A flexible strategy for the regiocontrolled synthesis of pyrazolo[1,5-a]pyrazines
作者： Peter J. Lindsay-Scott , Natalie G. Charlesworth , Alexandru Grozavu
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摘要: A four-step protocol for the synthesis of pyrazolo[1,5-a]pyrazines has been developed. Commercially available pyrazoles were alkylated and formylated in a regiocontrolled manner to give pyrazole-5-aldehydes bearing 2,2-dialkoxyethyl substitution on N-1. Efficient conditions subsequent deprotection cyclization these intermediates allowed access with multiple patterns. The versatility pyrazole-5-aldehyde was further demonstrated through double-reductive amination sequence 4,5,6,7-tetrahydropyrazolo[1,5-a]pyrazines.
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