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    Alkyl and aryl-thiotrifluoroacetates and process
    9.
    发明授权
    Alkyl and aryl-thiotrifluoroacetates and process 有权
    烷基和芳基 - 三油酰氯酸盐和方法

    公开(公告)号：US07470810B2

    公开(公告)日：2008-12-30

    申请号：US11032734

    申请日：2005-01-11

    申请人： Padam N. Sharma ,  Edward J. Gublo ,  Susan D. Boettger ,  Saibaba Racha ,  John Usher

    发明人： Padam N. Sharma ,  Edward J. Gublo ,  Susan D. Boettger ,  Saibaba Racha ,  John Usher

    IPC分类号： C07C321/04

    CPC分类号： C07C327/22 ,  C07C231/02 ,  C07C2603/74 ,  Y02P20/55 ,  C07C233/48

    摘要： Novel C3-C19 alkyl- and aryl-thiotrifluoroacetates are provided which have the structure wherein Q is C9-C19 alkyl or aryl, and are useful protecting agents for the amino or hydroxy functional groups of amines, amino acids or primary or secondary alcohols or amino alcohols to enable formation of amide bonds in peptides or proteins which are useful as screening agents, pharmaceuticals and cosmetics. A process for preparing C3-C19 alkyl- and aryl-thiotrifluoroacetates is also provided wherein a C3-C19 alkylthiol or arylthiol is treated with trifluoroacetic anhydride (TFAA) in the presence of organic base such as pyridine, a solvent such as dichloromethane (DCM) and dimethylaminopyridine (DMAP) as a catalyst to form the desired C3-C19 alkyl- or aryl-thiotrifluoroacetate.In addition, a process for protecting a primary or secondary amino group or a primary or secondary hydroxyl group or an amino alcohol with a trifluoroacetyl protecting group is provided wherein a primary or secondary amine, amino acid, a primary or secondary alcohol or an amino alcohol is treated with a C3 to C19 alkyl- or aryl-thiotrifluoroacetate in basic aqueous solution.

    摘要翻译： 提供新的C3-C19烷基 - 和芳基 - 三油酸乙酯，其具有其中Q是C9-C19烷基或芳基的结构，并且是胺，氨基酸或伯或仲醇或氨基的氨基或羟基官能团的有用的保护剂 醇，以在肽或蛋白质中形成酰胺键，其可用作筛选剂，药物和化妆品。 还提供了制备C 3 -C 19烷基 - 和芳基 - 三硫代三氟乙酸盐的方法，其中在有机碱如吡啶，溶剂如二氯甲烷（DCM））存在下，用三氟乙酸酐（TFAA）处理C 3 -C 19烷基硫醇或芳基硫醇， 和二甲基氨基吡啶（DMAP）作为催化剂形成所需的C 3 -C 19烷基 - 或芳基 - 三硫代三氟乙酸盐。 另外，提供了用三氟乙酰基保护基保护伯或仲氨基或伯或仲羟基或氨基醇的方法，其中伯胺或仲胺，氨基酸，伯或仲醇或氨基醇 在碱性水溶液中用C3至C19烷基 - 或芳基 - 三硫代三氟乙酸盐处理。

    Process for producing a dipeptidyl peptidase IV inhibitor
    10.
    发明授权
    Process for producing a dipeptidyl peptidase IV inhibitor 有权
    二肽基肽酶IV抑制剂的制备方法

    公开(公告)号：US07214702B2

    公开(公告)日：2007-05-08

    申请号：US11135217

    申请日：2005-05-23

    申请人： Padam N. Sharma

    发明人： Padam N. Sharma

    IPC分类号： A61K31/403 ,  C07D209/04

    CPC分类号： C07D209/52

    摘要： A process is provided for preparing the dipeptidyl peptidase of the structure I (also referred to as saxaglipitin) by direct dehydration, in one pot, of the amide II by reacting amide II with phosphorus oxychloride in an organic solvent such as dichloromethane, quenching the reaction mixture with water to form the hydrochloric acid salt of I, and treating the hydrochloric acid salt with base to form the free base of I.

    摘要翻译： 提供了通过使酰胺II与磷酰氯在有机溶剂如二氯甲烷中反应而使酰胺II与一氯化磷反应直接脱水制备结构I（也称为萨克斯名称）的二肽基肽酶的方法， 与水混合以形成I的盐酸盐，并用碱处理盐酸盐以形成I的游离碱。