An efficient and practical protocol for the protection of various structurally and electronically divergent aryl and aliphatic amines using (Boc)2O in the presence of a catalytic amount of molecular iodine (10 mol %) under solvent-free conditions at ambient temperature is presented.
Zn-proline (5 mol%) performs as a novel water-soluble and recyclable Lewis acid catalyst for the selective synthesis of 1,2-disubstituted benzimidazoles from wide range of substituted o-phenylenediamines and aldehydes in moderate to excellent isolated yields (42-92%) using water as solvent at ambient temperature.
A facile, efficient, concise, cost-effective, and scalable synthesis of thalidomide in high overall yield (55%) is presented. Treatment of Boc-protected L-glutamic acid diester via Na/ liquid (liq.) NH 3 (-33 °C) mediated cyclization methodology produces a corresponding glutarimide ring which was subsequently condensed with phthalic anhydride in the presence of glacial acetic acid to afford thalidomide.
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