The palladium-catalyzed coupling of an enolate with an ortho-functionalized aryl halide (an α-arylation) furnishes a protected 1,5-dicarbonyl moiety that can be cyclized to an isoquinoline with a source of ammonia. This fully regioselective synthetic route tolerates a wide range of substituents, including those that give rise to the traditionally difficult to access electron-deficient isoquinoline skeletons. These two synthetic operations can be combined to give a three-component, one-pot isoquinoline synthesis.
View Article and Find Full Text PDFProc Natl Acad Sci U S A
July 2012
The utilization of sequential palladium-catalyzed α-arylation and cyclization reactions provides a general approach to an array of isoquinolines and their corresponding N-oxides. This methodology allows the convergent combination of readily available precursors in a regioselective manner and in excellent overall yields. This powerful route to polysubstituted isoquinolines, which is not limited to electron rich moieties, also allows rapid access to analogues of biologically active compounds.
View Article and Find Full Text PDFNeurourol Urodyn
September 2008
Diabetes mellitus (DM) has reached epidemic proportions world wide. Many chronic complications of DM, including neuropathy, retinopathy and nephropathy, have been well studied and although urologic complications have been recognized since 1935, little is known about DM as a pathophysiological risk factor for development of lower urinary tract symptoms (LUTS) in women. Diabetic nephropathy, a life-threatening condition, has received considerable attention in the last few years.
View Article and Find Full Text PDFAims: To assess the safety and efficacy of rosiglitazone and insulin treatment in combination in poorly controlled insulin-treated type 2 diabetes mellitus (T2DM) patient.
Method: In this prospective, open-labelled, nonrandomised study, rosiglitazone was added to the insulin therapy in T2DM patients with baseline HbA1c>or=7.5%.