Parallel synthesis of bis-heterocyclic isoxazolylmethyl-and isoxazolinylmethylpyrazoles

…, BA Lorsbach, TC Sparks, JC Fettinger…

Index: Meng, Liping; Lorsbach, Beth A.; Sparks, Thomas C.; Fettinger, James C.; Kurth, Mark J. Journal of Combinatorial Chemistry, 2010 , vol. 12, # 1 p. 129 - 136

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Citation Number: 18

Abstract

The solution-phase parallel synthesis of a 136-member library of isoxazol (in) e-CH2- pyrazoles is described. X-ray crystallographic structure determination verified the regioselectivities of the N-alkylation and nitrile oxide 1, 3-dipolar cycloaddition steps. The construction of these pharmaceutically relevant heterocycles on solid support under microwave irradiation is also demonstrated. The resulting library of drug-like compounds ...