Tofacitinib for Prurigo Nodularis: A Case Report.

Purpose: Despite recent advances in the treatment of prurigo nodularis, conventional treatment suffers from a dilemma of poor efficacy. The clinical use of Janus kinase (JAK) inhibitors in the treatment of Prurigo nodularis has rarely been explored. Patients and Methods: We present a case of prurigo nodularis successfully treated with, JAK inhibitor tofacitinib with no adverse effects. Results: This case report of successful treatment shows a good clinical efficacy of using JAK inhibitor tofacitinib in the treatment of prurigo nodularis. Cytokines may be an important cause of prurigo nodularis. Conclusion: JAK inhibitor tofacitinib may be a new option for the treatment of prurigo nodularis, especially for patients who have failed conventional treatment.

Synthesis of 2-alkoxy(aroxy)-3-substituted quinolines by DABCO-promoted cyclization of o-alkynylaryl isocyanides.

Diversified 2-alkoxy- and 2-aroxy-3-substituted quinolines were synthesized from o-alkynylaryl isocyanides and alcohols and phenols promoted by DABCO, respectively. The reaction was initiated by nucleophilic addition of DABCO to isocyanide and subsequent cycliztion, leading to a DABCO-quinoline-based adduct as the reactive intermediate, followed by substitution of the DABCO moiety with oxygenated nucleophiles.

A direct intramolecular C-H amination reaction cocatalyzed by copper(II) and iron(III) as part of an efficient route for the synthesis of pyrido[1,2-a]benzimidazoles from N-aryl-2-aminopyridines.

A novel and efficient synthesis of pyrido[1,2-a]benzimidazoles through direct intramolecular aromatic C-H amination of N-aryl-2-aminopyridines has been developed. The reaction, cocatalyzed by Cu(OAc)(2) and Fe(NO(3))(3)·9H(2)O, is carried out in DMF under a dioxygen atmosphere. Diversified pyrido[1,2-a]benzimidazoles containing various substitution patterns are obtained in moderate to excellent yields by using this procedure. The results of mechanistic studies suggest that a Cu(III)-catalyzed electrophilic aromatic substitution (S(E)Ar) pathway is operating in this process. The unique role of iron(III) is believed to lie in its ability to facilitate formation of the more electrophilic Cu(III) species. In the absence of iron(III), a much less efficient and reversible Cu(II)-mediated S(E)Ar process takes place.