Automated peptide and oligonucleotide synthesizers enabled a revolution in molecular biology and helped pave the way to modern synthetic biology. Similarly, fully automated synthetic chemistry could herald a new wave of innovation in biology and materials sciences by greatly facilitating access to known and novel molecules. Here, we report on an automated multistep chemical synthesizer, AutoSyn, that makes milligram-to-gram-scale amounts of virtually any drug-like small molecule in a matter of hours and demonstrate its versatility with the synthesis of ten known drugs. Of the FDA-approved small-molecule drugs for which we were able to compute a synthetic route, 87% are predicted to be synthesizable on AutoSyn. Moreover, AutoSyn enables digital synthesis protocols that ensure the reproducibility and transferability of synthesis protocols from one lab to another.
A novel series of nitrofuran containing spiropyrrolidines has been synthesized with high regioselectivity in moderate to excellent yields via 1,3‐dipolar cycloaddition reaction of azomethine ylides with various substituted chalcones.
A new class of functionalized nitrothiophene containing spirropyrrolidines has been synthesized with high regioselectivity in moderate to excellent yields via microwave assisted solvent‐free‐three component 1,3‐dipolar cycloaddition reaction of in situ generated azomethineylides with various substituted chalcones as dipolarophiles. The structures of the newly synthesized compounds were established by analytical and spectral analysis. The product yields were slightly improved and reaction times were reduced to a great extent under microwave condition.
A new class of functionalized furan and 5-(p-chlorophenyl)furan containing spiropyrrolidines has been synthesized in moderate to excellent yields by the one-pot, three-component 1,3-dipolar cycloaddition reaction of in situ generated azomethine ylides with various furan/aryl furan-substituted chalcones as dipolarophiles. The effect of electron deficient substituents at the fifth position of the furan ring in the chalcone on the regiochemistry of the cycloaddition formed was studied. The structures of the newly synthesized cycloaddicts were proved by analytical and spectral data.
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