Novel technologies were developed and used for the synthesis and evaluation of new triazolopyridazine BRD9 inhibitors.

The synthesis of the aglycon of disciformycin, a new secondary metabolite from Pyxidicoccus fallax, is reported. The disciformycins are highly potent antibiotics including inhibitory activity towards methicillin‐ and vancomycin‐resistant Staphylococcus aureus. The stereocontrolled installation of the olefinic double bonds at C2–C3/C3–C4 and C12–C13, respectively, as well as the orthogonal differentiation of the oxy functionalities turned out to be key challenges of our approach.

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