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    IMPROVED PROCESS FOR THE PRODUCTION OF BIMATOPROST
    6.
    发明申请
    IMPROVED PROCESS FOR THE PRODUCTION OF BIMATOPROST 失效
    改进BIMATOPROST生产工艺

    公开(公告)号：US20110178340A1

    公开(公告)日：2011-07-21

    申请号：US12999112

    申请日：2009-06-10

    申请人： Dominic De Souza ,  Martin Albert ,  Hubert Sturm

    发明人： Dominic De Souza ,  Martin Albert ,  Hubert Sturm

    IPC分类号： C07C405/00

    CPC分类号： C07C231/24 ,  C07C231/12 ,  C07C235/34 ,  C07C2601/08

    摘要： The present invention relates to a process for the purification of crude bimatoprost to obtain pure bimatoprost comprising a chromatography, preferably a chromatography using an achiral stationary phase and an eluent comprising an alcohol and an apolar solvent; and crystallisation of the product obtained the chromatography to obtain pure bimatoprost.

    摘要翻译： 本发明涉及纯化比马前列素以获得纯比马前列素的方法，其包括色谱法，优选使用非手性固定相的色谱法和包含醇和非极性溶剂的洗脱液; 并将得到的产物进行结晶，得到纯比马前列素。

    Process for the production of bimatoprost
    7.
    发明授权
    Process for the production of bimatoprost 失效
    生育比马前列素的过程

    公开(公告)号：US08772544B2

    公开(公告)日：2014-07-08

    申请号：US12999112

    申请日：2009-06-10

    申请人： Dominic De Souza ,  Martin Albert ,  Hubert Sturm

    发明人： Dominic De Souza ,  Martin Albert ,  Hubert Sturm

    IPC分类号： C07C233/05

    CPC分类号： C07C231/24 ,  C07C231/12 ,  C07C235/34 ,  C07C2601/08

    摘要： The present invention relates to a process for the purification of crude bimatoprost to obtain pure bimatoprost comprising a chromatography, preferably a chromatography using an achiral stationary phase and an eluent comprising an alcohol and an apolar solvent; and crystallization of the product obtained the chromatography to obtain pure bimatoprost.

    摘要翻译： 本发明涉及纯化比马前列素以获得纯比马前列素的方法，其包括色谱法，优选使用非手性固定相的色谱法和包含醇和非极性溶剂的洗脱液; 并使产物结晶得到纯化比马前列素。

    Carbonyl Asymmetric Alkylation
    8.
    发明申请
    Carbonyl Asymmetric Alkylation 有权
    羰基不对称烷基化

    公开(公告)号：US20110009648A1

    公开(公告)日：2011-01-13

    申请号：US12223096

    申请日：2007-01-22

    申请人： Martin Albert ,  Hubert Sturm ,  Andreas Berger ,  Peter Kremminger

    发明人： Martin Albert ,  Hubert Sturm ,  Andreas Berger ,  Peter Kremminger

    IPC分类号： C07D307/87 ,  C07C253/30 ,  C07C255/59 ,  C07C213/08 ,  C07F5/02 ,  C07C29/38 ,  C07C215/20 ,  C07C31/38

    CPC分类号： C07C255/56 ,  C07C215/30 ,  C07C255/53 ,  C07D307/87

    摘要： This invention relates to processes and intermediates for the stereoselective alkylation of carbonyl groups. The invention in particular allows the stereoselective preparation of the antidepressant drug escitalopram. It has been found that boric or boronic acid derivatives are useful bridging elements for the attachment of a chiral group to a compound containing a carbonyl group to be alkylated. The said borates and boronates are thus useful in a process for the asymmetric alkylation of a carbonyl group in a compound containing a carbonyl group and an anchor group capable of reacting with a boric or boronic acid derivative. The asymmetric alkylation can be carried out by admixing the compound containing a carbonyl group to be alkylated and the anchor group capable of reacting with a boric or boronic acid derivative with a boric or boronic acid derivative, adding a chiral alcohol, and adding an organometallic compound. After the alkylation reaction, the borate and boronate can be easily removed by hydrolysis.

    摘要翻译： 本发明涉及羰基的立体选择性烷基化方法和中间体。 本发明特别允许立体选择性制备抗抑郁药物依他普仑。 已经发现硼酸或硼酸衍生物是用于将手性基团连接到含有待烷基化羰基的化合物的有用的桥连元件。 因此，所述硼酸盐和硼酸盐可用于在含有羰基和能够与硼酸或硼酸衍生物反应的锚定基团的化合物中羰基的不对称烷基化方法。 不对称烷基化可以通过将待烷基化的羰基和能够与硼酸或硼酸衍生物反应的锚定基团与硼酸或硼酸衍生物反应，加入手性醇，并加入有机金属化合物 。 在烷基化反应之后，可以通过水解容易地除去硼酸盐和硼酸盐。

    Carbonyl asymmetric alkylation
    9.
    发明授权
    Carbonyl asymmetric alkylation 有权
    羰基不对称烷基化

    公开(公告)号：US08288569B2

    公开(公告)日：2012-10-16

    申请号：US12223096

    申请日：2007-01-22

    申请人： Martin Albert ,  Hubert Sturm ,  Andreas Berger ,  Peter Kremminger

    发明人： Martin Albert ,  Hubert Sturm ,  Andreas Berger ,  Peter Kremminger

    IPC分类号： C07D307/87 ,  C07F5/02

    CPC分类号： C07C255/56 ,  C07C215/30 ,  C07C255/53 ,  C07D307/87

    摘要： This invention relates to processes and intermediates for the stereoselective alkylation of carbonyl groups. The invention in particular allows the stereoselective preparation of the antidepressant drug escitalopram. It has been found that boric or boronic acid derivatives are useful bridging elements for the attachment of a chiral group to a compound containing a carbonyl group to be alkylated. The said borates and boronates are thus useful in a process for the asymmetric alkylation of a carbonyl group in a compound containing a carbonyl group and an anchor group capable of reacting with a boric or boronic acid derivative. The asymmetric alkylation can be carried out by admixing the compound containing a carbonyl group to be alkylated and the anchor group capable of reacting with a boric or boronic acid derivative with a boric or boronic acid derivative, adding a chiral alcohol, and adding an organometallic compound. After the alkylation reaction, the borate and boronate can be easily removed by hydrolysis.

    摘要翻译： 本发明涉及羰基的立体选择性烷基化方法和中间体。 本发明特别允许立体选择性制备抗抑郁药物依他普仑。 已经发现硼酸或硼酸衍生物是用于将手性基团连接到含有待烷基化羰基的化合物的有用的桥连元件。 因此，所述硼酸盐和硼酸盐可用于在含有羰基和能够与硼酸或硼酸衍生物反应的锚定基团的化合物中羰基的不对称烷基化方法。 不对称烷基化可以通过将待烷基化的羰基和能够与硼酸或硼酸衍生物反应的锚定基团与硼酸或硼酸衍生物反应，加入手性醇，并加入有机金属化合物 。 在烷基化反应之后，可以通过水解容易地除去硼酸盐和硼酸盐。

    Process for production of intermediates for use in cefalosporin synthesis
    10.
    发明申请
    Process for production of intermediates for use in cefalosporin synthesis 有权
    生产用于头孢菌素合成的中间体的方法

    公开(公告)号：US20070191601A1

    公开(公告)日：2007-08-16

    申请号：US10583159

    申请日：2004-12-22

    申请人： Johannes Ludescher ,  Hubert Sturm ,  Katja Vorndran

    发明人： Johannes Ludescher ,  Hubert Sturm ,  Katja Vorndran

    IPC分类号： C07D501/04

    CPC分类号： C07D501/00 ,  Y02P20/55

    摘要： The invention relates to a new process for the production of intermediates for the synthesis of caephalosporin of formula (I) wherein R1, R2 and R3, independently of one another, are alkyl, alkenyl, aryl, hydroxy(C1-6)alkyl, carbamoyl-(C1-6)alkyl, amino-(C1-6)alkyl, acylamino-(C1-6)alkyl or carboxy(C1-6)alkyl, or wherein R2 and R3 together with the adjacent nitrogen atom, form an alicyclic 5- to 8-membered heterocyclic ring, and R1 signifies alkyl, alkenyl or aryl. The process according to the invention is notable in that the formation of undesired by-products, especially Δ2-analogous compounds of formula (I), is greatly reduced.

    摘要翻译： 本发明涉及用于合成式（I）的头孢菌素的中间体的新方法，其中R 1，R 2和R 3， 烷基，烷基，芳基，羟基（C 1-6 - ）烷基，氨基甲酰基 - （C 1-6 - ） - 烷基，氨基 - （C 1-6）烷基，酰氨基 - （C 1-6 - ）烷基或羧基（C 1-6 - ）烷基，或其中 R 2和R 3与相邻的氮原子一起形成脂环族5至8元杂环，R 1表示烷基 ，烯基或芳基。 根据本发明的方法是显着的，因为不期望的副产物，特别是式（I）的三羟甲基-D-类似化合物的形成大大降低。