1476-07-9Relevant articles and documents
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Valkanas,G. et al.
, p. 4248 - 4256 (1963)
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Bioactivity and structure–activity relationship of cinnamic acid derivatives and its heteroaromatic ring analogues as potential high-efficient acaricides against Psoroptes cuniculi
Chen, Dong-Dong,Zhang, Bing-Yu,Liu, Xiu-Xiu,Li, Xing-Qiang,Yang, Xin-Juan,Zhou, Le
supporting information, p. 1149 - 1153 (2018/03/05)
A series of cinnamic acid derivatives and its heteroaromatic ring analogues were synthesized and evaluated for acaricidal activity in vitro against Psoroptes cuniculi, a mange mite. Among them, eight compounds showed the higher activity with median lethal concentrations (LC50) of 0.36–1.07 mM (60.4–192.1 μg/mL) and great potential for the development of novel acaricidal agent. Compound 40 showed both the lowest LC50 value of 0.36 mM (60.4 μg/mL) and the smallest median lethal time (LT50) of 2.6 h at 4.5 mM, comparable with ivermectin [LC50 = 0.28 mM (247.4 μg/mL), LT50 = 8.9 h], an acaricidal drug standard. SAR analysis showed that the carbonyl group is crucial for the activity. The type and chain length of the alkoxy in the ester moiety and the steric hindrance near the ester group significantly influence the activity. The esters were more active than the corresponding thiol esters, amides, ketones or acids. Replacement of the phenyl group of cinnamic esters with α-pyridyl or α-furanyl significantly increase the activity. Thus, a series of cinnamic esters and its heteroaromatic ring analogues with excellent acaricidal activity emerged.
Use of Catalytic Static Mixers for Continuous Flow Gas-Liquid and Transfer Hydrogenations in Organic Synthesis
Hornung, Christian H.,Nguyen, Xuan,Carafa, Antony,Gardiner, James,Urban, Andrew,Fraser, Darren,Horne, Mike D.,Gunasegaram, Dayalan R.,Tsanaktsidis, John
supporting information, p. 1311 - 1319 (2017/09/23)
Catalytic static mixers were used for the continuous flow hydrogenation of alkenes, alkynes, carbonyls, nitro- and diazo-compounds, nitriles, imines, and halides. This technique relies on tubular reactors fitted with 3D printed static mixers which are coated with a catalytic metal layer, either Pd or Ni. Additive manufacturing of the metal mixer scaffold results in maximum design flexibility and is compatible with deposition methods such as metal cold spraying which allow for mass production and linear process scale up. High to full conversion was achieved for the majority of substrates, demonstrating the flexibility and versatility of the catalytic static mixer technology. In the example of an alkyne reduction, the selectivity of the flow reactor could be directed to either yield an alkene or alkane product by simply changing the reactor pressure.
