An Expeditious Synthesis Of 3-Amino B-Lactams Derived From Polyaromatic Compounds

Abstract

A simple an effective method for the synthesis of a few trans 3-amino β-lactams derived from polyaromatic compounds has been accomplished via the deprotection of phthalimido groups with ethylene diamine. Introduction Synthesis of β-lactams as biologically active compounds is very crucial. The use of β-lactams as antibiotics is experimentally proved by several thousands of papers and patents. In contrast, research on anticancer β-lactams is very limited. We have been conducting research on the synthesis and biological evaluation of β-lactams for the last two decades. We describe herein simple as well as efficient synthesis of a few 3-amino β-lactams derived from polyaromatic precursors. These types of β-lactams are new and novel. Furthermore, they may have potential anticancer activity as demonstrated in our previous publications. Results and Discussion Reaction of phthalimido β-lactams 1 with ethylene diamine at room temperature produced 2 in good yield. The stereochemistry of β-lactams remains unchanged during this conversation. No cleavage of the β-lactam rings was observed under this conditions.