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    PROCESS FOR THE PREPARATION OF IOPAMIDOL
    11.
    发明授权
    PROCESS FOR THE PREPARATION OF IOPAMIDOL 有权
    制备IOPAMIDOL的方法

    公开(公告)号：EP3066071B1

    公开(公告)日：2018-04-18

    申请号：EP14796024.9

    申请日：2014-11-04

    Applicant: Bracco Imaging S.p.A.

    Inventor： BATTISTINI, Elisa ,  BUONSANTI, Federica ,  IMPERIO, Daniela ,  LATTUADA, Luciano ,  NAPOLITANO, Roberta

    IPC: C07C231/02 ,  C07F5/02 ,  C07F5/04

    CPC classification number: C07C231/14 ,  C07C201/12 ,  C07C227/04 ,  C07C231/02 ,  C07C231/12 ,  C07F5/025 ,  C07F5/04 ,  C07F5/05 ,  Y02P20/55 ,  Y02P20/582 ,  C07C237/46

    Abstract: The present invention discloses a process for the preparation of Iopamidol of formula (II) and comprising the following steps: a) reacting the Compound (I) wherein X is OR2 or R3, and wherein R2 and R3 are a Ci-C6 linear or branched alkyl, C3-C6 cycloalkyl, C6 aryl, optionally substituted with a group selected from the group consisting of methyl, ethyl, n-propyl, i-propyl, n-butyl, sec-butyl, t-butyl and phenyl, with the acylating agent (S)-2-(acetyloxy)propanoyl chloride in a reaction medium to provide the acetyloxy derivative of Compound (I); b) hydrolyzing the intermediate from step a) with an aqueous solution at a pH comprised from 0 to 7, by adding water or a diluted alkaline solution such as sodium hydroxide or potassium hydroxide, freeing the hydroxyls from the boron-containing protective groups, obtaining the N—(S)-2-(acetyloxy)propanoyl derivative of Compound (II); c) alkaline hydrolysis to restore the (S)-2-(hydroxy)propanoyl group and to obtain Iopamidol (II) and optional recovery of the boron derivative from the solution obtained in step b). The boron-containing protective group is versatile, efficient and recyclable. A one-pot synthesis, without intermediate isolation is provided, leading to a decreasing of recovered and recycled solvents and a significant increasing in the yield, representing a significant advantage in terms of cost-effectiveness of the entire process and environmental awareness.

    CHIRAL SPIRO PHOSPHORUS-NITROGEN-SULPHUR TRIDENTATE LIGAND, AND PREPARATION METHOD AND APPLICATION THEREOF
    12.
    发明公开
    CHIRAL SPIRO PHOSPHORUS-NITROGEN-SULPHUR TRIDENTATE LIGAND, AND PREPARATION METHOD AND APPLICATION THEREOF 审中-公开
    手性螺旋磷 - 氮 - 硫 - 三齿配体及其制备方法和应用

    公开(公告)号：EP3296302A1

    公开(公告)日：2018-03-21

    申请号：EP16795647.3

    申请日：2016-01-26

    Applicant: Zhejiang Jiuzhou Pharmaceutical Co., Ltd.

    Inventor： ZHOU, Qilin ,  XIE, Jianhua ,  BAO, Denghui ,  WANG, Lixin

    IPC: C07F9/50 ,  B01J31/24 ,  C07B41/02 ,  C07C67/31 ,  C07C69/675 ,  C07C69/708 ,  C07C269/06 ,  C07C271/22 ,  C07C231/12 ,  C07C235/06 ,  C07C29/145

    CPC classification number: C07F9/5022 ,  B01J31/189 ,  B01J31/226 ,  B01J31/249 ,  B01J37/04 ,  B01J2231/643 ,  B01J2531/0241 ,  B01J2531/827 ,  C07B53/00 ,  C07C29/145 ,  C07C29/149 ,  C07C67/31 ,  C07C69/675 ,  C07C69/708 ,  C07C231/12 ,  C07C231/18 ,  C07C235/06 ,  C07C269/06 ,  C07C271/22 ,  C07F9/5054 ,  C07F9/655363 ,  C07F15/0033

    Abstract: The present invention relates to a chiral spiro phosphine-nitrogen-sulfur (P-N-S) tridentate ligand, preparation method and application thereof. The P-N-S tridentate ligand is a compound represented by Formula I or Formula II, their racemates, optical isomers, or catalytically acceptable salts thereof. The ligand has a primary structure skeleton characterized as a chiral spiro indan skeleton structure with a thio group. The chiral spiro phosphine-nitrogen-sulfur tridentate ligand can be synthesized by reacting racemic or optical active compound 7-diary/alkyl phosphine-7'-amino-1, 1'-spiro-dihydro- indene compound having a spiro-dihydro-indene skeleton as the starting material. The chiral spiro P-N-S tridentate ligand being complex with transition metal salt can be used in an asymmetric catalytic hydrogenation reaction for catalyzing carbonyl compound. In particular, in asymmetric hydrogenation reaction process, being complex with iridium for catalyzing β-alkyl-β-keto ester can obtain a high catalytic activity (a catalyst amount of 0.0002% mol) and high enantioselectivity (up to 99.9% ee) result. So the present invention has a practical value for industrial and commercial production.

    Abstract translation: 手性螺环膦 - 氮 - 硫（P-N-S）三齿配体及其制备方法和应用技术领域本发明涉及手性螺环膦 - 氮 - 硫（P-N-S）三齿配体及其制备方法和应用。 P-N-S三齿配体是由式I或式II表示的化合物，其外消旋体，旋光异构体或其催化可接受的盐。 该配体具有一级结构骨架，其特征在于具有硫基的手性螺茚骨架结构。 手性螺环膦 - 氮 - 硫 - 三齿配体可通过使具有螺 - 二氢 - 茚的外消旋或光学活性化合物7-二芳基/烷基膦-7'-氨基-1,1'-螺 - 二氢茚化合物 骨架作为起始材料。 与过渡金属盐络合的手性螺环P-N-S三齿配体可用于催化羰基化合物的不对称催化氢化反应。 特别是在不对称氢化反应过程中，与铱配合催化β-烷基-β-酮酯可获得高催化活性（催化剂用量为0.0002摩尔％）和高对映选择性（高达99.9％ee）。 所以本发明对于工业和商业生产具有实际价值。

    AGOMELATINE INTERMEDIATES AND PREPARATION METHOD THEREOF
    16.
    发明授权
    AGOMELATINE INTERMEDIATES AND PREPARATION METHOD THEREOF 有权
    AGOMELATINE中间体及其制备方法

    公开(公告)号：EP2580189B1

    公开(公告)日：2017-10-25

    申请号：EP11791930.8

    申请日：2011-06-08

    Applicant: Les Laboratoires Servier

    Inventor： ZHANG, Peng ,  HUANG, Yu ,  YUAN, Zhedong ,  SHAN, Hanbin ,  YU, Xiong

    IPC: C07C231/12 ,  C07C233/18 ,  A61K31/165 ,  A61P25/20 ,  A61P25/22 ,  A61P25/24 ,  A61P25/06

    CPC classification number: C07C231/06 ,  C07C231/12 ,  C07C233/18 ,  C07C233/22 ,  C07C2602/10

    Abstract: The present invention relates to the intermediate compounds for preparation of agomelatine, as well as the preparation methods thereof The intermediate of the present invention for preparation of agomelatine is compound A as shown in the following formula. Also provided are two novel intermediate compounds. When we use these new intermediate compounds to prepare agomelatine, it is simple to manipulate, well-controlled and with high purity, without complicated operations such as rectification and column chromatography separation, and suitable for industrial production. Meanwhile, the preparation methods of the two new intermediates themselves is simple and high yield, only using the most commonly-used 7-methoxy-tetralone as original starting material and undergoing one step of reaction to obtain the intermediates, followed by one more step of converting the intermediate compounds to desired product agomelatine. Said reaction processes are greatly simplified, with the reaction yield being improved and the difficulty in purification of previous method being overcome, as compare with the previous technique for preparation of agomelatine. Typically, the yield of the present invention is over 70%.

    PROCESS FOR THE PREPARATION OF (1S,2R)-MILNACIPRAN
    17.
    发明公开
    PROCESS FOR THE PREPARATION OF (1S,2R)-MILNACIPRAN 审中-公开
    制备（1S，2R） - 米利司他的方法

    公开(公告)号：EP3230258A1

    公开(公告)日：2017-10-18

    申请号：EP15804325.7

    申请日：2015-11-03

    Applicant: Química Sintética, S.A.

    Inventor： BARRECA, Giuseppe ,  ROMANO', Bruno Gaetano

    IPC: C07C231/00 ,  C07C233/00

    CPC classification number: C07C231/12 ,  C07B2200/07 ,  C07C231/02 ,  C07C231/18 ,  C07C2601/02 ,  C07C237/24 ,  C07C235/40

    Abstract: The invention relates to a process for the preparation of Levomilnacipran or salts thereof, compounds useful in the treatment of depression, with high yield.

    Abstract translation: 本发明涉及用于治疗抑郁症的化合物左旋霉素的制备方法，其包括以下步骤：a）将对映体富集形式的醇（D）直接转化为对映体富集形式的邻苯二甲酰亚氨基衍生物（C ）通过在三烷基或三芳基膦和偶氮二羧酸二烷基酯存在下用邻苯二甲酰亚胺处理，式（I）中相对于所用醇（D）的摩尔量，邻苯二甲酰亚胺的量为1至1.3当量， 相对于使用的醇（D）的摩尔量，膦和偶氮二羧酸酯的量彼此独立地包含1至1.5当量; b）将对苯二甲酰亚氨基衍生物（C）的对映体富集形式解封，得到式（II）的左旋米那普仑。

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