TBHP-Mediated Oxidative Decarboxylative Cyclization in Water: Direct and Sustainable Access to Anti-malarial Polycyclic Fused Quinazolinones and Rutaecarpine was written by Chen, Xingyu;Xia, Fei;Zhao, Yifan;Ma, Ji;Ma, Yue;Zhang, Dong;Yang, Lan;Sun, Peng. And the article was included in Chinese Journal of Chemistry in 2020.Safety of 7-Methyl-1,2,3,4-tetrahydroisoquinoline This article mentions the following:
Polycyclic fused quinazolinones I [R = H, Cl, Br, F, Cl; R1 = H, Me, Cl, etc.; R2 = H, MeO, F, Br, Cl; R3 = H, Me; R4 = H, F; R5 = H, MeO; R6 = H, Me, F, Br, MeO] with anti-malarial activity were synthesized through tert-Bu hydroperoxide (TBHP)-mediated oxidative decarboxylative cyclization between com. available isatins and cyclic amines in one step. The reaction proceeded smoothly in water without addnl. transition-metal catalyst, acid and base. The newly synthesized products were evaluated to exhibit moderate to good anti-malarial activity against chloroquine drug-sensitive Plasmodium falciparum 3D7 strain. Addnl., this method also provided direct approach to rutaecarpine in good yield. In the experiment, the researchers used many compounds, for example, 7-Methyl-1,2,3,4-tetrahydroisoquinoline (cas: 207451-81-8Safety of 7-Methyl-1,2,3,4-tetrahydroisoquinoline).
7-Methyl-1,2,3,4-tetrahydroisoquinoline (cas: 207451-81-8) belongs to tetrahydroisoquinoline derivatives. Tetrahydroisoquinoline motif is often present in natural products with a broad range of biological and pharmacological activities. Among them, 1-substituted tetrahydroisoquinolines are privileged scaffolds in drugs and pharmaceuticals. 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.Safety of 7-Methyl-1,2,3,4-tetrahydroisoquinoline
Referemce:
Tetrahydroisoquinoline – Wikipedia,
1,2,3,4-Tetrahydroisoquinoline | C9H11N – PubChem