a C2-C6 alkylene chain, the compounds of formula (I) being synthesized by nitration of the corresponding alkanediols with “stabilized” nitric acid is herein disclosed. The process is safer to operators and allows to obtain advantageous yields on an industrial scale.

    摘要翻译： 制备式（I）化合物的方法：<？in-line-formula description =“In-line formula”end =“lead”？HO-A-ONO 2（I ）<？in-line-formula description =“In-line Formulas”end =“tail”？>其中A是C 2 -C 6亚烷基链， 本文公开了通过用“稳定”的硝酸硝化相应的链烷二醇合成的式（I）化合物。 该过程对操作员更安全，并允许在工业规模上获得有利的产量。