SYNTHESIS OF SUBSTITUTED 1H-PYRAZOLO[3,4-D]PYRIMIDINES

摘要

The present invention refers to the synthesis and intermediates of substituted bicyclic compounds by using a central 1H- pyrazolo[3,4-d]pyrimidine of formula (I), which is assembled starting from 4,6-dichloropyrimidine carboxylic acid. The invention in particular refers to the synthesis of the Bruton's tyrosine kinase (Btk) inhibitor 1-((R)-3-(4-amino-3-(4-phenoxyphenyl)-1H-pyrazolo[3,4-d]pyrimidin-1-yl)piperidin-l-yl)prop-2-en-l-one(ibrutinib) and its synthesis intermediates.