1289646-93-0Relevant articles and documents
Scalable Process for Making 5,7-Dichlorotetrahydroisoquinoline-6-carboxylic Acid Using Methylene as the Protecting Group
Xu, Wanbin,Gong, Xudong,Odilov, Abdullajon,Hu, Tianwen,Jiang, Xiangrui,Zhu, Fuqiang,Guo, Shuang,Jiang, Dehui,Wu, Mingjun,Shen, Jingshan
, p. 2447 - 2452 (2021/11/13)
The development of an industrially scalable synthetic route for 5,7-dichlorotetrahydroisoquinoline-6-carboxylic acid (1), a key starting material for lifitegrast, is described. This route includes the following features: (1) tetrahydroisoquinoline19was pr
3,5-dichloro-4-bromoisoquinoline derivative, and preparation method and application thereof
-
, (2019/10/04)
The invention specifically relates to a novel compound, i.e., a 3,5-dichloro-4-bromoisoquinoline derivative, and a preparation method and application thereof, belonging to the technical field of pharmaceutical synthesis. 3,5-dichloro-4-bromoisoquinoline and the derivative thereof are obtained by ring closure of 3,5-dichloro-4-bromobenzene haloethylamine through a Friedel-Crafts alkylation reaction. The 3,5-dichloro-4-bromoisoquinoline and the derivative can be used for synthesizing the important intermediate 3,5-dichloro-4-carboxylisoquinoline of Lifitegrast. According to a technical scheme in the invention, low-cost and well-supplied 2,6-dichloroaniline is used as a starting material; and the preparation method comprises a plurality steps of reactions with mild conditions, mature operation and yield of 85% or more, and each step of reaction has passed pilot-scale test, so the feasibility of industrial conversion of the method is very high and overall production cost can be greatly reduced.