SYNTHESIS |
A new domino process transforms five components into a hexasubstituted benzene that resembles natural products with interesting biological activities. The process delivers seven chemical bonds and five elements of diversity from one pot. Authors accomplished this feat by developing conditions in which the three-component synthesis of an oxazole is compatible with two subsequent cycloaddition reactions. In domino processes, bond-forming transformations take place under the same reaction conditions, and subsequent transformations are the consequence of the functionality formed in the previous one. Simple to operate and giving good yields, the sequence authors developed is highly adaptable to diversity-oriented parallel synthesis. They have prepared a range of polyheterocycles with three different amines, three aldehydes, one isocyanoacetamide, two pentafluorophenyl 3-arylprop-2-ynoates, and three dienophiles as starting materials. Yields range from 32 to 67%.
|