( S )-2-(4-Chlorobenzoyl)-1,2,3,4-tetrahydrobenzo[ e ]pyrazino[1,2- a ][1,4]diazepine-6,12(11 H ,12 aH )-dione?￠????Synthesis and Crystallographic Studies

摘要

( S )-2-(4-Chlorobenzoyl)-1,2,3,4-tetrahydrobenzo[ e ]pyrazino[1,2- a ][1,4]diazepine-6,12(11 H ,12 aH )-dione was obtained in a three-step, one-pot synthesis, starting from optically pure ( S )-2-piperazine carboxylic acid dihydrochloride. Selective acylation of the ???2 -nitrogen atom followed by condensation with isatoic anhydride and cyclization with HATU/DIPEA to a seven-member benzodiazepine ring, led to the tricyclic benzodiazepine derivative. Crystallographic studies and initial biological screening were performed for the title compound.