Process for the synthesis of phenols from arenes
    1.
    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

    IPC分类号: C07C3700

    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。

    Synthesis of aminoarylboronic esters and substituted anilines from arenes via catalytic C-H activation/borylation/amination and uses thereof
    2.
    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

    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。

    Functionalization of polyglycolides by “click” chemistry
    4.
    发明授权
    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:US08927682B2

    公开(公告)日:2015-01-06

    申请号:US12229544

    申请日:2008-08-25

    IPC分类号: C08G63/08 C08G63/82

    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)。

    Functional polyglycolide nanoparticles derived from unimolecular micelles
    5.
    发明申请
    Functional polyglycolide nanoparticles derived from unimolecular micelles 有权
    衍生自单分子胶束的功能聚乙交酯纳米颗粒

    公开(公告)号:US20090325292A1

    公开(公告)日:2009-12-31

    申请号:US12460655

    申请日:2009-07-22

    IPC分类号: C12N5/06 C08G63/08 A61K9/00

    摘要: Poly(glycolide) polymers are disclosed. The polymers generally include a glycolide-based polymer backbone that includes one or more functional groups such as alkynyl groups, hydrophilic organic triazole groups, hydrophobic organic triazole groups (also including amphiphilic organic triazole groups), di-triazole organic crosslinking groups, and triazole-substituted drug derivatives. The alkynyl groups provide reactive sites for further functionalization of the polymer, for example by reaction with azide derivatives. The polymers can further encapsulate a drug for delivery to a patient (i.e., as compared to drug derivatives that are covalently attached to the polymer). The polymers can be in the form of thermodynamically stable unimolecular micelles or crosslinked nanoparticles. The polymer compositions are completely biodegradable and hold great potential for use in biomedical applications.

    摘要翻译: 公开了聚(乙交酯)聚合物。 聚合物通常包括基于乙交酯的聚合物主链,其包括一个或多个官能团,例如炔基,亲水有机三唑基,疏水性有机三唑基团(也包括两亲性有机三唑基团),二 - 三唑有机交联基团和三唑 - 取代的药物衍生物。 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反应。 聚合物可以进一步包封用于递送给患者的药物(即,与共价连接到聚合物上的药物衍生物相比)。 聚合物可以是热力学稳定的单分子胶束或交联纳米颗粒的形式。 聚合物组合物是完全可生物降解的,并且具有用于生物医学应用的巨大潜力。