公开(公告)号：US20030018215A1

公开(公告)日：2003-01-23

申请号：US10179246

申请日：2002-06-26

Applicant: PROCOS S.P.A.

Inventor： Mirco Fornaroli ,  Francesco Velardi

IPC: C07C053/126

CPC classification number: C07C51/43 ,  C07C51/412 ,  C07C51/46 ,  C07C53/128

Abstract: A process for the preparation of sodium divalproate by reacting valproic acid and sodium methoxide in an inert solvent, azeotropically removing the formed methanol.

公开(公告)号：US20040106829A1

公开(公告)日：2004-06-03

申请号：US10703545

申请日：2003-11-10

Applicant: PROCOS S.P.A.

Inventor： Mirco Fornaroli ,  Francesco Velardi ,  Corrado Colli ,  Roberto Baima

IPC: C07C315/00

CPC classification number: C07C319/14 ,  C07C315/02 ,  C07C335/32 ,  C07C317/44 ,  C07C323/60

Abstract: The present invention relates to a process for the preparation of 2-(benzhydrylthio)acetamide (II), key intermediate for the synthesis of modafinil, by reaction of benzhydryl chloride with thiourea and chloroacetamide.

Abstract translation: 本发明涉及通过二苯甲基氯与硫脲和氯乙酰胺的反应制备2-（二苯甲硫基）乙酰胺（II）的方法，该方法是合成莫达非尼的关键中间体。

公开(公告)号：US20030009055A1

公开(公告)日：2003-01-09

申请号：US10156059

申请日：2002-05-29

Applicant: PROCOS S.P.A

Inventor： Francesco Velardi ,  Mirco Fornaroli

IPC: C07C227/22 ,  C07D209/54

CPC classification number: C07D209/54 ,  C07C227/12 ,  C07C227/22 ,  C07C2601/14

Abstract: A process for the preparation of gabapentin of formula (I) 1 which comprises: a) reduction of (1-nitromethyl-cyclohexyl)acetonitrile of formula (II) 2 to give 3-imino-2-aza-spironull4.5nulldecan-2-ol of formula (III) 3 b) transformation of compound (III), by alkali treatment, into 2-hydroxy-2-aza-spironull4.5nulldecan-3-one of formula (IV) 4 c) reduction of compound (IV) to give 2-aza-spironull4.5nulldecan-3-one of 5 d) hydrolysis of compound (V) to gabapentin.

Abstract translation: 制备式（I）的加巴喷丁的方法，其包括：a）还原式（II）的（1-硝基甲基 - 环己基）乙腈，得到3-亚氨基-2-氮杂 - 螺[4.5]癸-2-酮 式（Ⅳ）的二醇b）通过碱处理将化合物（Ⅲ）转变成式（Ⅳ）的2-羟基-2-氮杂 - 螺[4.5]癸烷-3-酮c）化合物（Ⅳ）的还原 得到d）将化合物（V）水解成加巴喷丁的2-氮杂 - 螺[4.5]癸烷-3-酮。