Author's Organization：Faculty of Pharmaceutical Sciences, Hokkaido University Faculty of Pharmaceutical Sciences, Hokkaido University:(Present address)Department of Organic Chemistry, Faculty of Chemistry, Vilnius V. Kapsukas University Faculty of Pharmaceutical Sciences, Hokkaido University:(Present address)Faculty of Pharmaceutical Sciences, Higashi-Nippon-Gakuen University Faculty of Pharmaceutical Sciences, Hokkaido University
A pyrrolo-1, 4-benzodiazepine skeleton which constitutes the common part of a series of antibiotics exhibiting antitumor activity was synthesized by insertion of carbon monoxide into o-bromoprolylaniline derivatives in the presence of a catalytic amount of Pd (OAc)2 and PPh3. In this reaction, hexamethylphosphoramide (HMPA) gave a good result as the solvent and the use of a high pressure of carbon monoxide (5 atom) increased the yield of the desired pyrrolo-1, 4-benzodiazepine.
