专利号:US-2008319204-A1 优先权日:2007-06-25 标题 :Process for the synthesis of progesterone receptor modulators 发明人:WU YANZHONG; SUTHERLAND KAREN; CONSIDINE JOHN LEO; WILK BOGDAN KAZIMIERZ; GIGUERE PIERRE; MACEWAN MICHAEL; SHARMA ARCHANA; GONTCHAROV ALEXANDER 权利人:WYETH CORP 摘要:Processes for preparing substituted oxindole-2-ones, and specifically the following, are described, wherein R 1 -R 4 , R 6 , and n are defined herein. The processes include reacting a first alkali metal hydroxide, a tetraalkyl ammonium salt, a benzonitrile, and R 6 X or XCH 2 (CH 2 ) n X′, wherein R 6 is C 1 to C 6 alkyl, substituted C 1 to C 6 alkyl, C 3 to C 8 cycloalkyl, substituted C 3 to C 8 cycloalkyl, aryl, substituted aryl, heteroaryl, substituted heteroaryl, heterocyclic, or substituted heterocyclic, X and X′ are, independently, leaving groups, and n is 1 to 5; (ii) reacting the product of step (i) with a second alkali metal hydroxide at a temperature of at least about 60° C.; (iii) reacting the product of step (ii) with an alkali alkoxide at a temperature of at least about 140° C. to form an oxindol-2-one; (iv) brominating the oxindol-2-one; and (v) coupling the brominated oxindol-2-one with a coupling reagent.
专利号:CN-118221563-A 优先权日:2024-01-23 标题:Synthesis method of 2-aryl indole
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合成参考文献
参考文献:10.1134/s1070428009100194 摘要:Mai A, Artico M, Rotili D, Novakov IA, Orlinson BS, Navrotskii MB, Eremiichuk AS, Gordeeva EA. Stereoselective synthesis of 2-substituted 6-[1-(2,6-difluorophenyl)ethyl]-5-methylpyrimidin-4(3H)-ones. Russian Journal of Organic Chemistry. 2009 Oct;45(10):1531. doi: 10.1134/s1070428009100194. 参考文献:10.1134/s1070363217020128 摘要:Novakov IA, Yablokov AS, Navrotskii MB, Mkrtchyan AS, Vernigora AA, Babushkin AS, Kachala VV, Ruchko EA. Synthesis of 3-oxoesters and functional derivatives of pyrimidin-4(3Н)-one based on 1-(2,6-dihalophenyl)cyclopropan-1-carboxylic acids. Russian Journal of General Chemistry. 2017 Feb;87(2):224–30. doi: 10.1134/s1070363217020128.