4-氟苯胺置于n-甲基吗啉,Potassium Phosphate,Dichloro[1,1'-Bis(Di-T-Butylphosphino)Ferrocene]Palladium(II),2-氯-4,6-二甲氧基-1,3,5-三嗪,二碳酸二叔丁酯,硫酸,1-羟基苯并三唑,1,8-二氮杂双环[5.4.0]十一碳-7-烯,盐酸-N-乙基-N'-(3-二甲氨基丙基)碳二亚胺,N,N-二异丙基乙胺体系中,用 四氢呋喃,乙醇,水,N,N-二甲基甲酰胺,乙腈,二乙二醇 用作溶剂,化学反应 41.17H,反应生成N-[3-氟-4-[[1-甲基-6-(1H-吡唑-4-基)-1H-吲唑-5-基]氧基]苯基]-1-(4-氟苯基)-1,2-二氢-6-甲基-2-氧代-3-吡啶甲酰胺 参考文献:Route Design And Development Of A Met Kinase Inhibitor: A Copper-Catalyzed Preparation Of An N1-Methylindazole 标题:Route Design And Development Of A Met Kinase Inhibitor: A Copper-Catalyzed Preparation Of An N1-Methylindazole 摘要:The Synthesis Of A Met Kinase Inhibitor In An Overall Yield Of 22% Was Achieved Over Eight Steps Starting With 3-Hydroxybenzaldehyde,An Improvement From The Initial 12-Step Process With A 5.4% Yield. Highlights Of The Process Chemistry Design And Development Are A Cu-Catalyzed Cyclization To Form An Important N1-Methylindazole Ring,A Selective Nitro Reduction In The Presence Of An Aryl Bromide,A Late-Stage Suzuki Cross-Coupling,And A Base-Promoted Boc Deprotection To Form The Desired Drug Candidate. Doi:10.1021/op400317Z
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