1-苄基-4-哌啶酮的合成工艺改进

以苄胺和丙到甲酯为起始原料，合成OPC－21268的重要中间体1－苄基－4－哌啶酮，并对每步反应的工艺进行优化，确定了最佳反应条件，三步反应的总收率为74．5％，比文献值提高了14．5％，新工艺做法简单，成本降低，适于工业生产。     

Catalytic enhancement of hydrogen evolution reaction on copper in the presence of benzylamine

Benzylamine catalytic effect on the cathodic hydrogen evolution in acid aqueous solution has been studied on copper electrode. Experimental results obtained by voltammetric techniques emphasize that the presence of benzylamine in 1 M sulfuric acid solution enhances the hydrogen evolution reaction (HER). In such a solution, benzylamine is protonated and exists as benzylammonium cation. Kinetic parameters of HER have been determined, observing a significant increase of the exchange current in the presence of benzylamine. Also, a decrease of the cathodic transfer coefficient has been noticed. Activation energy for HER has been computed on the basis of the Arrhenius plots. In the presence of benzylamine the activation energy was 33.0 kJ mol⁻¹, whereas without benzylamine a greater value was obtained: 94.6 kJ mol⁻¹. The catalytic effect of benzylamine was confirmed by electrochemical impedance spectroscopy. The considerable diminution of the double layer capacity is a valid proof of the strong adsorption of benzylamine at the Cu - sulfuric acid solution interface, while the reduction of the charge transfer resistance is a symptom of the enhancement of HER. Ab initio molecular modeling of benzylammonium ion showed that, due to a high value of the dipole moment, the molecules are oriented in the most favorable position for the charge transfer reaction, i.e., with the protonated amino group facing toward the electrode.     

CL-20原料胺的工业制备方法

报道了 CL - 2 0原料胺的一种新的制备方法。在芳香醛存在下 ,苄基氯与氨水反应生成苄基胺 ,加入芳香醛可有效地抑制副产物二苄胺、三苄胺的生成 ,苄基胺的产率达到 70 %以上 ;反应物采用浓氨水可使反应体系体积缩小 ,提高生产能力 ,此方法设备简单 ,操作简便 ,采用密闭操作 ,防止空气污染 ,产率高 ,成本低 ,对降低 CL- 2 0的生产成本有重要意义