ƴ-Selective directed catalytic asymmetric hydroboration of 1,1-disubstituted alkenes

Directed catalytic asymmetric hydroborations of 1,1-disubstituted alkenes afford ƴ -dioxaborato amides and esters in high enantiomeric purity (90–95% ee)

Acute coronary syndrome: What do patients know?

Background: The effectiveness of therapy for an acute coronary syndrome (ACS) is dependent on patients' quick decision to seek treatment. We surveyed patients' level of knowledge about heart disease and self-perceived risk for a future acute myocardial infarction (AMI) in patients with documented ischemic heart disease. Methods: Patients (N = 3522) had a mean age of 67 years, 68% were male, and all had a history of AMI or invasive cardiac procedure for ischemic heart disease. Data were gathered using a 26-item instrument focusing on ACS symptoms and appropriate steps to seeking treatment. Patients were asked to identify their level of perceived risk for a future AMI. Results: Forty-six percent of patients had low knowledge levels (ie, <70% of answers were correct). The mean score was 71%. Higher knowledge scores were significantly related to female sex (P = .001), younger age (P = .001), higher education (P = .001), participation in cardiac rehabilitation (P = .001), and receiving care by a cardiologist rather than an internist or general practitioner (P = .005). Clinical history (eg, AMI [P = .24] and cardiac surgery [P = .38]) were not significant predictors of knowledge. Most (57%) identified themselves as being at higher risk for a future AMI compared with an age-matched individual without heart disease with 1 exception. Namely, patients who had undergone coronary artery bypass surgery felt significantly less vulnerable for a future AMI than other individuals of the same age. Conclusions: Even following diagnosis of ACS and numerous interactions with physicians and other health care professionals, knowledge about ACS symptoms and treatment on the part of patients with cardiac disease remains poor. Patients require continued reinforcement about the nature of cardiac symptoms, the benefits of early treatment, and their risk status. ©2008 American Medical Association. All rights reserved

Enantiospecific sp(2)-sp(3) coupling of secondary and tertiary boronic esters

The cross-coupling of boronic acids and related derivatives with sp² electrophiles (the Suzuki–Miyaura reaction) is one of the most powerful C–C bond formation reactions in synthesis, with applications that span pharmaceuticals, agrochemicals and high-tech materials. Despite the breadth of its utility, the scope of this Nobel prize-winning reaction is rather limited when applied to aliphatic boronic esters. Primary organoboron reagents work well, but secondary and tertiary boronic esters do not (apart from a few specific and isolated examples). Through an alternative strategy, which does not involve using transition metals, we have discovered that enantioenriched secondary and tertiary boronic esters can be coupled to electron-rich aromatics with essentially complete enantiospecificity. As the enantioenriched boronic esters are easily accessible, this reaction should find considerable application, particularly in the pharmaceutical industry where there is growing awareness of the importance of, and greater clinical success in, creating biomolecules with three-dimensional architectures

Identification of isoflavone derivatives as effective anticryptosporidial agents in vitro and in vivo.

We report the preparation and antiparasitic activity in vitro and in vivo of a series of isoflavone derivatives related to genistein. These analogues retain the 5,7-dihydroxyisoflavone core of genistein: direct genistein analogues (2-H isoflavones), 2-carboethoxy isoflavones, and the precursor deoxybenzoins were all evaluated. Excellent in vitro activity against Cryptosporidium parvum was observed for both classes of isoflavones in cell cultures, and the lead compound 19, RM6427, shows high in vivo efficacy against an experimental infection

Chemical examination of Anacardium occidentale. Isolation and structure determination of a novel biflavonoid-C-glycoside

A new biflavonoid-C-glycoside named occidentoside, also the known (-)salipurposide and β-sitosterol, have been isolated from the nut shells of Anacardium occidentale L. (Anacardiaceae). The structure of occidentoside has been established as tetrahydroninokiflavone-C-glucoside (III) from spectral and chemical evidence. This is the first biflavonoid to occur with one flavanone and one chalcone unit and also the first C-glycoside in the biflavonoid series. Identification of (-)salipurposide is also reported since it has been isolated for the first time from cashew nut shells