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    Process for preparation of perindopril and salts thereof
    21.
    发明授权
    Process for preparation of perindopril and salts thereof 有权
    培哚普利及其盐的制备方法

    公开(公告)号：US07521566B2

    公开(公告)日：2009-04-21

    申请号：US10547243

    申请日：2003-02-28

    Applicant: Debashish Datta ,  Girij Pal Singh ,  Himanshu Madhav Godbole ,  Rajinder Singh Siyan

    Inventor： Debashish Datta ,  Girij Pal Singh ,  Himanshu Madhav Godbole ,  Rajinder Singh Siyan

    IPC: C07D209/42

    CPC classification number: C07D209/42 ,  C07C227/32 ,  C07C227/34 ,  C07C229/12

    Abstract: A process for preparation of perindopril of formula (II) and salts thereof which is simple, safe, convenient and cost-effective. The process involves reaction of compound of formula (I), wherein X is chlorine or bromine with compound of formula (VII) wherein A signifies that the six-membered ring of the bicyclic system is either saturated or unsaturated to give compound of formula (VIII), wherein A is as defined above, followed by catalytic hydrogenation of the compound of formula (VIII) thus obtained to give the perindopril of formula (II). The above process for the manufacture of perindopril would specifically avoid the use of harmful chemicals like phosgene or costly coupling agents like dicyclohexylcarbodiimide and 1-hydroxybenxotriazole usually used for such manufacture. The process would also not require any intervention of a catalyst and does not require any alkaline or acidic reaction conditions. Importantly, the process provides for manufacture of perindopril with high stereoselectively giving perindopril (II) having (S)-configuration in all the five chiral centres of the molecule, conforming to pharmacoepeial specifications. The invention also relates to a method for preparation of the compound of formula (I) and also to a method for preparation of N-[(S)-1-carbethoxybutyl]-(S)-alanine of formula (III) used in the process.

    Abstract translation: 一种制备式（II）培哚普利及其盐的方法，其简单，安全，方便和具有成本效益。 该方法包括式（I）化合物，其中X是氯或溴与式（Ⅶ）化合物反应，其中A表示双环系统的六元环是饱和或不饱和的，得到式（Ⅷ）化合物 ），其中A如上所定义，然后将由此获得的式（VIII）化合物进行催化氢化，得到式（II）的培哚普利。 上述制造培哚普利的方法将特别避免使用通常用于制造的有害化学物质如光气或昂贵的偶联剂如二环己基碳二亚胺和1-羟基苯并三唑。 该方法也不需要任何催化剂的干预，并且不需要任何碱性或酸性反应条件。 重要的是，该方法提供了高度立体选择性地给予符合药代动力学规范的在分子的所有五个手性中心具有（S） - 构型的培哚普利（II）的培哚普利的培哚普利。 本发明还涉及制备式（I）化合物的方法，还涉及制备式（III）化合物的N - [（S）-1-乙酯基丁基] - （S） - 丙氨酸的方法， 处理。

    Novel intermediates for synthesis of cephalosporins and process for preparation of such intermediates
    26.
    发明申请
    Novel intermediates for synthesis of cephalosporins and process for preparation of such intermediates 失效
    用于合成头孢菌素的新型中间体及其制备方法

    公开(公告)号：US20060135761A1

    公开(公告)日：2006-06-22

    申请号：US10540770

    申请日：2002-12-26

    Applicant: Debashish Datta ,  Muralikrishna Dantu ,  Brijkishore Mishra ,  Pollepeddi Sharma

    Inventor： Debashish Datta ,  Muralikrishna Dantu ,  Brijkishore Mishra ,  Pollepeddi Sharma

    IPC: C07D501/14

    CPC classification number: C07D501/00 ,  C07C303/24 ,  C07C305/00 ,  Y02P20/55

    Abstract: A novel 4-halo-2-oxyimino-3-oxo butyric acid-N,N-dimethyl formiminium chloride chlorosulfate of formula (I) useful in the preparation of cephalosporin antibiotics wherein X is chlorine or bromine; R is hydrogen, C1-4 alkyl group, an easily removable hydroxyl protective group, —CH2COOR5, or —C(CH3)2COOR5, wherein R5 is hydrogen or an easily hydrolysable ester group. The compound of formula (I) is prepared by reacting 4-halo-2-oxyimino-3-oxobutyric acid of formula (IV1), wherein X, R and R5 are as defined above, with N,N-dimethylformiminium chloride chlorosulphate of formula (VII) in an organic solvent at a temperature ranging from −30° C. to −15° C. The cephalosporins that may be prepared from the intermediate include cefdinir, cefditoren pivoxil, cefepime, cefetamet pivoxil, cefixime, cefmenoxime, cefodizime, cefoselis, cefotaxime, cefpirome, cefpodoxime proxetil, cefquinome, ceftazidime, cefteram pivoxil, ceftiofur, ceftizoxime, ceftriaxone and cefuzonam.

    Abstract translation: 用于制备头孢菌素抗生素的式（I）的新的4-卤代-2-氧亚氨基-3-氧代丁酸-N-，N-二甲基氯化亚硫酸盐，其中X是氯或溴; R为氢，C 1-4烷基，易脱除的羟基保护基，-CH 2 COOR 5或-C（CH 3） 其中R 5是氢或易水解的酯基。其中R 5是氢或易水解的酯基。 式（I）化合物通过使式（IV ）的4-卤代-2-氧亚氨基-3-氧代丁酸（其中X，R和R 5） 与式（VII）的N，N-二甲基甲酰亚胺氯化硫酸盐在有机溶剂中在-30℃至-15℃的温度范围内。可从中间体制备的头孢菌素包括头孢地尼 头孢匹罗，头孢匹肟，头孢他啶，头孢克肟，头孢匹肟，头孢匹肟，头孢噻肟，头孢噻肟，头孢匹罗，头孢泊肟酯，头孢喹肟，头孢他啶，头孢曲松，头孢噻呋，头孢唑肟，头孢曲松和头孢唑胺。

    Intermediates for synthesis of cephalosporins and process for preparation of such intermediates
    30.
    发明授权
    Intermediates for synthesis of cephalosporins and process for preparation of such intermediates 失效
    用于合成头孢菌素的中间体及其制备方法

    公开(公告)号：US07452990B2

    公开(公告)日：2008-11-18

    申请号：US10540770

    申请日：2002-12-26

    Applicant: Debashish Datta ,  Muralikrishna Dantu ,  Brijkishore Mishra ,  Pollepeddi Lakshmi Narayana Sharma

    Inventor： Debashish Datta ,  Muralikrishna Dantu ,  Brijkishore Mishra ,  Pollepeddi Lakshmi Narayana Sharma

    IPC: C07D501/22 ,  C07D501/24 ,  C07D501/36 ,  C07D501/46 ,  C07D501/34 ,  C07C305/14

    CPC classification number: C07D501/00 ,  C07C303/24 ,  C07C305/00 ,  Y02P20/55

    Abstract: A novel 4-halo-2-oxyimino-3-oxo butyric acid-N,N-dimethyl formiminium chloride chlorosulfate of formula (I) useful in the preparation of cephalosporin antibiotics wherein X is chlorine or bromine; R is hydrogen, C1-4 alkyl group, an easily removable hydroxyl protective group, —CH2COOR5, or —C(CH3)2COOR5, wherein R5 is hydrogen or an easily hydrolysable ester group. The compound of formula (I) is prepared by reacting 4-halo-2-oxyimino-3-oxobutyric acid of formula (IV1), wherein X, R and R5 are as defined above, with N,N-dimethylformiminium chloride chlorosulphate of formula (VII) in an organic solvent at a temperature ranging from −30° C. to −15° C. The cephalosporins that may be prepared from the intermediate include cefdinir, cefditoren pivoxil, cefepime, cefetamet pivoxil, cefixime, cefmenoxime, cefodizime, cefoselis, cefotaxime, cefpirome, cefpodoxime proxetil, cefquinome, ceftazidime, cefteram pivoxil, ceftiofur, ceftizoxime, ceftriaxone and cefuzonam.

    Abstract translation: 用于制备头孢菌素抗生素的式（I）的新的4-卤代-2-氧亚氨基-3-氧代丁酸-N-，N-二甲基氯化亚硫酸盐，其中X是氯或溴; R为氢，C 1-4烷基，易脱除的羟基保护基，-CH 2 COOR 5或-C（CH 3） 其中R 5是氢或易水解的酯基。其中R 5是氢或易水解的酯基。 式（I）化合物通过使式（IV ）的4-卤代-2-氧亚氨基-3-氧代丁酸（其中X，R和R 5） 与式（VII）的N，N-二甲基甲酰亚胺氯化硫酸盐在有机溶剂中在-30℃至-15℃的温度范围内。可从中间体制备的头孢菌素包括头孢地尼 头孢匹罗，头孢匹肟，头孢他啶，头孢克肟，头孢匹肟，头孢匹肟，头孢噻肟，头孢噻肟，头孢匹罗，头孢泊肟酯，头孢喹肟，头孢他啶，头孢曲松，头孢噻呋，头孢唑肟，头孢曲松和头孢唑胺。

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