In step 3 (Figure ), the effect of a series of 46 additives on reaction performance was evaluated (Table ). The additives were chosen as a means of representing functional groups commonly present in druglike molecules. In terms of solvent effect, only minimal differences in performance between NMP (top bars) and DCE (bottom bars) were observed. To our delight, out of 47 modified conditions, 35 had no effect on the reaction outcome. Notably, excess water was well tolerated for the catalytic conditions used here, a feature important for use of reagents without prior drying. In terms of reagent and functional group tolerance the following insights were gained: 1) the presence of DMSO has a negative effect on the reaction outcome, while other commonly used polar and/or protic solvents are well tolerated. This observation is in accordance to similar studies. 2) The majority of polar functional groups commonly present in drug-like molecules were well tolerated. This includes the ether, alcohol, phenol, aldehyde, ketone, carboxylic acid, ester, primary and secondary amides, urea, Weinreb amide and sulfonamides. The same was observed with functional groups commonly present in cross-coupling reagents, such as aliphatic and aromatic halides and aryl-Bpin group.