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Synthesis of (S)-2-acetamido-3-(4-hydroxy-3-(3-methylbut-2-enyl) phenyl) propanoic acid derivatives

机译:(S)-2-乙酰氨基-3-(4-羟基-3-(3-甲基丁-2-烯基)苯基)丙酸衍生物的合成

摘要

A method for producing a compound of formula (I) or a pharmaceutically acceptable salt, solvate, tautomer or stereoisomer, such as compound 1 and compound 2 is disclosed. The method proceeds through an O-allylated tyrosine-based compound, such as compound 3 and preferably comprises [3,3] sigmatropic Claisen rearrangement and olefin cross metathesis reactions. In addition, a pharmaceutical composition comprising a compound of formula (I) a tumor necrosis factor (TNF) related apoptosis inducing ligand (TRAIL) and a pharmaceutically acceptable carrier or excipient is disclosed.
机译:公开了制备式(I)化合物或药学上可接受的盐,溶剂化物,互变异构体或立体异构体,例如化合物1和化合物2的方法。该方法通过基于O-烯丙基化的酪氨酸的化合物,例如化合物3进行,并且优选地包括[3,3]σ型克莱森重排和烯烃交叉复分解反应。另外,公开了包含式(I)的化合物,肿瘤坏死因子(TNF)相关的细胞凋亡诱导配体(TRAIL)和药学上可接受的载体或赋形剂的药物组合物。

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