Stereoselective electrochemical carboxylation ofα,β-unsaturated sulfones

As an attractive C1 synthon,carbon dioxide(CO_(2))has been extensively used in organic synthesis to produce carboxylic acids.In this research,stereoselective electrochemical carboxylation ofα,β-unsaturated sulfones has been developed under transition-metal-free conditions.All the cinnamic acids and the derivatives are obtained selectively in the E-configuration.Besides,arylpropiolates also can be produced from alkynyl sulfones.

肿瘤微环境诱导多肽聚合物原位组装行为研究

设计合成了一种pH响应型的多肽聚合物,在中性条件下能够以聚合物单链的形式存在,在肿瘤微环境弱酸的刺激下发生聚集,提升入胞能力,从而实现对肿瘤细胞的高效杀伤.首先,通过迈克尔加成的方法合成了一系列生物相容性较好的β-硫代酸酯聚合物,并利用固相合成方法合成了治疗肽和穿膜肽2种多肽.然后,将治疗肽修饰上一种酸敏感基团,并将2种多肽通过迈克尔加成反应与聚合物共价连接.得到的多肽聚合物能够在中性水溶液中以单链形式稳定存在,而在pH=6.5条件下发生聚集.最后,在细胞层面对多肽聚合物进行研究,发现其在微酸性条件下可以通过内吞作用进入到肿瘤细胞,并具有更高的抗肿瘤能力.