2-[4-(4-羟基苄基)哌嗪-1-基甲基]吡唑并[1,5-α]吡啶的合成及活性分析

Synthesis of 2-[4-(4-hydroxylbenzyl)piperazin-1-ylmethyl] Pyrazolo [1,5-α]Pyridine and Activity Assay

以吡唑并[1，5-α]吡啶-2一甲醛、N-甲酰基哌嗪和4-羟基苯甲醛为原料，经过三步反应合成了2-[4-（4-羟基苄基）哌嗪-1-基甲基]吡唑并[1，5-α]吡啶，通过1HNMR、ESIMS对中间体及目标化合物进行了结构表征，并通过体外活性实验，测定目标化合物对多巴胺对D2、D3、D4受体受体的亲和常数分别为4200、2590、2．2nM，对D4受体的亲和性较对D2、D3受体的均大于1000，显示对多巴胺D4受体具有一定的选择性亲和活性．

With the investment of the national infrastructure, the construction of large bridges crossing the big river and harbor has become more and more common. The super-long bored piles with large capacity and adaptability have become increasingly widespread in the application of bridge foundation. The present design of bridge piles based on the ＂code for design of ground base and foundation of highway bridges and culverts＂ which most of the design parameters are summarized from the ordinary pile becomes unsuitable for the super-long bored piles because of the difference in the load transfer mechanism and deformation. Therefore, based on the information gathered from the pile tests, we can obtain the statistical parameter of the typical strata properties. Then calculating the reliability index value and analyzing the impact factor of reliability index. At last, it can provide a theoretical reference for the design of super-long bored pile.