MRTX0902, a novel SOS1 inhibitor, is currently being evaluated in phase I trials for the treatment of cancer. The complexity molecule, which contains pyrido[3,4-d]pyridazine core and chiral amine moiety, makes it challenging target to prepare on multi-kilogram scale support clinical development studies. An efficient scalable synthesis key intermediate 4-methyl-7-morpholinopyrido[3,4-d]pyridazin...

Coupling of compound 1 with diazotized aromatic amines in ethanol afforded the arylhydrazones 3a,b. Fusion of 3a,b with active methylene derivatives 4a,b afforded the pyridazine derivatives 6a–d. Also, when compounds 6b,c were reacted with elemental sulphur afforded the thienopyridazine derivatives 7a,b. Treatment of compound 8 with hydrazine hydrate produced pyrazolopyridine derivative 9. Pyri...

In the title centrosymmetric complex, [Zn(C(7)H(5)N(2)O(4))(2)(H(2)O)(2)]·2H(2)O, the Zn(II) ion is coordinated in a trans mode by two symmetry-related bis-chelating 6-methoxycarbonyl-pyridazine-3-carboxyl-ate ligands via N and O atoms, and by two aqua ligand O atoms in axial positions, in a slightly distorted octa-hedral environment. In the crystal structure, complex mol-ecules are linked by i...

Aiming for the synthesis of new heterocyclic compounds containing a sulfonamido moiety suitable for use as antibacterial agents, the precursor ethyl {[4-N-(4,6-dimethylpyrimidin-2-yl)sulfamoyl]phenylazo}cyanoacetate was reacted with a variety of active methylene compounds producing pyran, pyridine and pyridazine derivatives. Also, the reactivity of the precursor hydrazone towards hydrazine deri...