Scalable Process of Making 5,7-Dichloro-tetrahydroisoquinoline-6-carboxylic Acid Using Methylene as the Protecting Group was written by Xu, Wanbin;Gong, Xudong;Odilov, Abdullajon;Hu, Tianwen;Jiang, Xiangrui;Zhu, Fuqiang;Guo, Shuang;Jiang, Dehui;Wu, Mingjun;Shen, Jingshan. And the article was included in Organic Process Research & Development in 2021.HPLC of Formula: 73075-47-5 This article mentions the following:
The development of an industrially scalable synthetic route for a key starting material for Lifitegrast, compound I was described. The features of this route include: (1) Tetrahydroisoquinoline II was prepared by three steps from readily com. available 3, 5-dichlorobenzoyl chloride and 2-aminoethanol in a high total yield of 76%; (2) Formaldehyde instead of triphenylmethyl chloride was employed in the protection of the secondary amine, owning much higher atom economy; (3) The target compound I was produced with an overall yield of 66%, and an HPLC purity of 99% by area. In the experiment, the researchers used many compounds, for example, 5,7-Dichloro-1,2,3,4-tetrahydroisoquinoline hydrochloride (cas: 73075-47-5HPLC of Formula: 73075-47-5).
5,7-Dichloro-1,2,3,4-tetrahydroisoquinoline hydrochloride (cas: 73075-47-5) belongs to tetrahydroisoquinoline derivatives. Tetrahydroisoquinoline motif is often present in natural products with a broad range of biological and pharmacological activities. An oxidative C1 arylation of tetrahydroisoquinolines with aryl Grignard reagents is mediated by diethyl azodicarboxylate (DEAD). This C-H activation under metal-free conditions delivers target compounds, including some naturally occurring alkaloids, in good yields.HPLC of Formula: 73075-47-5
Referemce:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem