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    Process for the synthesis of azetidinones
    1.
    发明授权
    Process for the synthesis of azetidinones 有权
    合成氮杂环丁酮的方法

    公开(公告)号：US06207822B1

    公开(公告)日：2001-03-27

    申请号：US09455482

    申请日：1999-12-05

    申请人： Tiruvettipuram K. Thiruvengadam ,  Xiaoyong Fu ,  Chou-Hong Tann ,  Timothy L. McAllister ,  John S. Chiu ,  Cesar Colon

    发明人： Tiruvettipuram K. Thiruvengadam ,  Xiaoyong Fu ,  Chou-Hong Tann ,  Timothy L. McAllister ,  John S. Chiu ,  Cesar Colon

    IPC分类号： C07D20508

    CPC分类号： C07D263/22 ,  C07D205/08 ,  Y02P20/55

    摘要： This invention provides a process for preparing the hypocholesterolemic compound comprising: (a) reacting p-fluorobenzoylbutyric acid with pivaloyl chloride and acylating the product with a chiral auxiliary to obtain a ketone of formula IV: (b) reducing the ketone of formula IV in the presence of a chiral catalyst to an alcohol: (c) reacting the chiral alcohol of step (b), an imine and a silyl protecting agent, then condensing the protected compounds to obtain a &bgr;-(substituted-amino)amide of formula VII: (d) cyclizing the &bgr;-(substituted-amino)amide of formula VII with a silylating agent and a fluoride ion catalyst to obtain a protected lactam of the formula VIII: and removing the protecting groups. The intermediates of formulas VII and VIII are also claimed.

    摘要翻译： 本发明提供了一种制备降血胆固醇化合物的方法，其包括：（a）使对氟苯甲酰基丁酸与新戊酰氯反应，并用手性助剂酰化产物，得到式IV的酮：（b）在存在下还原式IV的酮 的手性催化剂与醇反应：（c）使步骤（b）的手性醇与亚胺和甲硅烷基保护剂反应，然后使受保护的化合物缩合得到式VII的（取代的 - 氨基）酰胺： d）用甲硅烷基化剂和氟离子催化剂使式Ⅶ的（取代 - 氨基）酰胺环化，得到受保护的式Ⅷ的内酰胺，并除去保护基。式Ⅶ和Ⅷ的中间体也被称为 。

    Process for preparing netilmicin
    3.
    发明授权
    Process for preparing netilmicin 失效
    netilmicin的制备方法

    公开(公告)号：US4831123A

    公开(公告)日：1989-05-16

    申请号：US927765

    申请日：1986-11-06

    申请人： Chou-Hong Tann ,  Tiruvettipuram K. Thiruvengadam ,  John S. Chiu ,  Cesar Colon

    发明人： Chou-Hong Tann ,  Tiruvettipuram K. Thiruvengadam ,  John S. Chiu ,  Cesar Colon

    IPC分类号： C07H15/236

    CPC分类号： C07H15/236

    摘要： A high yielding process for converting 3,2',6'-tri-N-acetyl sisomicin to netilmicin comprising the step of silylating the starting material at the 5,2' positions, and optionally at the 4' position, converting the 1-amino substituent to a 1-N-imino substituent, converting the imino to an ethylamino, deprotecting the compound and recovering netilmicin. Also disclosed are novel intermediate compounds.

    摘要翻译： 将3,2'，6'-三-N-乙酰西索米星转化为净丝氨酸的高产率方法包括在5,2'位置和任选在4'位置使起始物质甲硅烷基化的步骤， 氨基取代基转化为1-N-亚氨基取代基，将亚氨基转化为乙基氨基，使化合物脱保护并回收西他咪啶。 还公开了新型中间体化合物。

    Process for the synthesis of azetidinones
    5.
    发明授权
    Process for the synthesis of azetidinones 有权
    合成氮杂环丁酮的方法

    公开(公告)号：US08383810B2

    公开(公告)日：2013-02-26

    申请号：US13323366

    申请日：2011-12-12

    申请人： Tiruvettipuram K. Thiruvengadam ,  John S. Chiu ,  Xiaoyong Fu ,  Timothy L. McAllister

    发明人： Tiruvettipuram K. Thiruvengadam ,  John S. Chiu ,  Xiaoyong Fu ,  Timothy L. McAllister

    IPC分类号： C07D205/08 ,  C07H7/02

    CPC分类号： C07D205/08 ,  C07H17/02

    摘要： A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.

    摘要翻译： 提供了一种制备氮杂环丁酮的方法，所述氮杂环丁酮可用作半乳聚糖和低胆固醇血症药物的合成中的中间体，包括使（b） - （取代的 - 氨基）酰胺，和（取代的 - 氨基）酸酯， （取代 - 氨基）硫代碳酸酯与甲硅烷基化剂和选自碱金属羧酸盐，季铵羧酸盐，季铵氢氧化物，季铵醇盐，季铵氧化物及其水合物的环化剂或其反应产物 ：（i）至少一种季铵卤化物和至少一种碱金属羧酸盐; 或（ii）至少一种季铵氯化物，季铵溴化物或季铵碘化物和至少一种碱金属氟化物，其中环化剂的季铵部分是未取代的或被一至四个独立地选自 由烷基，芳烷基和芳基烷基 - 烷基组成。

    PROCESS FOR THE SYNTHESIS OF AZETIDINONES
    6.
    发明申请
    PROCESS FOR THE SYNTHESIS OF AZETIDINONES 审中-公开
    合成AZETIDINONES的方法

    公开(公告)号：US20110144327A1

    公开(公告)日：2011-06-16

    申请号：US13008458

    申请日：2011-01-18

    申请人： Tiruvettipuram K. Thiruvengadam ,  John S. Chiu ,  Xiaoyong Fu ,  Timothy L. McAllister

    发明人： Tiruvettipuram K. Thiruvengadam ,  John S. Chiu ,  Xiaoyong Fu ,  Timothy L. McAllister

    IPC分类号： C07D205/08

    CPC分类号： C07D205/08 ,  C07H17/02

    摘要： A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.

    摘要翻译： 提供了一种制备氮杂环丁酮的方法，所述氮杂环丁酮可用作半乳聚糖和低胆固醇血症药物的合成中的中间体，包括使（b） - （取代的 - 氨基）酰胺，和（取代的 - 氨基）酸酯， （取代 - 氨基）硫代碳酸酯与甲硅烷基化剂和选自碱金属羧酸盐，季铵羧酸盐，季铵氢氧化物，季铵醇盐，季铵氧化物及其水合物的环化剂或其反应产物 ：（i）至少一种季铵卤化物和至少一种碱金属羧酸盐; 或（ii）至少一种季铵氯化物，季铵溴化物或季铵碘化物和至少一种碱金属氟化物，其中环化剂的季铵部分是未取代的或被一至四个独立地选自 由烷基，芳烷基和芳基烷基 - 烷基组成。

    PROCESS FOR THE SYNTHESIS OF AZETIDINONES
    7.
    发明申请
    PROCESS FOR THE SYNTHESIS OF AZETIDINONES 有权
    合成AZETIDINONES的方法

    公开(公告)号：US20120083601A1

    公开(公告)日：2012-04-05

    申请号：US13323366

    申请日：2011-12-12

    申请人： TIRUVETTIPURAM K. THIRUVENGADAM ,  John S. Chiu ,  Xiaoyong Fu ,  Timothy L. McAllister

    发明人： TIRUVETTIPURAM K. THIRUVENGADAM ,  John S. Chiu ,  Xiaoyong Fu ,  Timothy L. McAllister

    IPC分类号： C07D205/08

    CPC分类号： C07D205/08 ,  C07H17/02

    摘要： A process is provided for preparing azetidinones useful as intermediates in the synthesis of penems and as hypocholesterolemic agents, comprising reacting a β-(substituted-amino)amide, a β-(substituted-amino)acid ester, or a β-(substituted-amino)thiolcarbonic acid ester with a silylating agent and a cyclizing agent selected from the group consisting of alkali metal carboxylates, quaternary ammonium carboxylates, quaternary ammonium hydroxides, quaternary ammonium alkoxides, quaternary ammonium aryloxides and hydrates thereof, or the reaction product of: (i) at least one quaternary ammonium halide and at least one alkali metal carboxylate; or (ii) at least one quaternary ammonium chloride, quaternary ammonium bromide, or quaternary ammonium iodide and at least one alkali metal fluoride, wherein a quaternary ammonium moiety of the cyclizing agent is unsubstituted or substituted by one to four groups independently selected from the group consisting of alkyl, arylalkyl and arylalkyl-alkyl.

    摘要翻译： 提供了一种制备氮杂环丁酮的方法，所述氮杂环丁酮可用作半乳聚糖和低胆固醇血症药物的合成中的中间体，包括使（b） - （取代的 - 氨基）酰胺，和（取代的 - 氨基）酸酯， （取代 - 氨基）硫代碳酸酯与甲硅烷基化剂和选自碱金属羧酸盐，季铵羧酸盐，季铵氢氧化物，季铵醇盐，季铵氧化物及其水合物的环化剂或其反应产物 ：（i）至少一种季铵卤化物和至少一种碱金属羧酸盐; 或（ii）至少一种季铵氯化物，季铵溴化物或季铵碘化物和至少一种碱金属氟化物，其中环化剂的季铵部分是未取代的或被一至四个独立地选自 由烷基，芳烷基和芳基烷基 - 烷基组成。

    Synthesis of 3-(5-nitrocyclohex-1-enyl) acrylic acid and esters thereof
    10.
    发明授权
    Synthesis of 3-(5-nitrocyclohex-1-enyl) acrylic acid and esters thereof 失效
    3-（5-硝基环己-1-烯基）丙烯酸及其酯的合成

    公开(公告)号：US07678948B2

    公开(公告)日：2010-03-16

    申请号：US12274075

    申请日：2008-11-19

    申请人： Tiruvettipuram K. Thiruvengadam ,  Tao Wang ,  John S. Chiu ,  Jing Liao

    发明人： Tiruvettipuram K. Thiruvengadam ,  Tao Wang ,  John S. Chiu ,  Jing Liao

    IPC分类号： C07C205/01

    CPC分类号： C07C251/44 ,  C07C201/06 ,  C07C249/08 ,  C07C2601/16 ,  C07C205/56 ,  C07C251/42

    摘要： This application discloses provides a process for the introduction of nitro-group functionality into a compound which contains also a site of unsaturation and/or oxygen functionality by direct (one step) oxidation of an oxime functional group mediated by a molybdenum VI/VII peroxo complex, the process comprising: (a) providing a substrate of Formula I containing an oxime functional group; wherein R1 and R2 are selected independently from linear, branched or cyclic alkyl and linear, branched or cyclic alkenyl groups, optionally substituted, with the proviso that at least one of R1 or R2 contains a carbon/carbon double bond; and (b) contacting said substrate of Formula I with a molybdenum oxidation complex, thereby oxidizing said oxime functional group to a nitro functional group to yield the structure of Formula III. Where R1 and R2 are as defined above.

    摘要翻译： 本申请公开提供了一种通过由钼VI / VII过氧配合物介导的肟官能团的直接（一步）氧化将硝基官能团引入到还含有不饱和位和/或氧官能团位点的化合物的方法 该方法包括：（a）提供含有肟官能团的式I的底物; 其中R 1和R 2独立地选自直链，支链或环状的烷基和直链，支链或环状烯基，任选被取代，条件是R 1或R 2中的至少一个含有碳/碳双键; 和（b）使式I的底物与钼氧化络合物接触，从而将所述肟官能团氧化为硝基官能团，得到式III的结构。 其中R1和R2如上所定义。