| 第 51 卷第 6 期 |  | Vol. 51 No. 6 | | 2021 年 12 月 | Dec 2021 |
|
所属栏目：专论与综述
氮杂环醇制备方法及其药物合成中的应用进展 |
| 冯志强 1， 门 靖 1*， 李成利 1， 丁志新 1， 董 曼 2
（1.西安万隆制药股份有限公司， 陕西 西安 710119; 2. 陕西顺天医药有限公司， 陕西 西安 710077)
|
| 摘 要：氮杂环醇（Azacyclonol）属于含有氮杂环的二苯甲醇行生物， 具有良好的反应活性， 广泛应用于有
机合成、 药物及特种材料制备等领域。 综述了氮杂环醇的合成， 依据起始物料比较了以 4-咄唗甲酸乙趴、4-派唗甲酸、 N-乙酰基派唗-4-酰基氯、 4-氛基咄唗为原料制备氮杂环醇的 4 条合成路线。
其中， 以 4- 派唗甲酸路线较优， 具备工时短、 能耗低、 物料价廉易得、 操作简便之特点， 宜于工业化大生产。 同时归纳了氮杂环醇在药物合成中的应用并展望了其发展趋势。
为探究更经济、 高效的氮杂环醇合成方法及下游医药产品开发提供借鉴意义。
|
| 关键词：氮杂环醇； 二苯基甲醇； 合成方法； 应用进展
|
| 中图分类号：TQ463 文献标识码：B 文章编号：1009-9212(2021)06-0006-06 |
|
| Preparation for Azacyclonol and Its Application in Drug Synthesis
|
| FENG Zhi-qiangl, MEN Jingl*, LI Cheng-lil, DING Zhi-xinl, DONG Man2
( 1. Xi'an Wanlong Pharmaceutical Co.,Ltd., Xi'an 710119, China; 2. Shaanxi Shuntian Pharmaceutical
Limited Company, Xi 'an 710077, China)
|
| Abstract：Azacyclonol is a derivative compound of piperidine benzhydrol with high reactivity and
widely used in
research fields such as organic synthesis, pharmaceutical preparation, and special materials. In
this paper, the synthetic routes of azacyclonol in recent years were reviewed. Based on different
starting materials including ethyl 4 -picolinate, 4 -piperidine carboxylic acid, N
-acetylpiperidine -4 -acid chloride, and 4 -cyano, four synthetic routes for the preparation of
azacyclonol were analyzed including their advantages and disadvantages. Among these four synthesis
methods, the 4 -piperidine carboxylic acid route was the best one, which had the characteristics
including short working hours, low energy consumption, low cost and easy availability of raw
materials, and simple operation. It had advantages in large-scale industrial production. At the
same time, azacyclonol in drug synthesis was summarized, and its development trend was prospected.
It provided reference for exploring economical and efficient synthesis methods of azacyclonol and
the development of downstream products.
|
| Key words：azacyclonol; benzhydrol; synthesis method; application progress
|
|
作者简介：冯志强(1976—)，男，陕西扶风人，高级工程师，主要从事制剂和药物分析工作。
|
联 系 人：门 靖，高级工程师，硕士，主要从事医药研发、原料药技术转移及申报资料撰写工作（E-mail 1257391857@qq.com)。
|
收稿日期：2021-07-0
|
|