当前位置：
X-MOL 学术
›
Org. Process Res. Dev.
›
论文详情
Our official English website, www.x-mol.net, welcomes your
feedback! (Note: you will need to create a separate account there.)
Continuous and Selective Hydrogenation of Heterocyclic Nitroaromatics in a Micropacked Bed Reactor
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2021-08-15 , DOI: 10.1021/acs.oprd.1c00164 Xiaonan Duan 1 , Xuepeng Wang 2 , Xingkun Chen 2 , Jisong Zhang 1
Organic Process Research & Development ( IF 3.1 ) Pub Date : 2021-08-15 , DOI: 10.1021/acs.oprd.1c00164 Xiaonan Duan 1 , Xuepeng Wang 2 , Xingkun Chen 2 , Jisong Zhang 1
Affiliation
|
The hydrogenation of heterocyclic nitroaromatics is of great importance in the pharmaceutical industry for the synthesis of key intermediates. However, high selectivity is difficult to achieve in conventional batch reactors owing to severe back mixing and poor mass transfer performance, resulting in the high requirement for subsequent separation processes. In this work, a continuous flow system based on a micropacked bed reactor is developed for the selective hydrogenation of heterocyclic nitroaromatics and the reductions of 5-nitroisoquinoline to 5-aminoisoquinoline and 5-amino-1,2,3,4-tetrahydroisoquinoline are selected as the model reactions. With the optimal reaction conditions, maximal yields of 99.9% (5-aminoisoquinoline) and 99.3% (5-amino-1,2,3,4-tetrahydroisoquinoline) are obtained successfully. Moreover, this system exhibits remarkable performance for the selective hydrogenation of relevant heterocyclic nitroaromatics with all yields beyond the level of 97.5%. The continuous flow system enables efficient hydrogenation of heterocyclic nitroaromatics and remarkable selectivity of target products with shorter reaction time and safer operation compared with batch reactors.
中文翻译：
微填充床反应器中杂环硝基芳烃的连续选择性加氢
杂环硝基芳烃的加氢在制药工业中对关键中间体的合成具有重要意义。然而，传统间歇式反应器回混严重，传质性能差，难以实现高选择性，对后续的分离过程提出了很高的要求。在这项工作中，开发了一种基于微填充床反应器的连续流动系统，用于杂环硝基芳烃的选择性加氢，并选择将 5-硝基异喹啉还原为 5-氨基异喹啉和 5-氨基-1,2,3,4-四氢异喹啉作为模型反应。在最佳反应条件下，成功获得了99.9%（5-氨基异喹啉）和99.3%（5-氨基-1,2,3,4-四氢异喹啉）的最大产率。而且，该系统对相关杂环硝基芳烃的选择性加氢表现出卓越的性能，收率均超过97.5%。与间歇式反应器相比，连续流动系统能够实现杂环硝基芳烃的高效加氢和显着的目标产物选择性，反应时间更短，操作更安全。
更新日期：2021-09-17
中文翻译：
微填充床反应器中杂环硝基芳烃的连续选择性加氢
杂环硝基芳烃的加氢在制药工业中对关键中间体的合成具有重要意义。然而，传统间歇式反应器回混严重，传质性能差，难以实现高选择性，对后续的分离过程提出了很高的要求。在这项工作中，开发了一种基于微填充床反应器的连续流动系统，用于杂环硝基芳烃的选择性加氢，并选择将 5-硝基异喹啉还原为 5-氨基异喹啉和 5-氨基-1,2,3,4-四氢异喹啉作为模型反应。在最佳反应条件下，成功获得了99.9%（5-氨基异喹啉）和99.3%（5-氨基-1,2,3,4-四氢异喹啉）的最大产率。而且，该系统对相关杂环硝基芳烃的选择性加氢表现出卓越的性能，收率均超过97.5%。与间歇式反应器相比，连续流动系统能够实现杂环硝基芳烃的高效加氢和显着的目标产物选择性，反应时间更短，操作更安全。
京公网安备 11010802027423号