The pseudo-multicomponent reaction between propargyl amine, an aldehyde and an electron-deficient alkene is described. The C-H activation takes place thermally and allows to obtain cicloadducts in very good yields and...

The synthesis of the complex spiro{pyrrolidine‐3,1′‐pyrrolo[3,4‐c]pyrrole} skeleton under mild conditions is presented. The order of addition of a primary amine, two equivalents of the corresponding maleimide and, finally, the aldehyde is of a paramount importance to obtain these final compounds in very high yields. The mechanism was studied by performing very simple tests, the Michael type addition of the amine onto the maleimide being the key step. Interestingly, the hybrid scaffold was prepared by sequential addition of two different maleimides. In addition, a more interesting architecture was prepared through a metathesis reaction between allylic residues bonded in the molecule precursor.

A synthesis of new-to-nature aza-iridoids via ynamides is presented. ZrCl 4 proved to be the best acid to perform this transformation. Various ynamides were accommodated, and seco-iridoids could be obtained as well. Aza-iridoids were infiltrated into leaves of Scrophularia Nodosa, an iridoid-producing plant species. High-resolution mass spectrometry coupled to computational metabolomic approaches was employed for the detection of aza-iridoid bioconversion products.

The synthesis of 4-arylthiazol-2(3H)-ones is reported employing a novel and mild methodology using benign solvents. In a second objective the multicomponent preparation of 5,5’-methylenebis[4-arylthiazol-2(3H)-ones] is described following the same strategy. The analysis of the mechanism is also studied and confirmed using chemical tests.