CAS: 602303-26-4; 7-Chloro-2-Iodothieno[3,2-B]Pyridine

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CAS号69627-03-8 7-氯噻吩{3,2-B}吡啶 | CAS号69627-02-7 噻吩并[3,2-b]吡啶-7(4H)-酮 | CAS号913377-45-4 2,2-Dimethyl-5-... | CAS号225385-09-1 7-氯-2-(1-甲基-1H-...

7-氯噻吩并[3,2-B]吡啶置于正丁基锂,碘体系中,用 四氢呋喃,正己烷 作为反应溶剂,化学反应 21.3H,以84%的收率获得产物7-氯-2-碘噻吩并[3,2-B]吡啶
参考文献:大规模制备咪唑-噻吩并吡啶的交叉偶联方法:[2-(3-Methyl-3H-Imidazol-4-yl)-Thieno[3,2-B]Pyridin-7-Yl]-的合成(2-甲基-1H-吲哚-5-基)-胺
标题:大规模制备咪唑-噻吩并吡啶的交叉偶联方法:[2-(3-Methyl-3H-Imidazol-4-yl)-Thieno[3,2-B]Pyridin-7-Yl]-的合成(2-甲基-1H-吲哚-5-基)-胺
摘要:[2-(3-Methyl-3H-Imidazol-4-yl)-Thieno[3,2-B]Pyridin-7-Yl]-(2-Methyl-1H-Indol-5-yl)的数百克合成)-胺 (1) 描述了利用碘噻吩并吡啶 (3) 与 5-(三丁基甲锡烷基)-1-甲基咪唑 (11) 的 Stille 交叉偶联.评估了几种交叉偶联方法将噻吩并吡啶 3 转化为咪唑-噻吩并吡啶 2,但只有两种方法有效:Stille 偶联和源自 2-(叔丁基二甲基甲硅烷基)-1-的有机锌试剂的 Negishi 交叉偶联甲基咪唑和碘噻吩并吡啶 (3).后一种方法在实验室规模 (<50 G) 上运行非常好,但在放大时反复无常.讨论了有机锡烷试剂放大的问题,包括有机锡水平的控制和分析.
DOI:10.1021/op0340457

专利信息

专利号:US-11286268-B1
优先权日:2019-07-02
标题:EIF4E-inhibiting compounds and methods
发明人：SPERRY SAMUEL; XIANG ALAN X; ERNST JUSTIN T; REICH SIEGFRIED H; SPRENGELER PAUL A; SHAGHAFI MIKE; MICHELS THEO; NILEWSKI CHRISTIAN; TRAN CHINH VIET; PACKARD Garrick Kenneth; GRUBBS ALAN; URKALAN KAVERI; MUKAIYAMA TAKASUKE
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 n n n n n n n n n For Formula I compounds X 1 , X 2 , X 3 , X 4 , X 5 , X 6 , Q, L 1 , L 2 , Y, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R 7 , R 8 and rings A, B and C are as defined in the specification. The inventive Formula I compounds are inhibitors of eIF4e and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.