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    Process for preparing a dipeptidyl peptidase IV inhibitor and intermediates employed therein
    7.
    发明授权
    Process for preparing a dipeptidyl peptidase IV inhibitor and intermediates employed therein 有权
    制备二肽基肽酶IV抑制剂的方法及其中使用的中间体

    公开(公告)号：US07420063B2

    公开(公告)日：2008-09-02

    申请号：US11668641

    申请日：2007-01-30

    申请人： Padam N. Sharma ,  Edward J. Gublo ,  Gabriel M. Galvin ,  Susan D. Boettger ,  Saibaba Racha

    发明人： Padam N. Sharma ,  Edward J. Gublo ,  Gabriel M. Galvin ,  Susan D. Boettger ,  Saibaba Racha

    IPC分类号： C07C69/013 ,  C07D209/52

    CPC分类号： C07C233/47 ,  C07C2603/74 ,  C07D209/02

    摘要： A process is provided for preparing a dipeptidyl peptidase IV inhibitor of the structure is treated with TFAA in isopropyl acetate to protect the tertiary hydroxyl group as a trifluoroacetate group to form 4 (which is a novel intermediate) which is converted to acid chloride compound 5 (which is a novel compound) using Vilsmeier reagent or other chloro reaget and coupled with compound 6 in a heterogeneous mixture of ethyl acetate and aqueous bicabonate to give compound 7 The N,O-bis(trifluoroacetyl) groups of compound 7 are deprotected to give free base compound 10.

    摘要翻译： 提供了一种制备二肽基肽酶IV抑制剂的方法，其结构在乙酸异丙酯中用TFAA处理以保护作为三氟乙酸基团的叔羟基以形成4（其是新的中间体），其转化为酰氯化合物5（ 其是一种新型化合物），使用Vilsmeier试剂或其它氯代催化剂，并与化合物6在乙酸乙酯和二硼酸氢钠水溶液的非均相混合物中偶联，得到化合物7将化合物7的N，O-双（三氟乙酰基）基团去保护， 碱化合物10。

    Alkyl and aryl-thiotrifluoroacetates and process
    8.
    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。