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Chapter 6
Synthesis of benzodiazepines
Recently, Joshua et al. 58 has reported the synthesis of saturated 1,4-
benzodiazepines and 1,4-benzodiazepin-5-ones (Figure-16) via Pd-catalyzed
carboamination reactions using sodium tert-butoxide base and xylene as a solvent at
refluxing condition.
Figure-16
Veena Yadav et al. 59 has developed an efficient microwave assisted protocol
for the exclusive one pot synthesis of N-amino-methyl substituted 1,4-
benzodiazepine derivatives by the reaction of N-amino-methylsubstituted isatoic
anhydride with glycine and L-proline respectively has been described (Figure-17).
Figure-17
Line S. Laustsen et al. 60 has developed an efficient solid-phase method has
been for the parallel synthesis of 1,3-dihydro-1,4-benzodiazepine-2-one derivatives
(Figure-18). A key step in this procedure involves catching crude 2-aminobenzoimine
(1) products on an amino acid Wang resin (2). Mild acidic conditions then promote a
ring closure and in the same step cleavage from the resin to give pure benzodiazepine
products (3).These synthesis strategies involve catch and release phenomena.
Figure-18
Department of Chemistry, Saurashtra University, Rajkot-360005 209