欧盟法规
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CAS号106-37-6 对二溴苯 | CAS号861529-74-0 2,5-dibromo-ben... | CAS号7467-11-0 2,5-二溴苯磺酰胺 | CAS号832725-65-2 phenyl 5-bromo-... | CAS号832725-66-3 phenyl 5-bromo-...1,4-二溴苯置于氯磺酸体系中,化学反应生成2,5-二溴苯磺酰氯
参考文献:钯催化的芳烃碳-卤素键可用于(多)卤代二苯乙烯或肉桂酸酯衍生物的脱硫heck反应
标题:钯催化的芳烃碳-卤素键可用于(多)卤代二苯乙烯或肉桂酸酯衍生物的脱硫heck反应
摘要:摘要 研究了(多)卤代苯磺酰氯与烯烃的钯催化脱硫heck型反应.发现在溴或碘苯磺酰氯存在下,苯乙烯或丙烯酸酯和无膦的钯催化剂可提供具有完全区域和立体选择性的预期的β-芳基化的heck型产物.该反应可耐受卤代苯磺酰氯上的各种取代基.此外,在这些反应过程中未观测到c-br和c-i键的裂解,从而允许进一步转化.使用4-溴苯磺酰氯作为中心单元,连续的脱硫heck型反应,然后由钯催化的直接芳基化仅需两个步骤即可制备杂芳基二苯乙烯衍生物. 研究了(多)卤代苯磺酰氯与烯烃的钯催化脱硫heck型反应.发现在溴或碘苯磺酰氯存在下,苯乙烯或丙烯酸酯和无膦的钯催化剂可提供具有完全区域和立体选择性的预期的β-芳基化的heck型产物.该反应可耐受卤代苯磺酰氯上的各种取代基.此外,在这些反应过程中未观测到c-br和c-i键的裂解,从而允许进一步转化.使用4-溴苯磺酰氯作为中心单元,连续的脱硫heck型反应,然后由钯催
Doi:10.1055/s-0035-1560449
专利信息
专利号:WO-9838182-A9
优先权日:1997-02-28
标题:Hypolipidemic bicyclic derivatives
发明人:HANDLON ANTHONY LOUIS; HODGSON GORDON LEWIS; HYMAN CLIFTON EARL
权利人:GLAXO GROUP LTD; HANDLON ANTHONY LOUIS; HODGSON GORDON LEWIS; HYMAN CLIFTON EARL
摘要:The invention concerns compounds of formula (I) wherein: I is an integer of from 1 to 4; m is an integer of from 0 to 2; R is independently selected from hydrogen, halogen, nitro, hydroxy, phenylalkoxy, C1-4 alkoxy, C1-6 alkyl, -SO3R'', -CO2R'' and -O(CH2)pSO3R'' wherein p is an integer of from 1 to 4 and R'' is hydrogen or C1-6 alkyl, wherein said phenylalkoxy, alkoxy and alkyl groups are optionally substituted by one or more halogen atoms; R1 is phenyl or pyridyl optionally substituted by one to five groups independently selected from halogen, nitro, hydroxy, phenylalkoxy, C¿1-4? alkoxy, C1-6 alkyl, -SO3R''', -CO2R''' and -O(CH2)pSO3R''' wherein p is an integer of from 1 to 4 and R''' is hydrogen or C1-6 alkyl, wherein said phenylalkoxy, alkoxy and alkyl groups are optionally substituted by one or more halogen atoms; R?2¿ is a group independently selected from C¿1-6? alkyl (including cycloalkyl and cycloalkylalkyl), C2-6 alkenyl, and C2-6 alkynyl which groups are optionally substituted by one or more groups or atoms independently selected from halogen, oxo, C1-4 alkoxy, hydroxy, amino optionally substituted by C1-6 alkyl, thio, and C1-6 alkylthio; R?3¿ is a group independently selected from C¿1-6? alkyl (including cycloalkyl and cycloalkylalkyl), C2-6 alkenyl, and C2-6 alkynyl which groups are optionally substituted by one or more groups or atoms independently selected from halogen, oxo, C1-4 alkoxy, hydroxy, amino optionally substituted by C1-6 alkyl, thio, and C1-6 alkylthio; X is CH2 or NH; Y is CH2 or O; and Z is CH or N; provided that when X is CH2, Y is O; and pharmaceutically acceptable derivatives or solvates thereof, to processes for their synthesis, to pharmaceutical compositions containing them and to their use in medicine, particularly as hypolipidemic agents.