メマンチンの製造プロセス
    3.
    发明申请
    メマンチンの製造プロセス 审中-公开
    记忆的制造过程

    公开(公告)号:WO2014115638A1

    公开(公告)日:2014-07-31

    申请号:PCT/JP2014/050716

    申请日:2014-01-16

    Inventor: 下 哲也

    CPC classification number: C07C209/62 C07C231/06 C07C211/38 C07C233/06

    Abstract:  本発明の3,5-ジメチル-1-アダマンタンアミンの製造方法は、以下の工程(i)~(iii)を含む。 (i)3,5-ジメチル-1-アダマンタノールを有機溶媒中で酸及びニトリルと反応させて反応液を得る工程。 (ii)前記工程(i)で得られた反応液に水を加えて1-アミド-3,5-ジメチルアダマンタンを得る工程。 (iii)前記工程(ii)で得られた1-アミド-3,5-ジメチルアダマンタンをアルコール含有溶媒及び無機塩基の存在下で加水分解する工程。

    Abstract translation: 这种制造3,5-二甲基-1-金刚烷胺的方法包括以下步骤(i)至(iii)。 (i)使3,5-二甲基-1-金刚烷与氧和腈在有机溶剂中反应得到反应溶液的步骤。 (ii)向步骤(i)中得到的反应溶液中加入水以获得1-酰胺基-3,5-二甲基金刚烷的步骤。 (iii)在含醇溶剂和无机碱的存在下水解步骤(ii)中得到的1-酰氨基-3,5-二甲基金刚烷的步骤。

    METHOD OF PREPARING 1-CHLOROACETAMIDO-1,3,3,5,5-PENTAMETHYLCYCLOHEXANE
    5.
    发明申请
    METHOD OF PREPARING 1-CHLOROACETAMIDO-1,3,3,5,5-PENTAMETHYLCYCLOHEXANE 审中-公开
    1-氯代氨基甲酰基-1,3,3,5,5-三甲氧基环己烷的制备方法

    公开(公告)号:WO2011000537A1

    公开(公告)日:2011-01-06

    申请号:PCT/EP2010/003920

    申请日:2010-06-28

    Abstract: Method of preparing 1-chloroacetamido-1,3,3,5,5-pentamethylcyclohexane, an intermediate in the synthesis of 1-amino-1,3,3,5,5-pentamethylcyclohexane (Neramexane) or a pharmaceutically acceptable salt thereof, comprising step (iii): (iii) reacting 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane with chloroacetonitrile in the presence of an acid, wherein 1-hydroxy-1,3,3,5,5-pentamethylcyclohexane is employed in step (iii) as obtained in the reaction of a methylmagnesium halide with 3,3,5,5-tetramethylcyclohexanone without having been subjected to a purification step.

    Abstract translation: 1-氯乙酰氨基-1,3,3,5,5-五甲基环己烷的制备方法,1-氨基-1,3,3,5,5-五甲基环己烷(Neramexane)或其药学上可接受的盐的合成中间体, 包括步骤(iii):(iii)在酸存在下使1-羟基-1,3,3,5,5-五甲基环己烷与氯乙腈反应,其中1-羟基-1,3,3,5,5-五甲基环己烷 在甲基卤化镁与3,3,5,5-四甲基环己酮的反应中得到的步骤(iii)中,不经过纯化步骤。

    NEW PROCESS FOR THE SYNTHESIS OF ENEAMIDE DERIVATIVES
    8.
    发明申请
    NEW PROCESS FOR THE SYNTHESIS OF ENEAMIDE DERIVATIVES 审中-公开
    用于合成活性衍生物的新工艺

    公开(公告)号:WO2005063687A3

    公开(公告)日:2005-10-27

    申请号:PCT/IB2004004363

    申请日:2004-12-22

    CPC classification number: C07C231/10 C07C233/06 C07C2602/08 C07C2602/10

    Abstract: A process for the production of ene-amide derivatives represented by the formula (I) wherein R1 and R2 and R3 are independently a hydrogen atom, an alkyl, a cycloalkyl, a cycloalkylalkyl, an alkylaryl, an aryl, a heterocycle, a cyano, an alkoxy, an aryloxy, a carboxyl, a carbamoyl, -CONR5R6 (in which R5 and R6 are independently an alkyl, arylalkyl or aryl group said ring being substituted or not with a functional group or with R5) or -COOR5 group (in which R5 is an alkyl, alkylaryl or aryl group), said alkyl, cycloalkyl, cycloalkylalkyl, alkylaryl and aryl groups being substituted or not with a functional group or with R5; or R1 and R2 taken together, may form a ring (which terms includes mono-, di- and higher polycyclic ring systems); R4 is a hydrogen atom, an alkyl, an aryl, an alkylaryl, said groups are substituted or not with a halogen atom as Cl, Br, or F; X is an oxygen atom or a leaving group and m is an integer 1 or 2; when m is 1 then X is a leaving group; when m is 2 then X is a oxygen atom, which comprise: a hydrogenation/isanerization reaction in presence of a heterogeneous catalyst, of an oxime derivatives of formula (II) wherein R1, R2 and R3 are as defined above with an acyl derivative of formula (III) (R4CO)mXwherein R4, m and X are as defined above

    Abstract translation: 制备由式(I)表示的烯 - 酰胺衍生物的方法,其中R 1和R 2和R 3独立地为氢原子,烷基,环烷基,环烷基烷基,烷基芳基,芳基,杂环,氰基, 烷氧基,芳氧基,羧基,氨基甲酰基-CONR 5 R 6(其中R 5和R 6独立地是烷基,芳基烷基或芳基,所述环被取代或不被官能团或与R5)或-COOR5基团(其中 R5是烷基,烷基芳基或芳基),所述烷基,环烷基,环烷基烷基,烷基芳基和芳基被官能团取代或不与R5取代; 或R 1和R 2一起形成环(该术语包括单环,二和更高多环系统); R4是氢原子,烷基,芳基,烷基芳基,所述基团被卤素原子取代或未被取代为Cl,Br或F; X是氧原子或离去基团,m是整数1或2; 当m为1时,X为离去基团; 当m为2时,X为氧原子,其包括:在非均相催化剂存在下的式(II)的肟衍生物,其中R 1,R 2和R 3的定义如上所定义的肟衍生物与酰基衍生物 式(III)(R4CO)mX其中R4,m和X如上所定义

    ORGANIC COMPOUNDS
    9.
    发明申请
    ORGANIC COMPOUNDS 审中-公开
    有机化合物

    公开(公告)号:WO2003076387A2

    公开(公告)日:2003-09-18

    申请号:PCT/EP2003/002366

    申请日:2003-03-07

    Abstract: A process for preparing 5,6-diethyl-2,3-dihydro-1H-inden-2-amine and acid addition salts thereof from 2-aminoindan. The process comprises protecting the amino group of 2-aminoindan, acetylating the ring in the protected compound, reducing the acetyl group to ethyl to form a monoethyl derivative, acetylating the monoethyl derivative, reducing the acetyl group to form a diethyl derivative, deprotecting the latter by hydrolysis and recovering the product in free or salt form.

    Abstract translation: 从2-氨基茚满制备5,6-二乙基-2,3-二氢-1H-茚-2-胺及其酸加成盐的方法。 该方法包括保护2-氨基茚满的氨基,乙酰化保护的化合物中的环,将乙酰基还原为乙基以形成单乙基衍生物,乙酰化单乙基衍生物,还原乙酰基以形成二乙基衍生物,使后者脱保护 通过水解并以游离或盐形式回收产物。

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