ACS Combinatorial Science 2012-02-13

Efficient one-pot, three-component synthesis of a library of pyrrolo[1,2-c]pyrimidine derivatives.

Emilian Georgescu, Florentina Georgescu, Marcel M Popa, Constantin Draghici, Laszlo Tarko, Florea Dumitrascu

文献索引：ACS Comb. Sci. 14(2) , 101-7, (2012)

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摘要

Herein is reported a simple and efficient one-pot three-component synthesis of pyrrolo[1,2-c]pyrimidine derivatives starting from various substituted pyrimidines, 2-bromoacetophenones, and electron deficient alkynes in epoxides acting both as reaction medium and HBr scavanger. This method proved to be very lucrative and avoids formation of ylide inactivation products. The synthesis represents an environmentally benign alternative to classical methods. The new library of compounds was briefly characterized regarding the improved Lipinski rule to asses the potential drug-likeness of the compounds. The majority of compounds are statisfing the Lipinski rule.