专利号:US-8907083-B2 优先权日:2010-08-25 标题 :Process for the preparation, of 2-(2-hydroxyphenyl)-benz [1, 3] oxazin-4-one and its use for preparation of 4-[3, 5-bis (2-hydroxyphenyl)-IH-I, 2, 4-triazolTI-yl] benzoic acid 发明人:DAVULURI RAMAMOHAN RAO; PONNAIAH RAVI; BATTHNI GURUSWAMY; MEDIDA CHANDRA MURTHY V R; DUMMU SANTHOSH 权利人:DAVULURI RAMAMOHAN RAO; PONNAIAH RAVI; BATTHNI GURUSWAMY; MEDIDA CHANDRA MURTHY V R; DUMMU SANTHOSH; RAMAMOHAN RAO DAVULURI 摘要:The invention provides a novel process for the synthesis of 2-(2-hydroxyphenyl)-benz[1,3]oxazin-4-one, the process comprising of reacting the salicylic acid with salicylamide in the presence of p-toluenesulfonyl chloride, base and solvent. The use of 2-(2-hydroxyphenyl)-benz[1,3]oxazin-4-one in the preparation of Deferasirox is also disclosed in the invention.
参考文献:10.1371/journal.pone.0149996 摘要:Crowther GJ, Hillesland HK, Keyloun KR, Reid MC, Lafuente-Monasterio MJ, Ghidelli-Disse S, Leonard SE, He P, Jones JC, Krahn MM, Mo JS, Dasari KS, Fox AMW, Boesche M, El Bakkouri M, Rivas KL, Leroy D, Hui R, Drewes G, Maly DJ, Van Voorhis WC, Ojo KK. Biochemical Screening of Five Protein Kinases from Plasmodium falciparum against 14,000 Cell-Active Compounds. PLoS ONE. 2016 Mar 02;11(3):e0149996. doi: 10.1371/journal.pone.0149996.