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1. (WO2017039425) A METHOD FOR PREPARATION OF IBRUTINIB PRECURSOR

Pub. No.:    WO/2017/039425    International Application No.:    PCT/LV2015/000009
Publication Date: Fri Mar 10 00:59:59 CET 2017 International Filing Date: Sat Nov 14 00:59:59 CET 2015
IPC: C07D 487/04
A61K 31/519
A61P 35/00
Applicants: LATVIAN INSTITUTE OF ORGANIC SYNTHESIS
Inventors: LEBEDEVS, Antons
PONOMARJOVS, Jurijs
VARACEVA, Larisa
CERNAKS, Dmitrijs
CERNOBROVIJS, Aleksandrs
Title: A METHOD FOR PREPARATION OF IBRUTINIB PRECURSOR
Abstract:
A method for the preparation of ibrutinib's precursor, 3-(4-phenoxyphenyl)-1-((3R)-piperidin-3-il)-1H-pyrazolof [3,4-d]|pyrimidin-4-amine, involving arylation of N-protected 1-(piperidin-3-yl)pyrazolo[3,4-d]pyrimidin-4-amine in the presence of palladium catalyst, nitrogen-containing ligand, and base, with subsequent removal of the protecting groups by known methods, is reported. (Formula (II))