公开(公告)号：US06355597B1

公开(公告)日：2002-03-12

申请号：US09559855

申请日：2000-04-27

申请人： James Lawrence Spivack ,  Donald Wayne Whisenhunt, Jr. ,  James Norman Cawse ,  Bruce Fletcher Johnson ,  Kirill Shalyaev

发明人： James Lawrence Spivack ,  Donald Wayne Whisenhunt, Jr. ,  James Norman Cawse ,  Bruce Fletcher Johnson ,  Kirill Shalyaev

IPC分类号： B01J2316

CPC分类号： C07C68/005 ,  C07C69/96

摘要： A catalyst system for economically producing aromatic carbonates from aromatic hydroxy compounds. In one embodiment, the present invention provides a carbonylation catalyst system that includes a catalytic amount of an inorganic co-catalyst containing bismuth. In various alternative embodiments, the carbonylation catalyst system can include an effective amount of a palladium source and an effective amount of a halide composition. Further alternative embodiments can include catalytic amounts of various inorganic co-catalyst combinations.

摘要翻译： 用于从芳族羟基化合物经济地生产芳族碳酸酯的催化剂体系。 在一个实施方案中，本发明提供了包含催化量的含有铋的无机助催化剂的羰基化催化剂体系。 在各种替代实施方案中，羰基化催化剂体系可以包括有效量的钯源和有效量的卤化物组合物。 另外的替代实施方案可以包括催化量的各种无机助催化剂组合。

公开(公告)号：US06346499B1

公开(公告)日：2002-02-12

申请号：US09686741

申请日：2000-10-11

申请人： Bruce Fletcher Johnson ,  Grigorii Lev Soloveichik ,  Eric James Pressman ,  Kirill Vladimirovich Shalyaev

发明人： Bruce Fletcher Johnson ,  Grigorii Lev Soloveichik ,  Eric James Pressman ,  Kirill Vladimirovich Shalyaev

IPC分类号： B01J3100

CPC分类号： B01J31/2234 ,  B01J31/0247 ,  B01J31/2239 ,  B01J31/26 ,  B01J2531/16 ,  B01J2531/38 ,  B01J2531/46 ,  B01J2531/824 ,  C07C68/005 ,  C07C69/96

摘要： Hydroxyaromatic compounds such as phenol are carbonylated with oxygen and carbon monoxide in the presence of a catalyst system comprising a metal from Groups 8-10 of the Periodic Table having an atomic number of at least 44, preferably palladium; an alkali metal or alkaline earth metal halide, preferably sodium bromide; at least one carboxylic acid amide such as N-methylpyrrolidone or dimethylacetamide; and a cocatalyst which is a compound of one or more metals including copper, titanium, zinc, lead, cerium and manganese.

摘要翻译： 羟基芳族化合物如苯酚在含有原子序数至少为44，优选钯的周期表第8-10族的金属的催化剂体系存在下，用氧和一氧化碳羰基化; 碱金属或碱土金属卤化物，优选溴化钠; 至少一种羧酸酰胺如N-甲基吡咯烷酮或二甲基乙酰胺; 和作为一种或多种金属的化合物的助催化剂，包括铜，钛，锌，铅，铈和锰。

公开(公告)号：US06191299B1

公开(公告)日：2001-02-20

申请号：US09224162

申请日：1998-12-31

申请人： Eric James Pressman ,  Bruce Fletcher Johnson ,  Phillip Oscar Moreno ,  Richard Anthony Battista

发明人： Eric James Pressman ,  Bruce Fletcher Johnson ,  Phillip Oscar Moreno ,  Richard Anthony Battista

IPC分类号： C07C6800

CPC分类号： C07C68/005 ,  C07C69/96

摘要： An improved method for producing an aromatic carbonate by reacting an aromatic hydroxy compound, carbon monoxide and oxygen in the presence of a catalyst system comprising at least one of palladium or a palladium compound; at least one lead compound; at least one halide source; and at least one desiccant, wherein the ratio of equivalents of lead co-catalyst relative to equivalents of palladium catalyst is optimized to increase reaction rate, as well as to allow production of aromatic carbonate in an economically feasible continuous process.

摘要翻译： 一种通过使芳族羟基化合物，一氧化碳和氧在包含钯或钯化合物中的至少一种的催化剂体系的存在下反应制备芳族碳酸酯的改进方法; 至少一种铅化合物; 至少一个卤素源; 和至少一种干燥剂，其中铅助催化剂的当量相对于钯催化剂的当量的比率被优化以提高反应速率，以及允许在经济上可行的连续方法中生产芳族碳酸酯。

公开(公告)号：US20130071332A1

公开(公告)日：2013-03-21

申请号：US13234210

申请日：2011-09-16

申请人： Jack Mathew Webster ,  Bruce Fletcher Johnson ,  Brian Duh-Lan Lee ,  Chittari Pabba ,  Michael James Rishel

发明人： Jack Mathew Webster ,  Bruce Fletcher Johnson ,  Brian Duh-Lan Lee ,  Chittari Pabba ,  Michael James Rishel

IPC分类号： A61K49/04 ,  A61P43/00 ,  A61K49/00 ,  C07C55/02 ,  C12Q1/02

CPC分类号： A61K51/0406 ,  C07B59/001

摘要： Imaging agents are described that comprise labeled substrates capable of being introduced into cells via the cystine/glutamate antiporter. The substrates may be used for imaging or detecting oxidative stress in cells by introducing the labeled agents into cells via the cystine/glutamate antiporter and subsequent detection.

公开(公告)号：US08013161B1

公开(公告)日：2011-09-06

申请号：US11952325

申请日：2007-12-07

申请人： Kande Kankanamalage Dayarathna Amarasinghe ,  Michael James Rishel ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

发明人： Kande Kankanamalage Dayarathna Amarasinghe ,  Michael James Rishel ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

IPC分类号： C07D455/06

CPC分类号： C07D455/06 ,  A61K51/0455 ,  C07D455/02

摘要： The present invention provides novel fluoroalkyl tetrabenazine carbinol compounds having structure I wherein R1 is a C1-C10 fluorinated aliphatic radical; R2 is a C1-C10 aliphatic radical; R3 is hydrogen or a C1-C10 aliphatic radical; R4 is hydrogen or a C1-C10 aliphatic radical; and R5 is hydrogen, a C1-C10 aliphatic radical, a C2-C10 cycloaliphatic radical, or a C2-C20 aromatic radical. In a particular embodiment, —OR5 is an ester moiety. The fluoroalkyl tetrabenazine carbinol compounds are provided in both racemic and enantiomerically enriched forms and may comprise either or both of fluorine-18 and fluorine 19. The fluoroalkyl tetrabenazine carbinol compounds are shown to possess high affinity for VMAT-2, a biomarker implicated in human diabetes. The fluoroalkyl tetrabenazine carbinol compounds comprising a fluorine-18 group are useful as PET imaging agents targeting the VMAT-2 biomarker. The non-radiolabled fluoroalkyl tetrabenazine carbinol compounds are useful as probes for the discovery of PET imaging agents.

摘要翻译： 本发明提供具有结构I的新型氟代烷基四苯并嗪甲醇化合物，其中R 1是C 1 -C 10氟化脂族基; R2是C1-C10脂族基团; R3是氢或C1-C10脂族基; R4是氢或C1-C10脂族基; 并且R 5是氢，C 1 -C 10脂族基，C 2 -C 10脂环族基或C 2 -C 20芳族基。 在一个具体实施方案中，-OR 5是酯部分。 氟烷基四苯并嗪甲醇化合物以外消旋和对映异构体富集的形式提供，并且可以包含氟-18和氟19中的一种或两种。氟烷基丁苯那嗪甲醇化合物显示对VMAT-2具有高亲和力，VMAT-2是涉及人类糖尿病的生物标记 。 包含氟-18基团的氟代烷基四苯并嗪甲醇化合物可用作靶向VMAT-2生物标志物的PET显像剂。 非放射性氟烷基丁苯那嗪甲醇化合物可用作发现PET成像剂的探针。

公开(公告)号：US07910738B2

公开(公告)日：2011-03-22

申请号：US11947275

申请日：2007-11-29

申请人： Michael James Rishel ,  Kande Kankanamalage Dayarathna Amarasinghe ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

发明人： Michael James Rishel ,  Kande Kankanamalage Dayarathna Amarasinghe ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

IPC分类号： C07D455/06

CPC分类号： C07D455/06 ,  C07D491/20

摘要： The present invention provides novel fluorophilic compounds having structure VII wherein Q is a carbonyl group, a protected carbonyl group, a hydroxy methine group, or a protected hydroxy methine group; R1 is a C1-C20 aliphatic, C2-C20 cycloaliphatic, or C2-C20 aromatic radical comprising at least one functional group susceptible to reaction with nucleophilic fluoride ion or an electrophilic fluorinating agent; R2 is hydrogen or a C1-C10 aliphatic radical; and R3 is hydrogen or a C1-C10 aliphatic radical. The fluorophilic compounds are provided in both racemic and enantiomerically enriched forms and are useful as intermediates in the preparation of novel PET imaging agents and probes useful in the discovery and performance assessment of PET imaging agents. The fluorophilic compounds are particularly useful in the preparation of PET imaging agents and probes having a high affinity for VMAT-2, a biomarker implicated in human diabetes and other illnesses such as Parkinson's disease.

摘要翻译： 本发明提供具有结构VII的新型氟化合物，其中Q为羰基，被保护的羰基，羟基次甲基或被保护的羟基次甲基; R1是包含至少一个与亲核氟离子或亲电氟化剂反应敏感的官能团的C 1 -C 20脂族，C 2 -C 20脂环族或C 2 -C 20芳族基团; R2是氢或C1-C10脂族基; 并且R 3是氢或C 1 -C 10脂族基。 亲氟化合物以外消旋和对映体富集的形式提供，并且可用作制备用于PET成像剂的发现和性能评估的新型PET成像剂和探针的中间体。 亲氟化合物特别可用于制备对VMAT-2具有高亲和力的PET成像剂和探针，所述VMAT-2是涉及人类糖尿病和其它疾病如帕金森病的生物标志物。

公开(公告)号：US07902364B2

公开(公告)日：2011-03-08

申请号：US11947215

申请日：2007-11-29

申请人： Michael James Rishel ,  Kande Kankanamalage Dayarathna Amarasinghe ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

发明人： Michael James Rishel ,  Kande Kankanamalage Dayarathna Amarasinghe ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

IPC分类号： C07D455/06

CPC分类号： C07D491/12 ,  A61K51/0455 ,  C07D471/04

摘要： The present invention provides novel alpha-fluoroalkyl compounds having structure I and the corresponding dihydrotetrabenazine compounds IV wherein R1 is a C1-C10 fluorinated aliphatic radical; R2 is hydrogen or a C1-C10 aliphatic radical; and R3 is hydrogen or a C1-C10 aliphatic radical. The alpha-fluoroalkyl compounds are provided in both racemic and enantiomerically enriched forms and may comprise either or both of fluorine-18 and fluorine 19. The alpha-fluoroalkyl compounds are shown to possess high affinity for VMAT-2, a biomarker implicated in human diabetes. The alpha-fluoroalkyl compounds comprising a fluorine-18 group are useful as PET imaging agents targeting the VMAT-2 biomarker. The non-radiolabled alpha-fluoroalkyl compounds are useful as probes for the discovery of PET imaging agents.

摘要翻译： 本发明提供具有结构I和相应的二氢丁苯那嗪化合物IV的新的α-氟烷基化合物，其中R 1是C 1 -C 10氟化脂族基; R2是氢或C1-C10脂族基; 并且R 3是氢或C 1 -C 10脂族基。 α-氟烷基化合物以外消旋和对映异构体富集的形式提供，并且可以包含氟-18和氟19中的任一种或两者。所述α-氟代烷基化合物显示对VMAT-2具有高亲和力，VMAT-2是涉及人类糖尿病的生物标记 。 包含氟-18基团的α-氟烷基化合物可用作靶向VMAT-2生物标志物的PET成像剂。 非放射性α-氟烷基化合物可用作发现PET成像剂的探针。

公开(公告)号：US20090142265A1

公开(公告)日：2009-06-04

申请号：US11947215

申请日：2007-11-29

申请人： Michael James Rishel ,  Kande Kankanamalage Dayarathna Amarasinghe ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

发明人： Michael James Rishel ,  Kande Kankanamalage Dayarathna Amarasinghe ,  Sean Richard Dinn ,  Bruce Fletcher Johnson

IPC分类号： A61K51/04 ,  C07D471/04

CPC分类号： C07D491/12 ,  A61K51/0455 ,  C07D471/04

摘要： The present invention provides novel alpha-fluoroalkyl compounds having structure I and the corresponding dihydrotetrabenazine compounds IV wherein R1 is a C1-C10 fluorinated aliphatic radical; R2 is hydrogen or a C1-C10 aliphatic radical; and R3 is hydrogen or a C1-C10 aliphatic radical. The alpha-fluoroalkyl compounds are provided in both racemic and enantiomerically enriched forms and may comprise either or both of fluorine-18 and fluorine 19. The alpha-fluoroalkyl compounds are shown to possess high affinity for VMAT-2, a biomarker implicated in human diabetes. The alpha-fluoroalkyl compounds comprising a fluorine-18 group are useful as PET imaging agents targeting the VMAT-2 biomarker. The non-radiolabled alpha-fluoroalkyl compounds are useful as probes for the discovery of PET imaging agents.

摘要翻译： 本发明提供具有结构I和相应的二氢丁苯那嗪化合物IV的新的α-氟烷基化合物，其中R 1是C 1 -C 10氟化脂族基; R2是氢或C1-C10脂族基; 并且R 3是氢或C 1 -C 10脂族基。 α-氟烷基化合物以外消旋和对映异构体富集的形式提供，并且可以包含氟-18和氟19中的任一种或两者。所述α-氟烷基化合物显示对VMAT-2具有高亲和力，VMAT-2是涉及人类糖尿病的生物标记 。 包含氟-18基团的α-氟烷基化合物可用作靶向VMAT-2生物标志物的PET成像剂。 非放射性α-氟烷基化合物可用作发现PET成像剂的探针。

公开(公告)号：US06700008B2

公开(公告)日：2004-03-02

申请号：US10135723

申请日：2002-04-30

申请人： Kirill Vladimirovich Shalyaev ,  Bruce Fletcher Johnson ,  Donald Wayne Whisenhunt, Jr. ,  Grigorii Lev Soloveichik

发明人： Kirill Vladimirovich Shalyaev ,  Bruce Fletcher Johnson ,  Donald Wayne Whisenhunt, Jr. ,  Grigorii Lev Soloveichik

IPC分类号： C07C6996

CPC分类号： B01J31/0239 ,  B01J21/063 ,  B01J23/14 ,  B01J23/44 ,  B01J23/72 ,  B01J31/0251 ,  B01J31/128 ,  B01J31/2234 ,  B01J31/26 ,  B01J2219/0004 ,  B01J2231/321 ,  B01J2531/16 ,  B01J2531/38 ,  B01J2531/46 ,  B01J2531/72 ,  B01J2531/824 ,  C07C51/252 ,  C07C51/44 ,  C07C51/48 ,  C07C68/005 ,  C07C69/96 ,  C07C57/04

摘要： A method and catalyst composition for economically producing aromatic carbonates from aromatic hydroxy compounds is disclosed. The present invention provides a method for carbonylating aromatic hydroxy compounds, comprising the step of contacting at least one aromatic hydroxy compound with oxygen and carbon monoxide in the presence of a halide-free carbonylation catalyst composition comprising an effective amount of at least one Group 8, 9, or 10 metal source, an effective amount of a first inorganic co-catalyst comprising at least one Group 14 metal source, an effective amount of a salt co-catalyst, and optionally an effective amount of a second inorganic co-catalyst selected from the group consisting of a Group 4 metal source, a Group 7 metal source, a Group 11 metal source, and a lanthanide element source, and optionally an effective amount of a base. A significant advantage of the present method and catalyst compositions is that no halide is present or required in the reaction mixture for catalytic activity.

摘要翻译： 公开了一种用于从芳族羟基化合物经济地生产芳族碳酸酯的方法和催化剂组合物。 本发明提供了一种芳族羟基化合物的羰基化方法，包括使至少一种芳香族羟基化合物与氧和一氧化碳在不含卤化物的羰基化催化剂组合物存在下接触的步骤，该组合物包含有效量的至少一种第8族， 9或10个金属源，有效量的第一无机助催化剂，其包含至少一种第14族金属源，有效量的盐助催化剂和任选的有效量的第二无机助催化剂，其选自 由4族金属源，7族金属源，11族金属源和镧系元素源组成的组，以及任选的有效量的碱。 本发明方法和催化剂组合物的显着优点是在反应混合物中不存在或需要用于催化活性的卤化物。

公开(公告)号：US06403821B1

公开(公告)日：2002-06-11

申请号：US09677179

申请日：2000-10-02

申请人： Eric James Pressman ,  Grigorii Lev Soloveichik ,  Bruce Fletcher Johnson ,  Kirill Vladimirovich Shalyaev

发明人： Eric James Pressman ,  Grigorii Lev Soloveichik ,  Bruce Fletcher Johnson ,  Kirill Vladimirovich Shalyaev

IPC分类号： C07C6996

CPC分类号： B01J31/2239 ,  B01J31/0235 ,  B01J31/2234 ,  B01J31/26 ,  B01J2231/321 ,  B01J2531/38 ,  B01J2531/46 ,  B01J2531/824 ,  C07C68/005 ,  C07C69/96

摘要： Hydroxyaromatic compounds such as phenol are carbonylated with oxygen and carbon monoxide in the presence of a catalyst system comprising a Group VIIIB metal, preferably palladium; an alkali metal or alkaline earth metal halide, preferably sodium bromide; and a promoter compound which is at least one C2-8 aliphatic or C7-10 aromatic mono- or dinitrile, preferably acetonitrile or adiponitrile. The catalyst system also preferably contains a compound of a non-Group VIIIB metal, preferably lead.

摘要翻译： 在含有VIIIB族金属，优选钯的催化剂体系的存在下，用氧和一氧化碳将羟基芳族化合物如苯酚羰基化; 碱金属或碱土金属卤化物，优选溴化钠; 和至少一种C 2-8脂族或C 7-10芳族单或二腈，优选乙腈或己二腈的促进剂化合物。 催化剂体系还优选含有非ⅧB族金属化合物，优选含铅。