Toward a high-throughput screening: Dynamic Combinatorial Chemistry (DCC)

When we use a classical synthesis, we make a reaction between one compound A on one compound B in the goal of obtain an only product A-B. So: A+B give A-B. On the contrary, combinatorial synthesis based on reversible bonds which generated a library by the combinaison of building blocks:

A1                          B1

A2                          B2

A3                          B3

m compounds         n compounds

then, by an in situ mixture, we obtain all the combinaisons:

A1-B1  A1-B2  A1-B3 

A2-B1  A2-B2  A2-B3

A3-B1  A3-B2  A3-B3

If an activity is detected we need to use an efficient means to discover which compound produce this activity. Consequently, if we take the example of a large librarie of catalysts, we use the “iterative deconvolution against a target reaction” to find the catalyst which contains the best assembly.

It’s crucial to use Reversible covalent bonds, reaction of transesterification, imine, boronic ester, disulfide formation, etc

DCC makes use these reversible connections between the initial building blocks. This approach is in the fiel of supramolecular chemistry.

Lead References: Lehn, J.-M; Eliseev, A. V. Science, 2001, 291, 2331-2332

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