An efficient kinetic resolution of racemic trans-2,3-aziridinyl alcohols is established via zinc catalyzed ring opening reactions with various amines as the nucleophiles. The directing effect of the hydroxyl group and the precise enantiodiscrimination by dinuclear zinc cooperative catalyst are the keys to success of high regioselectivity and enantioselectivity. A range of enantioenriched vicinal diamines and trans-2,3-aziridinyl alcohols were obtained in good yields with excellent ee values. To the best of our knowledge, this is the first example of directed enantioselective nucleophilic ring opening reactions of 2,3-aziridinyl alcohols.

Objective: We evaluated the efficacy and safety of transdermal preparations of Sinomenium acutum (SA) for rheumatoid arthritis (RA).Methods: Randomized controlled trials (RCTs) of SA transdermal preparations for RA were extracted from relevant databases and screened in accordance with the inclusion criteria. The Cochrane System Evaluation Manual (version 5.1.0) was used to assess the quality of the included trials. We used the Cochrane Review Manager (version 5.4) to conduct the meta-analysis.Results: Six trials comprising 436 patients (220 patients in the treatment group and 216 patients in the control group) were analyzed. The meta-analysis indicated that SA transdermal preparations in combination with disease-modifying antirheumatic drugs (DMARDs) enhanced the overall effect (odds ratio [OR] 3.97, 95% confidence interval [CI] [2.25,7.00], P<0.00001), decreased visual analogue scale (VAS) results (mean difference [MD] -0.64, 95% CI [-1.20, -0.09], P=0.02), decreased laboratory indexes including the erythrocyte sedimentation rate (ESR) (MD -4.36, 95% CI [-5.63, -3.08], P<0.00001) and C-reactive protein (CRP) (MD -3.6, 95% CI [ -3.99, -3.21, P<0.00001]), and decreased the Disease Activity Score-28 (DAS28) (MD -0.41, 95% CI [-0.78, -0.03], P=0.03). The results suggest that combination therapy did not shorten the duration of morning stiffness (DMS; standardized MD [SMD] -6.13, 95% CI [-17.33, 5.06], P=0.28) or reduce rheumatoid factor (RF) laboratory indexes (SMD -0.85; 95% CI [-2.19, 0.49], P=0.21). Only one study reported adverse reactions, and thus, it was difficult to determine whether adverse drug reactions in the combination therapy group were significantly different from those in the control group. Conclusion:We found that SA transdermal preparations combined with DMARDs may have greater clinical efficacy than DMARDs for RA. More well-designed and high-quality RCTs are required to verify the findings and determine whether transdermal preparations cause fewer adverse events.

We described herein a neoteric enantioselective cascade Michael/acyl transfer reaction of enynones and α-hydroxy aryl ketones catalyzed by dinuclear zinc cooperative catalysis. A series of structurally diverse chiral 1,5-dicarbonyl compounds were synthesized in good yields with excellent stereoselectivities. This strategy features broad substrate scope, high atom economy, as well as enynones as efficient electrophilic acyl transfer reagents in asymmetric cascade reactions for the first time.

The umpolung activity of hemiacetals serving as α-carbon nucleophiles has been reported via dinuclear zinc cooperative catalysis. This umpolung strategy has been applied to catalytic asymmetric tandem reactions of 1-tosylindoline-2,3-diols with β,γ-unsaturated-α-keto compounds, providing a broad series of structurally diverse tetrahydrofuran spiro­oxindoles and dihydrofurans, respectively. In addition, products could be transformed to quinazoline and quinoline derivatives.

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