Fig. 3: Combinatorial reactivity shows potential for Direct-To-Biology (D2B) screenings.

a Experimental attributes, such as the use of DMSO as solvent and resulting homogeneous solution after filtration, are ideal for D2B screenings. b Combinatorial experiments revealed that 60% of reactions generated product in greater than 70% yield, an excellent range for D2B approaches. Reactions were carried out with 1.0 equiv Fa-f, 1.0 equiv of Ha-f in DMSO-d6. Yields were measured by 1H NMR with an internal standard and characterization was carried out by NMR and MS. NMR nuclear magnetic resonance, MS mass spectrometry.