Decarboxylation O 0296Microwave-Assisted Decarboxylation of Bicyclic 2-Pyridone Scaffolds and Identification of Aβ-Peptide Aggregation Inhibitors. -The lithium salts of pyridone derivatives (Ia) and (Ib) are found to inhibit the amyloid formation of the Alzheimer Aβ(1-40) peptide. -(AABERG, V.; NORMAN, F.; CHORELL, E.; WESTERMARK, A.; OLOFSSON, A.; SAUER-ERIKSSON, A. E.; ALMQUIST*, F.; Org. Biomol. Chem. 3 (2005) 15, 2817-2823; Dep. Chem., Org. Chem., Umea Univ., S-901 87 Umea, Swed.; Eng.) -Nuesgen 49-055

ChemInform is a weekly Abstracting Service, delivering concise information at a glance that was extracted from about 200 leading journals. To access a ChemInform Abstract, please click on HTML or PDF.

Fused pyridine derivatives R 0450Microwave-Assisted Synthesis of Highly Substituted Aminomethylated 2-Pyridones. -Aminomethyl pyridones (IV) are prepared by cyanodehalogenation of bromides (I) and subsequent reduction of the nitriles (III) by borane dimethyl sulfide. In both steps microwave irradiation (MW) is applied. Unfortunately, a substantial loss in enantiomeric purity is observed for both steps leading to compound (IVb). To prepare tertiary aminomethyl-substituted pyridones, Mannich reaction of pyridones (V) with preformed iminium salts is accomplished under MW. In the case of pyridone (Vb), only little loss of enantiopurity of product (IXb) occurs. -(PEMBERTON, N.; AABERG, V.; ALMSTEDT, H.; WESTERMARK, A.; ALMQVIST*, F.; J. Org. Chem. 69 (2004) 23, 7830-7835; Dep. Chem., Org. Chem., Umea Univ., S-901 87 Umea, Swed.; Eng.) -Klein 12-156