Development of a Scalable Synthesis of a VEGFR Inhibitor was written by Chen, Ying;Crockett, Richard D.;Wang, Xin;Larsen, Robert D.;Cui, Sheng;Faul, Margaret M.. And the article was included in Synlett in 2013.Safety of Isoquinolin-7-amine This article mentions the following:
Process development and salt selection for a novel -VEGFR inhibitor are described. The overall convergent synthesis involved coupling of three key fragments, 2-chloronicotinoyl chloride, 4-isopropyl-3-methylaniline and 7-aminoisoquinoline. A cost-effective and scalable synthesis of 7-aminoisoquinoline was also achieved. A transition-metal-free SNAr process enabled the final C-N coupling to afford the target mol. A phosphate form of the drug substance with improved phys. properties was selected for further development and the corresponding crystallization process was subsequently developed. Overall, a robust six-step route was developed and demonstrated on multikilogram scales affording the target compound in >30% yield and high purity (>99%). In the experiment, the researchers used many compounds, for example, Isoquinolin-7-amine (cas: 23707-37-1Safety of Isoquinolin-7-amine).
Isoquinolin-7-amine (cas: 23707-37-1) belongs to isoquinoline derivatives. Quinoline is a mancude organic heterobicyclic parent, an azaarene, an ortho-fused heteroarene and a member of isoquinolines. Isoquinoline-type alkaloids show biological activities similar to those of morphinane-, protoberberine-, and benzophenanthridine-type alkaloids.Safety of Isoquinolin-7-amine
Referemce:
Isoquinoline – Wikipedia,
Isoquinoline | C9H7N – PubChem