2,3-二氟溴苄,Potassium Cyanide置于18-冠醚-6 Sodium Hydroxide,Magnesium Sulfate体系中,用 乙腈,乙醚 用作溶剂,化学反应 5.5H,以to Afford 3.71 G Of Crude 2,3-Difluorobenzyl Cyanide的收率获得2,3-二氟苯乙腈 参考文献:Metabotropic Glutamate Receptor Antagonists And Their Use For Treating Central Nervous System Diseases 标题:Metabotropic Glutamate Receptor Antagonists And Their Use For Treating Central Nervous System Diseases 摘要:本发明提供了在代谢型谷氨酸受体上活性的化合物和含有这些化合物的药物组合物,这些化合物可用于治疗神经系统疾病和障碍.本发明还揭示了制备这些化合物的方法.
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.