Synthesis of Highly Substituted 4<i>H</i>‑Pyrido[1,2‑<i>a</i>]pyrimidines via a One-Pot Three-Component Condensation Reaction

A one-pot three-component reaction, involving condensation of 2-aminopyridines, aldehydes, and ketones/aldehydes under trifluoromethanesulfonic acid catalysis, provides rapid access to highly substituted novel 4<i>H</i>-pyrido­[1,2-<i>a</i>]­pyrimidines

Synthesis of Highly Substituted 4<i>H</i>‑Pyrido[1,2‑<i>a</i>]pyrimidines via a One-Pot Three-Component Condensation Reaction

A one-pot three-component reaction, involving condensation of 2-aminopyridines, aldehydes, and ketones/aldehydes under trifluoromethanesulfonic acid catalysis, provides rapid access to highly substituted novel 4<i>H</i>-pyrido­[1,2-<i>a</i>]­pyrimidines

Single-Electron Oxidation/Alterable C3- and C10-Arylation of 9‑MeO-phenanthrene

A reactivity pattern for C3-arylation of 9-MeO-phenanthrene has been established for the first time by using 2-naphthyl amines as coupling partners. A series of phenanthrene- and naphthalene-based multifunctionalized polycyclic aromatic hydrocarbons have been obtained in good to excellent yields. Alternative C10-arylation of 9-MeO-phenanthrene has also been accomplished, using 2-naphthalenol derivatives as coupling partners. Trifluoroacetic acid is found crucial for the regioselectivity. Density functional theory calculations and electrochemical analyses have been performed to rationalize the reaction mechanism

Discovery of Novel Tricyclic Thiazepine Derivatives as Anti-Drug-Resistant Cancer Agents by Combining Diversity-Oriented Synthesis and Converging Screening Approach

An efficient discovery strategy by combining diversity-oriented synthesis and converging cellular screening is described. By a three-round screening process, we identified novel tricyclic pyrido­[2,3-<i>b</i>]­[1,4]­benzothiazepines showing potent inhibitory activity against paclitaxel-resistant cell line H460_TaxR (EC₅₀ < 1.0 μM), which exhibits much less toxicity toward normal cells (EC₅₀ > 100 μM against normal human fibroblasts). The most active hits also exhibited drug-like properties suitable for further preclinical research. This redeployment of antidepressing compounds for anticancer applications provides promising future prospects for treating drug-resistant tumors with fewer side effects