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7H-pyrrolo[2,3-d]pyrimidine 5-bromo-7-(p-toluenesulfonyl)-7H-pyrrolo[2,3-d]pyrimidine tert-butyl 2-(5-bromo-7H-pyrrolo[2,3-d]pyrimidin-7-yl)acetate 7H-吡咯并[2,3-D]嘧啶置于溴体系中,用 N,N-二甲基甲酰胺 用作溶剂,化学反应 2.0H,以40%的收率获得5-溴-7H-吡咯并[2,3-D]嘧啶
参考文献:稠合杂芳族环系统.第24部分.吡咯烷[2,3-D ]嘧啶海洋生物碱刚性蛋白的合成
标题:稠合杂芳族环系统.第24部分.吡咯烷[2,3-D ]嘧啶海洋生物碱刚性蛋白的合成
摘要:海洋生物碱刚性蛋白是由2,4-二甲氧基-7-苯基磺酰基吡咯并[2,3-D ]嘧啶合成的.吡咯并[2,3-D ]嘧啶的锂化,然后用n,4-二甲氧基-N-甲基苯甲酰胺进行亲电取代,得到6-(4-甲氧基)苯甲酰基衍生物,其通过碱水解和随后的碘化反应转化为2,4-二甲氧基-5-碘吡咯并[2,3-D ]嘧啶-6-基4-甲氧基苯基酮.用2-(4-甲氧基苯基)-1,3,2-二氧杂硼烷进行钯催化的芳基化反应,然后用三溴化硼脱甲基,得到刚性蛋白.
Doi:10.1039/p19960000459
专利信息
专利号:US-11014926-B2
优先权日:2015-10-29
标 题 :Pyrrolo-, pyrazolo-, imidazo-pyrimidine and pyridine compounds that inhibit MNK1 and MNK2
发明人:SPRENGELER PAUL A; REICH SIEGFRIED H; ERNST JUSTIN T; WEBBER STEPHEN E
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 A 1 , A 2 . A 3 , A 4 , A 5 , A 6 , A 7 , W 1 , R 1 , R 2 , R 3 , R 4 , R 5a , R 5b , R 6 , R 7 , R 7a , R 7b , R 8 , R 8a , R 8b , R 9 , R 9a , R 9b and R 10 and subscripts “mâ€? and “nâ€? are as defined in the specification. The inventive Formula I compounds are inhibitors of Mnk and find utility in any number of therapeutic applications, including but not limited to treatment of inflammation and various cancers.