1802929-43-6Relevant academic research and scientific papers
Discovery of the Irreversible Covalent FGFR Inhibitor 8-(3-(4-Acryloylpiperazin-1-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2-(methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one (PRN1371) for the Treatment of Solid Tumors
Brameld, Ken A.,Owens, Timothy D.,Verner, Erik,Venetsanakos, Eleni,Bradshaw, J. Michael,Phan, Vernon T.,Tam, Danny,Leung, Kwan,Shu, Jin,Lastant, Jacob,Loughhead, David G.,Ton, Tony,Karr, Dane E.,Gerritsen, Mary E.,Goldstein, David M.,Funk, Jens Oliver
, p. 6516 - 6527 (2017)
Aberrant signaling of the FGF/FGFR pathway occurs frequently in cancers and is an oncogenic driver in many solid tumors. Clinical validation of FGFR as a therapeutic target has been demonstrated in bladder, liver, lung, breast, and gastric cancers. Our go
Synthetic route of generic FGFR covalent inhibitor PRN1371
-
, (2021/01/11)
The invention relates to a synthetic route of a generic FGFR covalent inhibitor PRN1371, and belongs to the field of medicinal chemistry. The synthetic route steps of the PRN1371 comprise 11 steps, purification of a product can be achieved through simple operation of various intermediates in the aftertreatment process, the problems that the product is difficult to separate, the purification operation yield is low and the like are solved, and industrial production is facilitated. The invention aims to provide a synthetic route of the FGFR irreversible covalent inhibitor PRN1371, and the methodhas the advantages of few synthesis steps, simple operation, high yield, reduction of the production cost, and provision of a new synthesis idea for the industrial production of PRN1371.
PROCESSES FOR PREPARING AN FGFR INHIBITOR
-
, (2017/03/17)
Disclosed herein are processes for preparing 8-(3-(4-acryloylpiperazin-l-yl)propyl)-6-(2,6-dichloro-3,5-dimethoxyphenyl)-2- (methylamino)pyrido[2,3-d]pyrimidin-7(8H)-one and FGFR inhibitor, as well as polymorphs and/or salt forms thereof.
