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    Synthesis of aminoarylboronic esters and substituted anilines from arenes via catalytic C-H activation/borylation/amination and uses thereof
    4.
    发明授权
    Synthesis of aminoarylboronic esters and substituted anilines from arenes via catalytic C-H activation/borylation/amination and uses thereof 有权
    通过催化C-H活化/硼化/胺化合成氨基芳基硼酸酯和芳烃的取代苯胺及其用途

    公开(公告)号：US06958420B2

    公开(公告)日：2005-10-25

    申请号：US10623196

    申请日：2003-07-18

    申请人： Robert E. Maleczka, Jr. ,  Milton R. Smith, III ,  Daniel Holmes

    发明人： Robert E. Maleczka, Jr. ,  Milton R. Smith, III ,  Daniel Holmes

    IPC分类号： C07F5/02

    CPC分类号： C07F5/025

    摘要： A process is described for synthesizing aminoarylboronic esters of the general formula wherein R, R2, and R3 are each an alkyl, aryl, vinyl, alkoxy, carboxylic esters, amides, or halogen; Ar is any variety of phenyl, naphthyl, anthracyl, heteroaryl; and R1 is alkyl, hydrogen, or aryl. The aminoarylboronic esters are produced via the metal-catalyzed coupling of arylboronic esters of the general formula wherein R and R1 are any non-interfering group and X is chloro, bromo, iodo, triflates, or nonaflates to amines (primary and secondary). In particular, a process is described for the synthesis of the aminoarylboronic esters via a step-wise or tandem process in which one catalytic event is a metal-catalyzed borylation and the other catalytic event is a metal-catalyzed amination.

    摘要翻译： 描述了用于合成通式的氨基芳基硼酸酯的方法，其中R 1，R 2和R 3各自为烷基，芳基，乙烯基，烷氧基，羧酸酯，酰胺 ，或卤素; Ar是任何各种苯基，萘基，蒽基，杂芳基; 并且R 1是烷基，氢或芳基。 氨基芳基硼酸酯通过以下通式的芳基硼酸酯的金属催化偶合而制备：其中R和R 1是任何非干扰基团，X是氯，溴，碘，三氟甲磺酸酯或非卤化物， 胺（初级和次级）。 特别地，描述了通过逐步或串联方法合成氨基芳基硼酸酯的方法，其中一个催化事件是金属催化的硼化反应，另一个催化事件是金属催化的胺化。

    Process for the synthesis of phenols from arenes
    6.
    发明授权
    Process for the synthesis of phenols from arenes 有权
    从芳烃合成苯酚的方法

    公开(公告)号：US06828466B2

    公开(公告)日：2004-12-07

    申请号：US10620122

    申请日：2003-07-15

    申请人： Robert E. Maleczka, Jr. ,  Milton R. Smith, III ,  Daniel Holmes ,  Feng Shi

    发明人： Robert E. Maleczka, Jr. ,  Milton R. Smith, III ,  Daniel Holmes ,  Feng Shi

    IPC分类号： C07C3700

    CPC分类号： C07D213/68 ,  C07B41/02 ,  C07C37/50 ,  C07C41/26 ,  C07C67/31 ,  C07C213/00 ,  C07C69/88 ,  C07C69/92 ,  C07C215/76 ,  C07C39/27 ,  C07C43/23 ,  C07C39/28 ,  C07C39/245 ,  C07C39/32 ,  C07C39/07 ,  C07C39/24 ,  C07C39/30 ,  C07C69/84

    摘要： A process to synthesize substituted phenols such as those of the general formula RR′R″Ar(OH) wherein R, R′, and R″ are each independently hydrogen or any group which does not interfere in the process for synthesizing the substituted phenol including, but not limited to, halo, alkyl, alkoxy, carboxylic ester, amine, amide; and Ar is any variety of aryl or hetroaryl by means of oxidation of substituted arylboronic esters is described. In particular, a metal-catalyzed C—H activation/borylation reaction is described, which when followed by direct oxidation in a single or separate reaction vessel affords phenols without the need for any intermediate manipulations. More particularly, a process wherein Ir-catalyzed borylation of arenes using pinacolborane (HBPin) followed by oxidation of the intermediate arylboronic ester by OXONE is described.

    摘要翻译： 合成取代酚的方法，例如通式为R'R''Ar（OH）的取代酚，其中R，R'和R“各自独立地为氢或任何不干扰合成取代基的方法的基团 苯酚，包括但不限于卤素，烷基，烷氧基，羧酸酯，胺，酰胺; 并且描述了通过取代的芳基硼酸酯的氧化的任何种类的芳基或杂芳基。 特别地，描述了金属催化的C-H活化/硼烷化反应，当在单个或单独的反应容器中直接氧化时，其提供酚，而不需要任何中间操作。 更具体地说，描述了使用频哪醇硼烷（HBPin）进行Ir催化的芳烃硼烷化，然后用OXONE氧化中间体芳基硼酸酯的方法。

    Process for the preparation of polymers of dimeric cyclic esters
    7.
    发明授权
    Process for the preparation of polymers of dimeric cyclic esters 有权
    制备二聚环酯聚合物的方法

    公开(公告)号：US06469133B2

    公开(公告)日：2002-10-22

    申请号：US09736991

    申请日：2000-12-13

    申请人： Gregory L. Baker ,  Milton R. Smith, III

    发明人： Gregory L. Baker ,  Milton R. Smith, III

    IPC分类号： C08G6308

    CPC分类号： C08G63/08 ,  C08G63/823

    摘要： The present invention provides a process for the direct synthesis of high melting polymers made from dimeric cyclic esters. In particular, the present invention provides a process for synthesis of polylactic acid (PLA) from racemic materials such as racemic lactide and polymandelide from mandelide. The process further provides racemic metal organic ligand catalysts such as racemic salbinap that catalyzes the polymerization of racemic dimeric cyclic ester monomers to a polylactide stereocomplex. Polymandelide and mixed dimeric cyclic esters are also prepared in the presence of low amounts of water.

    摘要翻译： 本发明提供直接合成由二聚环酯制成的高熔点聚合物的方法。 特别地，本发明提供从外消旋材料如外消旋丙交酯和来自扁桃体的聚扁桃酸酯合成聚乳酸（PLA）的方法。 该方法进一步提供外消旋金属有机配位体催化剂，例如外消旋萨拉宾酸，其催化外消旋二聚环状酯单体聚合成聚丙交酯立体络合物。 聚山梨糖苷和混合的二聚环状酯也是在少量水存在下制备的。

    "> Functionalization of polyglycolides by
    10.
    发明申请
    Functionalization of polyglycolides by "click" chemistry 有权
    通过“点击”化学功能化聚乙交酯

    公开(公告)号：US20090054619A1

    公开(公告)日：2009-02-26

    申请号：US12229544

    申请日：2008-08-25

    申请人： Gregory L. Baker ,  Milton R. Smith, III ,  Xuwei Jiang ,  Erin B. Vogel

    发明人： Gregory L. Baker ,  Milton R. Smith, III ,  Xuwei Jiang ,  Erin B. Vogel

    IPC分类号： C08G63/08

    CPC分类号： C08G63/08 ,  C08G63/823

    摘要： Poly(glycolide) polymers are disclosed. The polymers generally include a polymerized alkynyl-substituted glycolide having a polymer backbone with one or more alkynyl groups appended thereto. The alkynyl groups provide reactive sites for further functionalization of the polymer, for example by reaction with azide derivatives (e.g., azide-substituted organic compounds). Alkynyl and azide groups react via the “click” chemistry mechanism to form functional groups covalently bonded to the polymer via a triazole link. The polymers are biodegradable and can be used to deliver drugs or other therapeutic substances (e.g., large biomolecules such as single strand RNA) at targeted locations in a patient's body and/or at controlled release rates.

    摘要翻译： 公开了聚（乙交酯）聚合物。 聚合物通常包括聚合的炔基取代的乙交酯，其具有带有一个或多个炔基的聚合物主链。 炔基提供用于聚合物进一步官能化的反应位点，例如通过与叠氮化物衍生物（例如叠氮取代的有机化合物）反应。 炔基和叠氮基通过“点击”化学机理反应以形成通过三唑连接共价键合到聚合物上的官能团。 聚合物是可生物降解的，并且可以用于在患者身体的目标位置和/或以控制释放速率递送药物或其它治疗物质（例如大的生物分子，例如单链RNA）。