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📜尼可刹胺杂质1置于硼酸三异丙酯,Lithium Diisopropyl Amide体系中,用 四氢呋喃,水 用作溶剂,化学反应 1.83H,反应生成1-(3-羟基吡啶-2-基)乙酮
参考文献:甲硅烷基醚的锂化:邻位油炸羟基酮的形成
标题:甲硅烷基醚的锂化:邻位油炸羟基酮的形成
摘要:使用lda(二异丙基锂酰胺)和氯硅烷的简单试剂组合,开发了使用cipe辅助的α-甲硅烷基碳负离子对n,N-二乙基芳基酰胺进行羟基定向的烷基化反应(cipe =络合物诱导的邻近效应).报道了对该机理的研究,以及该方法在阴离子snieckus-Fries重排中的应用,以高效合成强效磷脂酰肌醇3-激酶(pi3K)抑制剂ly294002.
Doi:10.1002/anie.201404495

专利信息

专利号:CN-103880740-B
优先权日:2014-04-14
标题 :Synthesis of 4-nitro-3-hydroxy-2-pyridinecarboxylic acid

专利号:CN-103880740-A
优先权日:2014-04-14
标 题:Synthesis of 4-nitro-3-hydroxy-2-pyridinecarboxylic acid

专利号:US-9957277-B2
优先权日:2015-11-25
标题 :eIF4A-inhibiting compounds and methods related thereto
发明人：ERNST JUSTIN T; REICH SIEGFRIED H; SPRENGELER PAUL A; TRAN CHINH VIET; PACKARD Garrick Kenneth; XIANG ALAN X; NILEWSKI CHRISTIAN; MICHELS THEO
权利人:EFFECTOR THERAPEUTICS INC
摘要:The present invention provides synthesis, pharmaceutically acceptable formulations and uses of compounds in accordance with Formula I, or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof. n nFor Formula I compounds X, Y, R 1 , R 2 , R 3a , R 3b , R 4a , R 4b and R 5 are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4A and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.