A general method for the construction of tetrahydro-1,4-benzodiazepine
-2-ones on solid-support has been developed utilising a cleavage-conju
gate addition protocol as the key step in the design. Using this novel
methodology the synthesis of a diverse one hundred and twenty compoun
d library with three points of diversity has been achieved starting fr
om readily available anthranilic esters. (C) 1997 Elsevier Science Ltd
.