Method for producing enantiomer-pure aminoalcohols
    12.
    发明申请
    Method for producing enantiomer-pure aminoalcohols 有权
    产生对映体纯氨基醇的方法

    公开(公告)号:US20070128704A1

    公开(公告)日:2007-06-07

    申请号:US10587440

    申请日:2005-01-18

    申请人: Rainer Sturmer

    发明人: Rainer Sturmer

    IPC分类号: C12P13/06 C07D333/22

    CPC分类号: C07D333/16

    摘要: The invention relates to a process for preparing enantiomerically pure alcohol of the formula 1, which comprises (i) reducing the ketone of the formula 3 to the racemic alcohol of the formula 4, (ii) enantioselectively acylating the racemic alcohol of the formula 4 with succinic anhydride in the presence of a lipase to give the succinic semiester of the formula 7, (iii) separating off the succinic semiester of the formula 7 from the unreacted enantiomer of the formula 4, (iv) reacting the enantiomerically pure alcohol of the formula 4 with methylamine to give the enantiomerically pure alcohol of the formula 1.

    摘要翻译: 本发明涉及一种制备式1的对映体纯的醇的方法,其包括(i)将式3的酮还原为式4的外消旋醇,(ⅱ)用式4的外消旋醇对 琥珀酸酐在脂肪酶的存在下得到式7的琥珀酸半酯,(iii)将式7的琥珀酸半酯与式4的未反应的对映异构体分离,(ⅳ)使式 4与甲胺反应,得到式1的对映异构体纯的醇。

    3-Methylamino-1-(2-thienyl)-1-propanone, production and use thereof
    13.
    发明申请
    3-Methylamino-1-(2-thienyl)-1-propanone, production and use thereof 有权
    3-甲基氨基-1-(2-噻吩基)-1-丙酮,的制备和应用

    公开(公告)号:US20060128791A1

    公开(公告)日:2006-06-15

    申请号:US10542003

    申请日:2004-01-15

    申请人: Rainer Sturmer

    发明人: Rainer Sturmer

    IPC分类号: A61K31/381 C07D333/22

    CPC分类号: C07D333/16

    摘要: The present invention relates to the preparation of 3-methylamino-1-(2-thienyl)-1-propanone and its use for preparing the pharmaceutical (+)-(S)-N-methyl-3-(1-naphthyloxy)-3-(2-thienyl)propylamine oxalate—(trade name Duloxetine®).

    摘要翻译: 本发明涉及3-甲基氨基-1-(2-噻吩基)-1-丙酮的制备及其制备药物(+) - (S)-N-甲基-3-(1-萘氧基)-1-丙酮的用途。 3-(2-噻吩基)丙胺草酸盐 - (商品名称)。

    Process for preparing chromanol derivatives
    18.
    发明授权
    Process for preparing chromanol derivatives 失效
    色原醇衍生物的制备方法

    公开(公告)号:US6096907A

    公开(公告)日:2000-08-01

    申请号:US395774

    申请日:1999-09-14

    CPC分类号: C07D311/72 Y02P20/55

    摘要: A process for preparing chromanol derivatives of the formula I ##STR1## where n is from 1 to 10,R.sup.1, R.sup.2,R.sup.3, R.sup.4 independently of one another are hydrogen or C.sub.1 -C.sub.4 alkyl,R.sup.5 is hydrogen, C.sub.1 -C.sub.4 alkyl, C.sub.6 -C.sub.10 aryl, C.sub.7 -C.sub.18 aralkyl, C.sub.7 -C.sub.18 alkylaryl, C.sub.1 -C.sub.22 acyl, or a group protecting the hydroxyl,by reduction of the corresponding 4-oxochromanol derivatives of the formula II ##STR2## comprises reacting the 4-oxochromanol derivatives of the formula II with metallic zinc in the presence of an acid or an acid mixture.Compounds of the formula I having C.sub.1 -C.sub.22 acyl as radical R.sup.5 can also be prepared by the above-described reduction of the compounds of the formula II with hydrogen as radical R.sup.5 and simultaneous or subsequent esterification.

    摘要翻译: 一种制备式I的色原烷醇衍生物的方法,其中n为1至10,R 1,R 2,R 3,R 4彼此独立地为氢或C 1 -C 4烷基,R 5为氢,C 1 -C 4烷基,C 6 -C 10芳基 ,C 7 -C 18芳烷基,C 7 -C 18烷基芳基,C 1 -C 22酰基或保护羟基的基团,通过还原相应的式II的4-氧杂铬醇衍生物包括使式II的4-氧杂铬醇衍生物与金属锌 在酸或酸的混合物存在下进行。 具有作为自由基R5的C 1 -C 22酰基的式I化合物也可以通过上述将式II化合物以氢作为自由基R5还原并同时或随后进行酯化来制备。

    Metal complexes with an adamantane-like structure
    19.
    发明授权
    Metal complexes with an adamantane-like structure 失效
    具有金刚烷结构的金属络合物

    公开(公告)号:US6077965A

    公开(公告)日:2000-06-20

    申请号:US284412

    申请日:1999-04-14

    CPC分类号: C07F7/28 C07F7/006 C08F10/00

    摘要: In metal complexes of the formula I ##STR1## the substituents have the following meanings: M is a metal of transition group III, IV, V or VI of the Periodic Table of the Elements or a metal of the lanthanide series,Y is a negative leaving atom or a negative leaving group,X and X.sup.1 are negatively charged or uncharged atoms of main group IV, V or VI of the Periodic Table of the Elements,Z is hydrogen, C.sub.1 -C.sub.10 -alkyl, C.sub.3 -C.sub.10 -cycloalkyl, C.sub.1 -C.sub.10 -alkoxy, C.sub.1 -C.sub.10 -alkylthio or dialkylamido having from 1 to 4 carbon atoms in each alkyl radical,R.sup.1 to R.sup.11 are hydrogen, carboorganic or organosilicon radicals,n is 0, 1 or 2 andthe valence of M is 2+n.

    摘要翻译: PCT No.PCT / EP97 / 05206 Sec。 371 1999年4月14日第 102(e)1999年4月14日PCT PCT 1997年9月23日PCT公布。 公开号WO98 / 16534 日期:1998年4月23日在式I的金属络合物中,取代基具有以下含义:M是元素周期表的III,IV,V或VI族过渡金属或镧系金属,Y是 负离子原子或负离去基团,X和X1是元素周期表的主要IV,V或VI族的带负电荷或不带电原子,Z是氢,C1-C10-烷基,C3-C10-环烷基 在每个烷基中具有1至4个碳原子的C 1 -C 10 - 烷氧基,C 1 -C 10 - 烷硫基或二烷基酰氨基,R 1至R 11为氢,有机碳或有机硅基,n为0,1或2,并且M的化合价为 2 + n。