An Organocatalysis Based Carbocyclic Spiroindoline Synthesis Enables Facile Structure–Activity Relationship (SAR) Study at C2 Position

An asymmetric synthesis of carbocyclic spiroindoline by sequential Michael reaction and [3 + 2]-cycloaddition is described. This protocol demonstrates excellent enantio- and diastereoselectivity with broad functional group tolerance. A diverse range of spiroindolines were prepared by this approach, and the products served as ideal substrates for C2 derivatization

A Highly Stereoselective and Scalable Synthesis of l‑allo-Enduracididine

A highly stereoselective and scalable synthesis of l-allo-enduracididine from hydroxyproline derivative is described. Pyrrolidine oxidation and reductive ring opening are the key steps in the synthesis. Compared to previously reported approaches, the current route affords l-allo-enduracididine in 10 steps from <b>3</b> in 31% overall yield with >50:1 diastereoselectivity

Active sp³ C–H Bond Oxidation Initiated sp³–sp² Consecutive C–H Functionalization of <i>N</i>‑Arylglycine Amides: Construction of Isatins

In the presence of catalytic triarylamine radical cation, an sp³–sp² consecutive C–H functionalization of <i>N</i>-arylglycine amides was achieved, providing a series of isatin derivatives in high yields. In this transformation, the initial aerobic oxidation of the relatively active sp³ C–H bonds triggered the following intramolecular cyclization, in which the aniline group was employed as a removable auxiliary group to enable the consecutive process

Iridium(III)-Catalyzed Direct Arylation of C–H Bonds with Diaryliodonium Salts

By developing a new Ir­(III)-catalyzed C–C cross-coupling, a versatile method for direct arylation of sp² and sp³ C–H bonds in ketoximes, nitrogen-containing heterocycles, various arenes, and olefins has been established. The key to this arylation depends on the appropriate choice of catalyst and the use of diaryliodonium triflate salts as the coupling partners. This transformation has good functional group compatibility and can serve as a powerful synthetic tool for late-stage C–H arylation of complex compounds. Mechanistic studies by density functional theory calculations suggested that the sp³ C–H activation was realized by a triflate-involved concerted metalation–deprotonation process, and the following oxidation of Ir­(III) to Ir­(V) is the most favorable when a bistriflimide is contained in the diaryliodonium salt. Calculations indicated that both steps are enabled by initial anion exchange between the reactant complexes

Lewis score in diabetic patients with or without different types of complications.

<p>Lewis score in diabetic patients with or without different types of complications.</p

Correlation test for Lewis score.

<p>Correlation test for Lewis score.</p

C–H Activation Relay (CHAR): An Efficient Construction of Isatin Skeleton by Aerobic Oxidation of Glycine Esters

Directed by the strategy of C–H activation relay (CHAR), an efficient construction of isatin skeleton was developed through catalytic oxidation of glycine esters. The mechanistic study reveals that the oxidation of the relatively active C–H bonds initiated the followed activation of remote and inert C–H bonds, and an intramolecular 1,6-hydrogen shift was involved as a key step

Iridium(III)-Catalyzed Direct Arylation of C–H Bonds with Diaryliodonium Salts

By developing a new Ir­(III)-catalyzed C–C cross-coupling, a versatile method for direct arylation of sp² and sp³ C–H bonds in ketoximes, nitrogen-containing heterocycles, various arenes, and olefins has been established. The key to this arylation depends on the appropriate choice of catalyst and the use of diaryliodonium triflate salts as the coupling partners. This transformation has good functional group compatibility and can serve as a powerful synthetic tool for late-stage C–H arylation of complex compounds. Mechanistic studies by density functional theory calculations suggested that the sp³ C–H activation was realized by a triflate-involved concerted metalation–deprotonation process, and the following oxidation of Ir­(III) to Ir­(V) is the most favorable when a bistriflimide is contained in the diaryliodonium salt. Calculations indicated that both steps are enabled by initial anion exchange between the reactant complexes

Association of drinking pattern with risk of coronary heart disease incidence in the middle-aged and older Chinese men: Results from the Dongfeng-Tongji cohort

<div><p>Background</p><p>Epidemiologic studies have found that moderate alcohol consumption was associated with a decreased risk of coronary heart disease (CHD) incidence. Nevertheless, whether the drinking pattern is associated with CHD incidence still remains inconclusive.</p><p>Methods</p><p>We included 8,469 Chinese men aged 45–81 years, who were free of CHD, stroke, or cancer at baseline from Dongfeng-Tongji cohort. A semi-structured questionnaire was used to collect information on alcohol consumption and other covariates. Cox proportional hazard regression model was applied to estimate the multivariable-adjusted hazard rations (HRs) and 95% confidence intervals (95% CIs).</p><p>Results</p><p>During an average of 4.36 years of follow-up, we identified 959 incident CHD events. Compared with non-drinkers, the multivariable-adjusted HR (95% CI) of CHD incidence was 0.84 (0.71–0.98) in current drinkers. With respect to drinking pattern, men who consumed 20.01–40 grams ethanol once a time had a 24% lower risk of incident CHD (HR = 0.76, 95% CI = 0.62, 0.94) compared with non-drinkers. The adjusted HRs (95% CI) of CHD incidence were 0.80 (0.65, 0.99), 1.02 (0.84, 1.22), and 0.75 (0.59–0.96) in subjects who consumed 0.01–10, 10.01–30, and > 30 grams ethanol per day, respectively. Participants who consumed 20.01–40 grams ethanol per time with less than 5 times per week had the lowest risk of CHD incidence (HR = 0.73, 95% CI = 0.52, 0.96). No significant associations were observed between type or frequency of alcohol consumption and CHD incidence.</p><p>Conclusions</p><p>Drinking was associated with a lower risk of CHD incidence in middle-aged and older Chinese men and moderate quantity of ethanol amounts once a time with lower frequency could been considered as a healthy drinking pattern, which might modify the relationship between alcohol consumption and incident CHD.</p></div

Adjusted HRs (95% CIs) for incident CHD according to type of alcohol consumption.

<p>Adjusted HRs (95% CIs) for incident CHD according to type of alcohol consumption.</p