A novel approach to 2-substituted-2-(dimethoxyphosphoryl)-pyrrolidines 7a−7o and 9a−9r has been developed, which features a TMSOTf-mediated one-pot intramolecular cyclization and phosphonylation of substituted tert-butyl 4oxobutylcarbamates. The major advantages of this method include simple operation under mild reaction conditions, the use of cheap Lewis acid, and good to excellent yields with high diastereoselectivities (dr up to 99:1).

Simvastatin may inhibit VSMC phenotype modulation and proliferation by downregulating the expression of PCNA and upregulating that of p27kip1.

Convenient and stereoselective methods for the preparation of 2-deoxy-d-glucose and purine 2-deoxy-α-d-glucopyranonucleosides were developed. Halogen-mediated O-glycosidation of d-glucal by bromine in MeOH followed by reductive removal of the halo group and hydrolysis of methoxy group by zinc in saturated aqueous sodium dihydrogen phosphate gave 2-deoxy-d-glucose. Treatment of 3,4,6-tri-O-acetyl-d-glucal with IBr and 2,6-dichloropurine based on haloetherification and subsequent reductive removal of iodine and deprotection allowed the isolation of purin-9-yl 2-deoxy-α-d-glucopyranonucleoside. Preparation of several purin-9-yl 2-deoxy-α-d-glucopyranoside derivatives is also reported. Their configuration was confirmed by single crystal X-ray analysis of the key intermediate 2,6-dichloro-9-(2-iodo-2-deoxy-α-d-glucopyranosyl)purine.

ObjectiveTo investigate differences in clinical and angiographic outcomes between patients with acute myocardial infarction with red and white thrombi.MethodsA total of 137 patients with ST-segment elevation myocardial infarction undergoing primary percutaneous coronary interventions were included. Thrombus material was classified as white or red based on its pathology. Information on characteristics of thrombi was available for 97 (70.8%) patients.ResultsThe total ischaemic time was significantly longer in the red thrombus group compared with the white thrombus group. The incidence of major adverse cardiovascular events in hospital was higher in the red thrombus group than in the white thrombus group (15.6% vs 0%). Multivariable logistic analysis showed that the total ischaemic time was the only predictor of thrombus composition (odds ratio 1.353; 95% confidence interval 1.003, 1.826).ConclusionRed thrombi were present in nearly two-thirds of cases, and were associated with a longer ischaemic time and higher incidence of major adverse cardiovascular events in hospital.

A catalyzed process to 4,6-substituted 3,4-dihydro-1,3-oxazin-2-one skeleton has been developed through cycloaddition of in situ generated acyliminium intermediates with alkynes. A range of chain N,O-acetals and terminal alkynes were amenable...

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An asymmetric approach to access 2‐substituted isoindolin‐1‐ones 9–11 was developed through TiCl4‐mediated addition‐chlorination of N,O‐acetals 7 a–7 c with terminal alkynes 8. A range of substrates were amenable to this transformation, and the desired substituted isoindolin‐1‐ones were obtained in moderate to good yields with moderate diastereoselectivities.

A novel approach to skipped dienes has been developed through the TMSOTf-mediated one-pot addition-substitution of olefins 2a, 2f-2g with imines 1a-1g, and a series of aryl substituted skipped dienes 3aa-3gf...