一种吡啶基咪唑并苯并二氮杂卓丙酸酯化合物及其合成和应用

文档序号:1116968 发布日期:2020-09-29 浏览:7次 >En<

阅读说明:本技术 一种吡啶基咪唑并苯并二氮杂卓丙酸酯化合物及其合成和应用 (Pyridyl imidazobenzodiazepine propionate compound and synthesis and application thereof ) 是由 漆又毛 于 2018-12-28 设计创作,主要内容包括:本发明公开了一种吡啶基咪唑并苯并二氮杂卓丙酸酯(化合物1)及其合成和应用。本发明还提供制备中间体。本发明提供的化合物1具有明显的静脉麻醉活性,静脉麻醉活性等同于阳性对照药瑞马唑仑对甲苯磺酸盐或者瑞马唑仑苯磺酸盐。此外化合物1在小鼠模型实验中可以明显降低,甚至克服了瑞马唑仑苯磺酸盐或者瑞马唑仑对甲苯磺酸盐作为在研药物在临床前动物实验中常见的四肢抖动,昂头,角弓反张等副作用,因此可在制备静脉麻醉药物中的应用。化合物1的结构通式如下,其中各基团和取代基的定义如说明书中所述。&lt;Image he="552" wi="563" file="DDA0002627645510000011.GIF" imgContent="drawing" imgFormat="GIF" orientation="portrait" inline="no"&gt;&lt;/Image&gt;(The invention discloses pyridyl imidazobenzodiazepine propionate (compound 1) and synthesis and application thereof. The invention also provides a preparation intermediate. The compound 1 provided by the invention has obvious intravenous anesthetic activity, and the intravenous anesthetic activity is equal to that of a positive control medicament of remazolam p-toluenesulfonate or remazolam benzenesulfonate. In addition, the compound 1 can be obviously reduced in a mouse model experiment, and even overcomes the side effects of extremity shaking, head raising, angle reversal, and the like which are commonly seen in animal experiments before clinical use of remazolen benzene sulfonate or remazolen p-toluenesulfonate as a research medicament, so that the compound can be applied to the preparation of intravenous anesthesia medicaments. The compound 1 has the following structural general formula, wherein the definitions of each group and substituent are described in the specification.)

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