Artificial macrocycles recently became popular as a novel search ground for drug discovery. As opposed to their natural twins, artificial macrocycles promise to have better control on synthesisability and control over their physicochemical properties resulting in drug-like properties. Very few synthetic methods allow for the convergent, fast but diverse access to large macrocycles chemical space. Here we will review multicomponent reaction technology with a focus on our work to access artificial macrocycles with potential biological activity. While there seems to be a MW cut-off of 1000 Dalton for passive membrane transportation, there is also indication that specifically the macrocyclic space between 500 and 1000 Dalton is virtually unexplored but holds promise to harbour a large number of macrocycles with drug-like ADMET properties and therefore represents a vast opportunity for those prepared to venture into new territories of drug discovery. In our laboratory novel strategies are elaborated to synthetically access specifically the space of 500 to 1000 Dalton using convergent chemistries including MCR.

Short and efficient access to very large non-peptidic macrocyclic space and applications to difficult targets

255th National Meeting (2018)

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