A Prospective Single-arm Open-label Study of Baclofen and Bupropion SR Combination Therapy for Smoking Cessation
Conclusions: Combination of baclofen and bupropion SR seems safe and well tolerated with preliminary efficacy for smoking cessation comparing favorably with current first-line smoking cessation aids. The combination of baclofen and bupropion SR may provide an additional treatment option to varenicline or bupropion SR monotherapy. (Health Canada Clinical Trial Registration Control number: 105226). (Source: Addictive Disorders and Their Treatment)
Hyphenating the curtius rearrangement with Morita-Baylis-Hillman adducts: synthesis of biologically active acyloins and vicinal aminoalcohols
Using Morita-Baylis-Hillman adducts as substrates, the Curtius rearrangement was performed in a sequence that allowed the synthesis of several hydroxy-ketones (acyloins) with great structural diversity and in good overall yields. These acyloins in turn were easily transformed into 1,2-anti aminoalcohols through a highly diastereoselective reductive amination step. The synthetic utility of these approaches was exemplified by performing the syntheses of (±)-bupropion, a drug used to treat the abstinence syndrome of smoker and (±)-spisulosine, a potent anti-tumoral compound originally isolated from a marine source.Um rearranjo de Curtius, utilizando adutos de Morita-Baylis-Hillman como substrato, foi realizado em uma sequência que permitiu a síntese de várias hidroxi-cetonas (aciloínas)...
