Synthesis of fluoroalkylated alkynes via visible-light photocatalysis.

Fluoroalkylated alkynes, which are versatile building blocks for the synthesis of various biologically active organofluorine compounds, were synthesized from easily available alkynyl halides and fluoroalkyl halides by visible-light photocatalysis. Addition of fluoroalkyl radicals to alkynes and subsequent dehalogenation selectively yielded fluoroalkylated alkynes.

Access to Multifunctionalized Benzofurans by Aryl Nickelation of Alkynes: Efficient Synthesis of the Anti-Arrhythmic Drug Amiodarone.

An unconventional nickel-catalyzed reaction was developed for the synthesis of multifunctionalized benzofurans from alkyne-tethered phenolic esters. The transformation involves the generation of a nucleophilic vinyl NiII species by the regioselective syn-aryl nickelation of an alkyne, which then undergoes an intramolecular cyclization with phenol ester to yield highly functionalized 1,1-disubstituted alkenes with 3-benzofuranyl and (hetero)aryl substituents. The methodology can be used for the late-stage benzofuran incorporation of various drug molecules and natural products, such as 2-propylvaleric acid, gemfibrozil, biotin, and lithocholic acid. Furthermore, this arylative cyclization method was successfully applied for the efficient synthesis of the anti-arrhythmic drug amiodarone.

Construction of a Pentacyclic Framework Enabled by Nickel Catalysis.

We present a novel nickel-catalyzed reaction of indole-tethered 2-alkynylphenol esters with various (hetero)aryl boronic acids, resulting in the synthesis of diversely functionalized pentacyclic benzofurocyclohepta[b]indole derivatives. This unprecedented cascade reaction involves the arylative cyclization of alkynes, nucleophilic attack of the indole moiety on the oxonium ion intermediate, 1,2-alkyl group migration, and aromatization. The synthesized molecules exhibit exceptional cytotoxicity against multiple cancer cell lines while maintaining biocompatibility toward healthy cells.

The relationship between anxiety and irritable bowel syndrome symptoms among females: A cross-sectional study in Egypt.

There is a scarcity of studies focusing on irritable bowel syndrome (IBS) and anxiety in Egypt. Accordingly, our study aimed to assess the association between anxiety and IBS symptomatology among Egyptian females. Three hundred eighty-three females (145 IBS and 238 controls) were included in the study, and data were obtained using structured predesigned questionnaires. IBS and anxiety symptoms were assessed according to the Rome IV criteria and the Arabic version of the beck anxiety inventory, respectively. Both IBS and non-IBS groups showed increased anxiety during the pandemic, without a significant difference between both groups (P value = .657). Higher levels of education were significantly associated with severe anxiety (P value = .031). Multivariate analysis of IBS patients showed that intermediate education was significantly associated with 75% lower odds for increased IBS symptoms compared with illiterate or read-and-write IBS patients [odds ratio (OR): 0.25, 95% confidence interval (CI) 0.06-0.95, P value = .042]. Urban residence was significantly associated with 13.5 times greater odds of increased IBS symptoms, compared with rural residence (OR: 13.48, 95% CI 3.55-51.25, P value < .001). Moreover, patients who lost their job during the pandemic were 12.9 times more likely to have increased symptoms (OR: 12.89, 95% CI 1.84-90.15, P value = 0.01). A unit increase in patients age and beck anxiety inventory score was associated with 68% and 75% greater odds for increased IBS symptoms, respectively (OR: 1.68, 95% CI 1.12-2.53, P value = .012; OR: 1.75, 95% CI 1.08-2.84, P value = .024). Increasing anxiety is associated with increased IBS symptoms. Therefore, IBS patients should be screened for anxiety, and the role of psychiatric management of anxiety in the amelioration of IBS symptoms must be explored.

Sustainable radical approaches for cross electrophile coupling to synthesize trifluoromethyl- and allyl-substituted tert-alcohols.

Trifluoromethylated molecules have gained privileged recognition among the medicinal and pharmaceutical chemists. Sustainable photoredox- and electrochemical processes were employed to facilitate the relatively less explored radical cross-electrophile coupling to access trifluoromethyl- and allyl-substituted tert-alcohols. Reactions proceed through trifluoromethyl ketyl radical and allyl radical intermediates, which undergo challenging radical-radical cross-coupling. The developed transformations are mild and chemo-selective to give cross-coupled products and deliver a wide range of valuable trifluoromethyl- and allyl-containing tertiary alcohols. Both processes can also be applied for the synthesis of amine variant containing trifluoromethyl and allyl moiety, which is considered as amide bioisostere.

Organophotocatalytic Arene Functionalization: C-C and C-B Bond Formation.

Organophotocatalytic C-C and C-B bond formation reactions of aryl halides have been developed in the presence of an organophotosensitizer, 3,7-di([1,1'-biphenyl]-4-yl)-10-(4-(trifluoromethyl)phenyl)-10H-phenoxazine that has highly negative reduction potential at its photoexcited state. The developed reaction conditions are mild and allow the intermolecular C-C bond formation of the generated aryl radical with electron-rich (hetero)arenes and C-B bond formation with bis(pinacolato)diboron.