Liquid-phase synthesis of combinatorial libraries based on 7-trifluoromethyl-substituted pyrazolo[1,5-a]pyrimidine scaffold |
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Authors: | Dalinger Igor L Vatsadse Irina A Shevelev Svyatoslav A Ivachtchenko Alexandre V |
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Institution: | Zelinski Institute of Organic Chemistry, Russian Academy of Sciences, Leninsky prospekt, 47, 119991, Moscow, Russian Federation. |
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Abstract: | The parallel solution-phase synthesis of more than 2200 7-trifluoromethyl-substituted pyrazolo1,5-a]pyrimidine and 4,5,6,7-tetrahydropyrazolo1,5-a]pyrimidine carboxamides on a 50-100-mg scale has been accomplished. Key reactions include assembly of the pyrazolo1,5-a]pyrimidine ring by condensation of 5-aminopyrazole derivatives with the corresponding trifluoromethyl-beta-diketones. The libraries from libraries were then obtained in good yields and purities using solution-phase acylation and reduction methodologies. Simple manual techniques for parallel reactions using special CombiSyn synthesizers were coupled with easy purification procedures (crystallization from the reaction mixtures) to give high-purity final products. The scope and limitations of the developed approach are discussed. |
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