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    Process for the preparation of rotigotine
    2.
    发明授权
    Process for the preparation of rotigotine 有权
    罗替戈汀的制备方法

    公开(公告)号：US08519160B2

    公开(公告)日：2013-08-27

    申请号：US13120682

    申请日：2009-09-24

    申请人： Aldo Banfi ,  Gialunca Belogi ,  Claudio Fuganti ,  Roberta Pizzocaro

    发明人： Aldo Banfi ,  Gialunca Belogi ,  Claudio Fuganti ,  Roberta Pizzocaro

    IPC分类号： C07D333/20

    CPC分类号： C07D333/08 ,  C07C211/38 ,  C07C213/08 ,  C07C215/64 ,  C07C2602/10 ,  C07D333/20

    摘要： A process for the preparation of Rotigotine (I) and of pharmaceutically acceptable salts thereof, which comprises the reductive amination of an amine of formula 6 with the 2-thienylacetic acid-sodium boron hydride complex and which makes use of hydrobromide 5 as an intermediate (II). The process is advantageous from the industrial point of view in that it allows to obtain Rotigotine with high enantiomeric purity starting from optically active 5,6,7,8-tetrahydro-6-(S)-N-propylamino-1-methoxynaphthalene (2), avoiding the use of dangerous reactives, the need for difficult chromatographic separation or the formation of by-products. Furthermore, two novel crystalline forms are disclosed.

    摘要翻译： 制备罗替戈汀（I）及其药学上可接受的盐的方法，其包括用2-噻吩基乙酸 - 硼氢化钠络合物还原胺化式6的胺并使用氢溴酸盐5作为中间体（ II）。 该方法从工业观点来看是有利的，因为它允许从光学活性5,6,7,8-四氢-6-（S）-N-丙基氨基-1-甲氧基萘（2）开始获得具有高对映体纯度的罗替高汀 ），避免使用危险的反应物，难以进行色谱分离或形成副产物。 此外，公开了两种新的结晶形式。

    Process for preparing .alpha.-L-aspartyl-L-phenylalanine methyl ester
    7.
    发明授权
    Process for preparing .alpha.-L-aspartyl-L-phenylalanine methyl ester 失效
    制备α-L-天冬氨酰-L-苯丙氨酸甲酯的方法

    公开(公告)号：US4613460A

    公开(公告)日：1986-09-23

    申请号：US661390

    申请日：1984-10-16

    申请人： Paolo Casati ,  Biagio Elefante ,  Claudio Fuganti

    发明人： Paolo Casati ,  Biagio Elefante ,  Claudio Fuganti

    IPC分类号： C07K1/113 ,  C07K5/075 ,  C07K5/06

    CPC分类号： C07K5/0613

    摘要： A process for preparing .alpha.-L-aspartyl-L-phenylalanine methyl ester: ##STR1## in which: (a) the compound methyl N(.alpha.-L-aspartyl).alpha.-aminocinnamate, protected at the nitrogen, of formula: ##STR2## where R is a protector group at the nitrogen, is subjected to hydrogenation at the olefin bond by means of gaseous hydrogen in the presence of a hydrogenation catalyst, to give the compound of formula: ##STR3## where R has the aforesaid meaning, in the form of a mixture of .alpha.-L-aspartyl-L-phenylalanine methyl ester protected at the nitrogen, and .alpha.-L-aspartyl-D-phenylalanine methyl ester protected at the nitrogen;(b) the protector group is removed from the .alpha.-L-aspartyl-L-phenylalanine and .alpha.-L-aspartyl-D-phenylalanine methyl esters protected at the nitrogen;(c) the .alpha.-L-aspartyl-L-phenylalanine methyl ester is separated and recovered from the deprotection reaction product.

    摘要翻译： 制备α-L-天冬氨酰基-L-苯丙氨酸甲酯的方法：其中：（a）在氮保护下的式（A）化合物甲基N（α-L-天冬氨酰基）α-氨基肉桂酸酯 ：其中R是氮的保护基，在氢化催化剂存在下，通过气态氢在烯烃键上进行氢化，得到下式的化合物：（IV） ）其中R具有上述含义，以氮保护的α-L-天冬氨酰基-L-苯丙氨酸甲酯和氮保护的α-L-天冬氨酰-D-苯丙氨酸甲酯的混合物形式; （b）保护基团从α-L-天冬氨酰基-L-苯丙氨酸和α-L-天冬氨酰-D-苯丙氨酸甲酯在氮气保护下除去; （c）从脱保护反应产物中分离并回收α-L-天冬氨酰基-L-苯丙氨酸甲酯。

    Process for the Preparation of 1-Naphthol Mixed Ethers and Intermediates of Crystalline Forms of (+) and (-)-Duloxetine
    8.
    发明申请
    Process for the Preparation of 1-Naphthol Mixed Ethers and Intermediates of Crystalline Forms of (+) and (-)-Duloxetine 失效
    （+）和（ - ） - 度洛西汀的结晶形式的1-萘酚混合醚和中间体的制备方法

    公开(公告)号：US20080287693A1

    公开(公告)日：2008-11-20

    申请号：US12090619

    申请日：2006-10-13

    申请人： Samuele Frigoli ,  Claudio Fuganti ,  Roberta Pizzocaro

    发明人： Samuele Frigoli ,  Claudio Fuganti ,  Roberta Pizzocaro

    IPC分类号： C07D333/20

    CPC分类号： C07D333/20

    摘要： The invention relates to a process for the preparation of duloxetine (1a), comprising the reaction between 1-fluoronaphthalene and 3-N,N-dimethylamino-1-(2-thienyl)-propan-1-ol in the presence of 1,3-dimethyl-2-oxo-hexahydropyrimidine (DMPU) as the solvent; a method for the identification of duloxetine enantiomers and for the determination of its optical purity is also disclosed.

    摘要翻译： 本发明涉及度洛西汀（1a）的制备方法，该方法包括1-氟萘与3-N，N-二甲基氨基-1-（2-噻吩基） - 丙-1-醇的反应， 3-二甲基-2-氧代 - 六氢嘧啶（DMPU）作为溶剂; 还公开了用于鉴别度洛西汀对映体并测定其光学纯度的方法。