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    PROCESS FOR THE PREPARATION OF OXCARBAZEPINE
    1.
    发明申请
    PROCESS FOR THE PREPARATION OF OXCARBAZEPINE 有权
    制备奥沙拉贝的方法

    公开(公告)号：US20110065917A1

    公开(公告)日：2011-03-17

    申请号：US12991600

    申请日：2009-05-06

    申请人： Nageswara Rao Karusala ,  Uma Sankara Sastry Tummalapally ,  Appi Reddy Talatala ,  Debashish Datta

    发明人： Nageswara Rao Karusala ,  Uma Sankara Sastry Tummalapally ,  Appi Reddy Talatala ,  Debashish Datta

    IPC分类号： C07D223/18

    CPC分类号： C07D223/22

    摘要： The present invention relates to an improved process for the preparation of 10-oxo-10,11-dihydiO-5H-dibenz[b,fjazepine-5-carboxamide (Oxcarbazepine) by reacting 10-methoxy-5H-dibenz[b,f]azepine (10-methoxyiminostilbene) and alkali metal cyanate in presence of α-hydroxy acids, and also relates to the process for the preparation of carbamazepine from iminostilbene. Further the present invention is directed to the novel crystalline form of 10-methoxy carbamazepine.

    摘要翻译： 本发明涉及通过使10-甲氧基-5H-二苯并[b，f]喹唑啉反应制备10-氧代-10,11-二氢-5H-二苯并[b，fjazepine-5-甲酰胺（奥卡西平） 吖庚因（10-甲氧基亚氨基芪）和碱金属氰酸盐存在的α-羟基酸，也涉及从亚氨基茋制备卡马西平的方法。 此外，本发明涉及10-甲氧基卡马西平的新结晶形式。

    Process for the preparation of oxcarbazepine
    2.
    发明授权
    Process for the preparation of oxcarbazepine 有权
    奥卡西平制备方法

    公开(公告)号：US08530647B2

    公开(公告)日：2013-09-10

    申请号：US12991600

    申请日：2009-05-06

    申请人： Nageswara Rao Karusala ,  Uma Sankara Sastry Tummalapally ,  Appi Reddy Talatala ,  Debashish Datta

    发明人： Nageswara Rao Karusala ,  Uma Sankara Sastry Tummalapally ,  Appi Reddy Talatala ,  Debashish Datta

    IPC分类号： C07D223/26

    CPC分类号： C07D223/22

    摘要： The present invention relates to an improved process for the preparation of 10-oxo-10,11-dihydro-5H-dibenz[b,f]azepine-5-carboxamide (Oxcarbazepine) by reacting 10-methoxy-5H-dibenz[b,f]azepine (10-methoxyiminostilbene) and alkali metal cyanate in presence of α-hydroxy acids, and also relates to the process for the preparation of carbamazepine from iminostilbene. Further the present invention is directed to the novel crystalline form of 10-methoxy carbamazepine.

    摘要翻译： 本发明涉及通过使10-甲氧基-5H-二苯并[b，f]咔唑反应制备10-氧代-10,11-二氢-5H-二苯并[b，f]吖庚因-5-甲酰胺（奥卡西平） f]吖庚因（10-甲氧基亚氨基芪）和碱金属氰酸酯，还涉及从亚氨基茋制备卡马西平的方法。 此外，本发明涉及10-甲氧基卡马西平的新结晶形式。

    ENZYMATIC PROCESS FOR THE PREPARATION OF (S)-5-(4-FLUORO-PHENYL)-5-HYDROXY- 1MORPHOLIN-4-YL-PENTAN-1-ONE, AN INTERMEDIATE OF EZETIMIBE AND FURTHER CONVERSION TO EZETIMIBE
    3.
    发明申请
    ENZYMATIC PROCESS FOR THE PREPARATION OF (S)-5-(4-FLUORO-PHENYL)-5-HYDROXY- 1MORPHOLIN-4-YL-PENTAN-1-ONE, AN INTERMEDIATE OF EZETIMIBE AND FURTHER CONVERSION TO EZETIMIBE 有权
    （S）-5-（4-氟 - 苯基）-5-羟基-1-吗啉-4-基 - 戊-1-酮的制备方法，EZETIMIBE的中间体和进一步转化成EZETIMIBE

    公开(公告)号：US20160280642A1

    公开(公告)日：2016-09-29

    申请号：US15179086

    申请日：2016-06-10

    申请人： Mofazzal Husain ,  Srikanth G.S.C. ,  Swapna Thorpunuri ,  Debashish Datta

    发明人： Mofazzal Husain ,  Srikanth G.S.C. ,  Swapna Thorpunuri ,  Debashish Datta

    IPC分类号： C07D205/08 ,  C12P17/10 ,  C12P17/14 ,  C07D263/26 ,  C07C229/22

    CPC分类号： C07D205/08 ,  C07C229/22 ,  C07D263/26 ,  C12N9/20 ,  C12P17/10 ,  C12P17/14 ,  Y02P20/55

    摘要： The present invention provides an enzymatic process for the preparation of (S)-5-(4-Fluoro-phenyl)-5-hydroxy-Imorpholin-4-yl-pentan-1-one by the reduction of 1-(4-Fluoro-phenyl)-5-morpholin-4-yl-pentane-1,5-dione by using a suitable enzyme or by the resolution of (R, S)-5-(4-Fluoro-phenyl)-5-hydroxy-1 morpholin-4-yl-pentan-1-one by using an enzyme. The present invention also provides process for the preparation of Ezetimibe comprising the steps of a) protecting the componnd (S)-5-(4-Fluoro-phenyl)-5-hydroxy-1 morpholin-4-yl-pentan-1-one with hydroxy protecting group b) hydrolyzing the obtained componnd c) condensing with a chiral auxiliary d) reacting with an protected imine componnd e) converting to alkyl ester f) cyclizing and g) deprotecting to obtain Ezetimibe.

    摘要翻译： 本发明提供了通过还原1-（4-氟苯基）-5-（4-氟 - 苯基）-5-羟基 - 吗啉-4-基 - 戊-1-酮制备（S） - 苯基）-5-吗啉-4-基 - 戊烷-1,5-二酮，通过使用合适的酶或通过（R，S）-5-（4-氟 - 苯基）-5-羟基-1 吗啉-4-基 - 戊-1-酮。 本发明还提供了制备依泽替米贝的方法，包括以下步骤：a）保护部分（S）-5-（4-氟 - 苯基）-5-羟基-1-吗啉-4-基 - 戊-1-酮 用羟基保护基b）水解得到的组分c）与手性助剂缩合d）与被保护的亚胺组分反应e）转化为烷基酯f）环化并g）脱保护得到依泽替米贝。

    Novel Process For The Preparation Of Leuprolide And Its Pharmaceutically Acceptable Salts Thereof
    8.
    发明申请
    Novel Process For The Preparation Of Leuprolide And Its Pharmaceutically Acceptable Salts Thereof 审中-公开
    用于制备亮丙瑞林及其药学上可接受的盐的新方法

    公开(公告)号：US20130060004A1

    公开(公告)日：2013-03-07

    申请号：US13696656

    申请日：2011-05-04

    申请人： Ananda Kuppanna ,  Bulli Raju Kamana ,  Sreelatha Vanjivaka ,  Debashish Datta

    发明人： Ananda Kuppanna ,  Bulli Raju Kamana ,  Sreelatha Vanjivaka ,  Debashish Datta

    IPC分类号： C07K1/10 ,  C07K1/14 ,  C07K7/08

    CPC分类号： C07K7/23

    摘要： The present invention relates to a novel process for the preparation of Leuprolide or its pharmaceutically acceptable salts thereof by solid and solution phase peptide synthesis (Hybrid approach). The present invention also relates to a process for the preparation of Leuprolide or its pharmaceutically acceptable salts thereof by synthesizing the peptide fragments by solid phase (7 and 5 amino acids fragment) and solution phase (2 and 4 amino acids fragment) respectively. The final solution phase condensation of these peptide fragments (7+2 and 5+4) led to a nonapeptide Leuprolide in the protected form. The present invention further relates to novel peptide fragements—Pyr-His(Trt)-Trp(Boc)-Ser(tBu)-Tyr(tBu)-DLeu-Leu-OH (Fragment-11); H-Arg(Pbf)-Pro-NHEt (Fragment-I11); Pyr-His(Trt)-Trp(Boc)-Ser(tBu)-Tyr(tBu)-DLeu-Leu-Arg(Pbf)-Pro-NHEt (Protected Leuprolide) (Fragment-IV); Pyr-His(Trt)-Trp(Boc)-Ser(tBu)-Tyr(tBu)-OH (Fragment-V); H-DLeu-Leu-Arg(Pbf)-Pro-NHEt (Fragment-VI) and process for the preparation thereof.

    摘要翻译： 本发明涉及通过固相和溶液相肽合成制备亮丙瑞林或其药学上可接受的盐的新方法（Hybrid approach）。 本发明还涉及通过分别通过固相（7和5个氨基酸片段）和溶液相（2和4个氨基酸片段）合成肽片段来制备亮丙瑞林或其药学上可接受的盐的方法。 这些肽片段（7 + 2和5 + 4）的最终溶液相缩合导致了受保护形式的一种单肽亮丙瑞林。 本发明还涉及新颖的肽片段 - Pyr-His（Trt）-Trp（Boc）-Ser（tBu）-Tyr（tBu）-DLeu-Leu-OH（片段-11）; H-Arg（Pbf）-Pro-NHEt（Fragment-I11）; Pyr-His（Trt）-Trp（Boc）-Ser（tBu）-Tyr（tBu）-DLeu-Leu-Arg（Pbf）-Pro-NHEt（受保护的亮丙瑞林）（片段-IV） Pyr-His（Trt）-Trp（Boc）-Ser（tBu）-Tyr（tBu）-OH（片段-V）; H-DLeu-Leu-Arg（Pbf）-Pro-NHEt（片段-VI）及其制备方法。