(4E)-4-(苯基亚肼基)萘-1-酮置于铁粉,氯化铵体系中,用 乙醇,水 作为反应溶剂,化学反应 0.25H,以88%的收率获得产物4-氨基-1-萘酚盐酸盐 参考文献:A Simple Reduction Method Of Azo-Compounds To Amines Using Fe Powder In The Presence Of Nh4Cl 标题:A Simple Reduction Method Of Azo-Compounds To Amines Using Fe Powder In The Presence Of Nh4Cl 摘要:A Series Of Azo-Compounds Were Reduced To Related Aromatic Amines In The Presence Of Fe Powder And Ammonium Chloride. This One Step Protocol Led To The Formation Of Products In Middle To High Yields,Especially When Electron Releasing Substituted Aromatic Azo-Compounds Were Reduced. DOI:10.1007/s00706-007-0633-2
专利号:US-7550510-B2 优先权日:2001-07-06 标 题 :Solid phase synthesis of arylretinamides 发明人:CURLEY JR ROBERT W; MERSHON SERENA M; BARNETT DEREK W; CLAGETT-DAME MARGARET; CHAPMAN JASON S 权利人:WISCONSIN ALUMNI RES FOUND 摘要:A solid phase synthetic method for preparing arylretinamides is provided. The method comprises reacting hexachloroacetone with a solvent-suspended resin-bound triphenylphosphine to provide a suspension comprising an activated chlorinating reagent; reacting retinoic acid with the activated chlorinating reagent to provide retinoyl chloride; adding pyridine and a select arylamine to the resulting mixture; and stirring the resulting mixture for a time and at a temperature sufficient for the select arylamine to react with the retinoyl chloride and provide the arylretinamide. Also provided, are select arylretinamides that can be prepared by the present method, and methods of using such arylretinamides to induce apoptosis in cancer cells.
专利号:US-2004102650-A1 优先权日:2001-07-06 标 题:Solid phase synthesis of arylretinamides
专利号:US-6492529-B1 优先权日:2000-01-18 标题 :Bis pyrazole-1H-pyrazole intermediates and their synthesis 发明人:KAPADIA SURESH R; SONG JINHUA J; YEE NATHAN K 权利人:BOEHRINGER INGELHEIM PHARMA 摘要:Disclosed are aromatic heterocyclic compounds of the formula (I) wherein Ar 1 , Ar 2 , L, Q and X are described herein, and intermediate compounds useful for making such compounds. The compounds are useful in pharmaceutic compositions for treating diseases or pathological conditions involving inflammation such as chronic inflammatory diseases. n Also disclosed are processes of making compounds of the formula (I), their intermediates and processes of making such intermediates, including bis pyrazole-1H-pyrazole intermediates of the formula: n wherein Alk, R x and R z are described herein.
专利号:US-2003105164-A1 优先权日:2001-07-06 标 题 :Solid phase synthesis of arylretinamides
专利号:WO-03003987-A2 优先权日:2001-07-06 标题:Solid phase synthesis of arylretinamides
专利号:US-6696606-B2 优先权日:2001-07-06 标 题 :Solid phase synthesis of arylretinamides
[参考文献]: Ute F Rhrig, Et Al. Rational Design Of Indoleamine 2,3-Dioxygenase Inhibitors. J Med Chem. 2010 Feb 11;53(3):1172-89.
合成参考文献
参考文献:10.1007/978-1-4419-8718-1_72 摘要:Sabir J, Tavassoli M, Shall S. Purification and characterisation of NAD:Arginine mono ADP-Ribosyl Transferase from chicken erythrocytes; identification of some enzyme inhibitors. 1992. In: ADP-Ribosylation Reactions. : Springer New York; 1992.