铑催化吲哚导向芳烃与氮杂苯并冰片烯的加成开环反应

碳氢键的直接官能团化已成为有机合成中构筑碳碳键的一种高效方法.这种转化不需要预官能团化,被认为是原子步骤经济的合成途径.在不同导向基辅助过渡金属催化下,区域选择性碳氢官能团化为C–C和C–X键的构建提供了一种简洁的方法.Rh(Ⅲ)催化氮杂苯并冰片烯C–H活化开环反应已有研究,但反应体系中通常需要添加氧化剂或者反应条件苛刻.本文开发了2-芳基吲哚与氮杂苯并降冰片烯的开环反应研究.该反应体系无需氧化剂,化学区域选择性高,官能团兼容性好,条件温和,反应产率高达98%,为2-芳基氢化萘衍生物的合成提供了高效便捷的方法.

Expert consensus on the technical specifications of the in vitro skin penetration test of cosmetic product by Franz diffusion cell

Background:Diffusion cell test is one of the most commonly used in vitro model to detect the percutaneous absorption of cosmetic ingredients.Although PRC State Administration of Quality Supervision and Quarantine has issued the guideline for the in vitro test method for the percutaneous absorption of drug molecules,there is still a lack of guideline for the percutaneous absorption test of cosmetic components.Objective:In order to improve the standardized level and make the in vitro percutaneous absorption test of cosmetic ingredients more comparable,based on the international and domestic experience,Transdermal Drug Delivery Committee of the World Federation of Chinese Medicine Societies organized the experts to discuss and formed this consensus as reference for the percutaneous absorption test of cosmetic components.Materials and Methods:To standardize the in vitro diffusion cell test technique for transdermal penetration of functional cosmetic ingredients,the Transdermal Drug Delivery Professional Committee of the World Federation of Societies of Traditional Chinese Medicine has organized many discussions among experts.

可见光敏化的肉桂酰胺构型异构化反应

肉桂酰胺是一类具有苯乙烯结构的化合物,立体构型(Z/E构型)对其物理性质、化学性质及生物活性均有着较大的影响.天然提取和合成的肉桂酰胺一般为反式异构体,而顺式异构体的合成较为困难.本文主要研究了在可见光促进下,肉桂酰胺的构型异构化反应.通过对反应条件的优化,建立了一种简单、高效的肉桂酰胺的顺反构型异构化方法.该方法仅需要万分之一的有机光敏剂4CzIPN,即可顺利实现未保护的(E)式肉桂酰胺转化为(Z)式构型,Z/E比例最高可以达到95:5,具有条件温和、催化剂用量少、官能团耐受等优点.