Department of Organic Chemistry and Technology, Budapest University of Technology and Economics, 1521 Budapest, Hungary.
Gedeon Richter Plc, PO Box 27, 1475 Budapest, Hungary.
Molecules. 2021 Apr 2;26(7):2040. doi: 10.3390/molecules26072040.
A new, continuous-flow consecutive reduction method was developed for the C-N bond formation in the synthesis of the key intermediate of the antipsychotic drug cariprazine. The two-step procedure consists of a DIBAL-H mediated selective ester reduction conducted in a novel, miniature alternating diameter reactor, followed by reductive amination using catalytic hydrogenation on 5% Pt/C. The connection of the optimized modules was accomplished using an at-line extraction to prevent precipitation of the aluminum salt byproducts.
一种新的、连续流动连续还原方法被开发用于合成抗精神病药物卡利拉嗪的关键中间体的 C-N 键形成。该两步法包括在新型微型交替直径反应器中进行的 DIBAL-H 介导的选择性酯还原，然后使用 5%Pt/C 上的催化氢化进行还原胺化。通过在线萃取来连接优化的模块，以防止铝盐副产物沉淀。
