Alkyl radicals generated via an acridine photocatalyzed decarboxylation reaction of feedstock carboxylic acids engage with a range of cyclic imine-BF complexes to provide α-functionalized azacycles in an operationally simple process. A three-component variant of this transformation incorporating [1.1.
View Article and Find Full Text PDFSynthesis (Stuttg)
August 2023
Secondary alicyclic amines are converted to their corresponding ring-fused imidazoles in a simple procedure consisting of oxidative imine formation followed by a van Leusen reaction. Amines with an existing α-substituent undergo regioselective ring-fusion at the α'-position. This method was utilized in a synthesis of fadrozole.
View Article and Find Full Text PDFA new strategy to access α-functionalized alicyclic amines via their corresponding imine-BF complexes is reported. Isolable imine-BF complexes, readily prepared via dehydrohalogenation of N-bromoamines in a base-promoted/18-crown-6 catalyzed process followed by addition of boron trifluoride etherate, undergo reactions with a wide range of organometallic nucleophiles to afford α-functionalized azacycles. Organozinc and organomagnesium nucleophiles add at ambient temperatures, obviating the need for cryogenic conditions.
View Article and Find Full Text PDFWe establish a synthetically convenient method to degrade polyacrylate homopolymers. Carboxylic acids are installed along the polymer backbone by partial hydrolysis of the ester side chains, and then, in a one-pot sequential procedure, the carboxylic acids are converted into alkenes and oxidatively cleaved. This process enables the robustness and properties of polyacrylates to be maintained during their usable lifetime.
View Article and Find Full Text PDFMod Rheumatol Case Rep
June 2022
Takayasu arteritis (TA) is a large-vessel vasculitis most commonly affecting women of childbearing age. The disease process is usually slow and smoldering, presenting over months to years. Digital gangrene is an uncommon manifestation of TA because of the formation of good collateral circulation.
View Article and Find Full Text PDFObjective: To develop and validate a prognostic nomogram for predicting the probability of 12-month progression-free survival (PFS) for patients receiving first-line pazopanib for advanced renal cell carcinoma (RCC).
Methods: Statistical modeling was performed with data from 557 pazopanib-treated patients in the phase 3 COMPARZ trial. A multivariable Cox model was fit using known prognostic indicators.
Background: Topotecan is currently the only US Federal Drug Administration (FDA)-approved drug for second-line treatment of relapsed small-cell lung cancer (SCLC). We investigated the efficacy and safety of a novel topotecan-bevacizumab combination in treating relapsed SCLC.
Patients And Methods: Each 21-day treatment cycle consisted of bevacizumab (15 mg/kg) administration on day 1 and oral topotecan (2.