RESUMO
A simple, efficient, and inexpensive procedure has been developed for the synthesis of 2,4,5-triaryl imidazoles by a three-component, one-pot condensation of benzyl, aldehydes, and ammonium acetate in refluxing ethanol without adding catalyst. The "catalyzed-by-itself" approach shows a new direction in green synthesis of the title products.
Assuntos
Química Verde/métodos , Imidazóis/síntese química , Acetatos/síntese química , Acetatos/química , Aldeídos/síntese química , Aldeídos/química , Química Verde/economia , Imidazóis/química , Estrutura MolecularRESUMO
A sequential three-component synthesis of functionalized benzisothiazoline-3-acetic acid 1,1-dioxides utilizing a domino Heck-aza-Michael pathway is reported. This one-pot procedure rapidly assembles functionalized benzylsulfonamides, which undergo a palladium-catalyzed, domino, Heck-aza-Michael transformation in an experimentally straightforward manner. This attractive protocol has been utilized to synthesize three combinatorial sublibraries (I-III) comprising a total of 95 compounds in high purities (> or =95% for 75 compounds), yield and quantities.
Assuntos
Acetatos/síntese química , Técnicas de Química Combinatória/métodos , Óxidos/síntese química , Bibliotecas de Moléculas Pequenas/síntese química , Tiazóis/química , Acetatos/química , Técnicas de Química Combinatória/economia , Óxidos/química , Bibliotecas de Moléculas Pequenas/química , Tiazóis/síntese químicaRESUMO
A simple, efficient and remotely operated synthesis apparatus for carrying out routine [(11)C]carboxylation, on-column and bubbling [(11)C]methylation was essential for reliable, day-to-day production of [(11)C]-labelled PET radiopharmaceuticals. We developed an in-house apparatus specifically applied to the synthesis of [(11)C]acetate, [(11)C]choline, [(11)C]methionine and 2-(4'-N-[(11)C]methylaminophenyl)-6-hydroxybenzothiazole ([(11)C]PIB), where high radiochemical purity (>or= 97%) and moderate radiochemical yields (18% for [(11)C]PIB, 41-55% for the others) could be achieved. These findings provided evidence that this was a fast, versatile and reliable apparatus suitable for a PET/CT centre with limited financial budget and hot cell space for synthesis of [(11)C]-labelled radiopharmaceuticals.