Abstract
MRTX0902, a novel SOS1 inhibitor, is currently being evaluated in phase I trials for the treatment of cancer. The complexity of the molecule containing a pyrido[3,4-d]pyridazine core and a chiral amine moiety makes it a challenging target to prepare on multi-kilogram scale to support clinical development studies. An efficient and scalable synthesis to the key intermediate, 4-methyl-7-morpholinopyrido[3,4-d]pyridazin-1(2H)-one and a much improved end-game to MRTX0902 was developed.
Supplementary materials
Title
Supporting Information containing NMR spectra
Description
Supporting Information containing NMR spectra (1H and 13C) for the compounds in Scheme 6
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