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    Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds
    2.
    发明授权
    Copper-catalyzed formation of carbon-heteroatom and carbon-carbon bonds 有权
    铜催化形成碳 - 杂原子和碳 - 碳键

    公开(公告)号：US07323608B2

    公开(公告)日：2008-01-29

    申请号：US11090951

    申请日：2005-03-24

    申请人： Stephen L. Buchwald ,  Artis Klapars ,  Fuk Y. Kwong ,  Eric R. Streiter ,  Jacopo Zanon

    发明人： Stephen L. Buchwald ,  Artis Klapars ,  Fuk Y. Kwong ,  Eric R. Streiter ,  Jacopo Zanon

    IPC分类号： C07C17/20

    CPC分类号： C07D213/70 ,  C07B39/00 ,  C07C17/208 ,  C07C45/63 ,  C07C51/363 ,  C07C67/307 ,  C07C201/12 ,  C07C231/12 ,  C07C233/15 ,  C07C253/14 ,  C07C253/30 ,  C07C255/53 ,  C07C303/40 ,  C07C319/14 ,  C07D209/08 ,  C07D213/38 ,  C07D213/73 ,  C07D215/18 ,  C07D215/54 ,  C07D231/14 ,  C07D271/107 ,  C07D333/62 ,  C07D333/68 ,  C07C25/18 ,  C07C21/17 ,  C07C25/02 ,  C07C49/807 ,  C07C57/60 ,  C07C69/65 ,  C07C323/62 ,  C07C323/37 ,  C07C323/32 ,  C07C323/22 ,  C07C323/20 ,  C07C323/12 ,  C07C323/09 ,  C07C321/28 ,  C07C311/16 ,  C07C255/35 ,  C07C255/50 ,  C07C255/52 ,  C07C255/54 ,  C07C255/57 ,  C07C255/58 ,  C07C205/12

    摘要： One aspect of the present invention relates to copper-catalyzed carbon-heteroatom and carbon-carbon bond-forming methods. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-sulfur bond between the sulfur atom of a thiol moiety and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In other embodiments, the present invention relates to copper(II)-catalyzed methods of forming a carbon-nitrogen bond between the nitrogen atom of an amide and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In certain embodiments, the present invention relates to copper-catalyzed methods of forming a carbon-carbon bond between the carbon atom of cyanide ion and the activated carbon of an aryl, heteroaryl, or vinyl halide or sulfonate. In another embodiment, the present invention relates to a copper-catalyzed method of transforming an aryl, heteroaryl, or vinyl chloride or bromide into the corresponding aryl, heteroaryl, or vinyl iodide. Yet another embodiment of the present invention relates to a tandem method, which may be practiced in a single reaction vessel, wherein the first step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl iodide from the corresponding aryl, heteroaryl, or vinyl chloride or bromide; and the second step of the method involves the copper-catalyzed formation of an aryl, heteroaryl, or vinyl nitrile, amide or sulfide from the aryl, heteroaryl, or vinyl iodide formed in the first step.

    摘要翻译： 本发明的一个方面涉及铜催化的碳 - 杂原子和碳 - 碳键形成方法。 在某些实施方案中，本发明涉及在硫醇部分的硫原子和芳基，杂芳基或乙烯基卤化物或磺酸酯的活性炭之间形成碳 - 硫键的铜催化方法。 在其它实施方案中，本发明涉及在酰胺的氮原子和芳基，杂芳基或卤化乙烯或磺酸盐的活性炭之间形成碳 - 氮键的铜（II）催化方法。 在某些实施方案中，本发明涉及在氰化物离子的碳原子和芳基，杂芳基或乙烯基卤化物或磺酸盐的活性炭之间形成碳 - 碳键的铜催化方法。 在另一个实施方案中，本发明涉及将芳基，杂芳基或氯乙烯或溴化物转化为相应的芳基，杂芳基或碘乙烯的铜催化方法。 本发明的另一个实施方案涉及可以在单个反应容器中实施的串联方法，其中该方法的第一步涉及从相应的芳基铜催化形成芳基，杂芳基或乙烯基碘， 杂芳基或氯乙烯或溴化物; 并且该方法的第二步涉及在第一步中形成的芳基，杂芳基或乙烯基腈，酰胺或硫化物从芳基，杂芳基或乙烯基碘形成铜催化的形成。

    Protecting groups useful in the synthesis of polysaccharides, natural products, and combinatorial libraries
    3.
    发明授权
    Protecting groups useful in the synthesis of polysaccharides, natural products, and combinatorial libraries 失效

    公开(公告)号：US07102023B2

    公开(公告)日：2006-09-05

    申请号：US10774070

    申请日：2004-02-06

    申请人： Stephen L. Buchwald ,  Obadiah J. Plante ,  Peter H. Seeberger

    发明人： Stephen L. Buchwald ,  Obadiah J. Plante ,  Peter H. Seeberger

    IPC分类号： C07C309/06 ,  C07C317/04

    CPC分类号： C07H15/18 ,  C07H15/203 ,  Y02P20/55

    摘要： One aspect of the present invention relates to optionally substituted halogenated benzyl halides and the like. These compounds are useful as halogenated benzyl ether-based protecting groups for a variety of functional groups. Another aspect of the present invention relates to use of said protecting groups in an orthogonal protecting group strategy for the synthesis of complex molecules that comprise a number of suitable functional groups. Another aspect of the present invention relates to saccharides bearing various arrays of protecting groups of the present invention. Another aspect of the present invention relates to a method of synthesizing an oligosaccharide or glycoconjugate, comprising the steps of: using a saccharide bearing at least one protecting group of the present invention to glycosylate a second molecule to give a product comprising said saccharide; and removing a protecting group of the present invention from said product.

    Preparation of arylamines
    6.
    发明授权
    Preparation of arylamines 失效
    芳基胺的制备

    公开(公告)号：US5576460A

    公开(公告)日：1996-11-19

    申请号：US281449

    申请日：1994-07-27

    申请人： Stephen L. Buchwald ,  Anil Guram

    发明人： Stephen L. Buchwald ,  Anil Guram

    IPC分类号： C07C209/10 ,  C07C209/18 ,  C07C213/02 ,  C07C227/08

    CPC分类号： C07C213/02 ,  C07C209/10 ,  C07C209/18 ,  C07C227/08

    摘要： A method of preparing an arylamine compound includes reacting a metal amide comprising a metal selected from the group consisting of tin, boron, zinc, magnesium, indium and silicon, with an aromatic compound comprising an activated substituent in the presence of a transition metal catalyst to form an arylamine. The method is useful in preparing mixtures of arylamines for use in screening for pharmaceutical and biological activity and in preparing poly(anilines).

    摘要翻译： 制备芳基胺化合物的方法包括在过渡金属催化剂存在下将包含选自锡，硼，锌，镁，铟和硅的金属的金属酰胺与包含活化的取代基的芳族化合物反应， 形成芳胺。 该方法可用于制备用于筛选药物和生物活性的芳基胺混合物，以及制备聚（苯胺）。

    Abuse-deterrent pharmaceutical compositions of opiods and other drugs
    10.
    发明授权
    Abuse-deterrent pharmaceutical compositions of opiods and other drugs 有权
    阿片类药物和其他药物的滥用药物组合物

    公开(公告)号：US07399488B2

    公开(公告)日：2008-07-15

    申请号：US10614866

    申请日：2003-07-07

    申请人： Jane Hirsh ,  Alexander M. Kibanov ,  Timothy M. Swager ,  Stephen L. Buchwald ,  Whe Yong Lo ,  Alison B. Fleming ,  Roman V. Rariy

    发明人： Jane Hirsh ,  Alexander M. Kibanov ,  Timothy M. Swager ,  Stephen L. Buchwald ,  Whe Yong Lo ,  Alison B. Fleming ,  Roman V. Rariy

    IPC分类号： A61K9/14 ,  A61K9/50

    CPC分类号： A61K31/485 ,  A61K9/145 ,  A61K9/1617 ,  A61K9/1682 ,  A61K9/1694 ,  A61K9/4858 ,  A61K9/50 ,  A61K9/5052 ,  A61K9/5084 ,  A61K31/20 ,  A61K47/12

    摘要： An abuse-deterrent pharmaceutical composition has been developed to reduce the likelihood of improper administration of drugs, especially drugs such as opiods. In the preferred embodiment, a drug is modified to increase its lipophilicity. In preferred embodiments the modified drug is homogeneously dispersed within microparticles composed of a material that is either slowly soluble or not soluble in water. In some embodiments the drug containing microparticles or drug particles are coated with one or more coating layers, where at least one coating is water insoluble and preferably organic solvent insoluble, but enzymatically degradable by enzymes present in the human gastrointestinal tract. The abuse-deterrent composition retards the release of drug, even if the physical integrity of the formulation is compromised (for example, by chopping with a blade or crushing) and the resulting material is placed in water, snorted, or swallowed. However, when administered as directed, the drug is slowly released from the composition as the composition is broken down or dissolved gradually within the GI tract by a combination of enzymatic degradation, surfactant action of bile acids, and mechanical erosion.

    摘要翻译： 已经开发了一种滥用威慑药物组合物，以减少药物不当管理的可能性，特别是诸如阿片类药物。 在优选的实施方案中，修饰药物以增加其亲油性。 在优选实施方案中，改性药物均匀地分散在由缓慢溶解或不溶于水的材料组成的微粒内。 在一些实施方案中，含有微粒或药物颗粒的药物涂覆有一个或多个涂层，其中至少一个涂层是水不溶性的，优选有机溶剂不溶，但是通过存在于人胃肠道中的酶可酶促降解。 即使制剂的物理完整性受到损害（例如通过用刀片切碎或破碎）并且将所得材料置于水中，嗅到或吞咽，滥用威慑组合物也会延缓释放药物。 然而，当按照指导给药时，由于组合物通过酶降解，胆汁酸的表面活性作用和机械侵蚀的组合被分解或逐渐溶解在胃肠道内，药物从组合物中缓慢释放。