In 2017,Saifuzzaman, Md.; Morrison, Rick; Zheng, Zhaohua; Orive, Stephanie; Hamilton, Justin; Thompson, Philip E.; Al-rawi, Jasim M. A. published 《Synthesis and biological evaluation of 8-aryl-2-morpholino-7-O-substituted benzo[e][1,3]oxazin-4-ones against DNA-PK, PI3K, PDE3A enzymes and platelet aggregation》.Bioorganic & Medicinal Chemistry published the findings.Application In Synthesis of 2-(Bromomethyl)pyridine hydrobromide The information in the text is summarized as follows:
A series of 40 7-(O-substituted)-2-morpholino-8-aryl-4H-benzo[e][1,3]oxazin-4-ones I [R1 = benzyl, 2-pyridylmethyl, (4-methylpiperazinyl)ethyl; R2 = 2-thiophenyl, 4-ClC6H4, dibenzo[b,d]thiophen-4-yl, etc.] were synthesized. They were prepared via synthesis of a key precursor, I [R1 = H; R2 = Br] which was amenable to ether synthesis at the 7-position and Suzuki coupling at the 8-position. The 2 protons of 7-OCH2 in compounds I [R1 = benzyl; R2 = benzo[b]thiophen-2-yl, dibenzo[b,d]thiophen-4-yl, dibenzo[b,d]furan-4-yl, naphthalen-1-yl, thianthren-1-yl] prove to be magnetically non-equivalent, atropisomerism (axial chirality), as result of sterically hindered rotation of the bulky 8-aryl-substituent. The products I were evaluated for their activities against PI3K isoforms, DNA-PK and PDE3. The results showed that this substitution pattern had a deleterious effect on PI3K activities, which may arise from steric hindrance in the active site. PI3Kδ was somewhat more tolerant of this substitution particularly where 8-(4-methoxylphenyl) substituents were present (IC50s ∼ 2-3 μM). Good activities against PDE3 were also obtained for compounds, with particular members of the 7-(2-pyridinyl) methoxy series showing good inhibition (IC50s ∼ 2-3 μM), comparable to previously described analogs. Compound I [R1 = (4-methylpiperazinyl)ethyl, R2 = Ph] effectively inhibited ADP-induced platelet aggregation with an IC50 of 8 μM. The results came from multiple reactions, including the reaction of 2-(Bromomethyl)pyridine hydrobromide(cas: 31106-82-8Application In Synthesis of 2-(Bromomethyl)pyridine hydrobromide)
2-(Bromomethyl)pyridine hydrobromide(cas: 31106-82-8) belongs to pyridine. In industry and in the lab, pyridine is used as a reaction solvent, particularly when its basicity is useful, and as a starting material for synthesizing some herbicides, fungicides, and antiseptics.Application In Synthesis of 2-(Bromomethyl)pyridine hydrobromide