Generation of 500-Member Library of 10-Alkyl-2-R1,3-R2-4,10-Dihydrobenzo[4,5]imidazo[1,2-α]pyrimidin-4-ones

Abstract

Representative benzimidazopyrimidinones were previously reported to be intercalating antitumor agents. In this work, we used 2-substituted 4,10-dihydrobenzo Dihydrobenzo[4,5]imidazo[1,2-a]pyriminin-4-ones for their diversification by regioselective alkylation. Under the conditions established, the alkylation gave 10-alkyl derivatives which permitted the parallel generation of a 500-member library of the title compounds.

Microwave assisted synthesis of dihydrobenzo[4,5]imidazo[1,2-a]pyrimidin-4-ones; synthesis, in vitro antimicrobial and anticancer activities of novel coumarin substituted dihydrobenzo[4,5]imidazo[1,2-a]pyrimidin-4-ones

“…This method gave the higher yield (74e94%) and required a shorter reaction time (3 min). The compounds (2deh) have already been reported by the thermal method (Table 1) in the literature [11].…”

“…The known synthetic method of dihydrobenzo [4,5]imidazo[1,2-a]pyrimidin-4-one derivatives [11] had many demerits such as long reaction time, drastic condition, tedious experimental procedure and low yield. Hence, there is a need for a simple and straight forward method for the synthesis of dihydrobenzo [4,5]imidazo [1,2-a]pyrimidin-4-one derivatives.…”

One‐Pot Synthesis of Benzo[4,5]imidazo[1,2‐a]pyrimidin‐2‐ones Using a Hybrid Catalyst Supported on Magnetic Nanoparticles in Green Solvents

“… [23] Benzimidazopyrimidines have also been reported as pyrimidobenzimidazoles in literature. [ 23 , 24 , 25 ] They have widely biological properties such as antibacterial, [26] antiviral, [27] antifungal, [28] antiulcer, [29] anti‐HIV, [30] anticancer,[ 31 , 32 ] antiproliferative [33] and anti‐inflammatory [34] activities. For treatment of Alzheimer disease, some of these compounds have been applied as allosteric enhancer of acetylcholine affinity at muscarinic M 3 receptor, [35] imaging agent for detecting neurological disorders [36] and protection against amyloid β associated neurotoxicity.…”

“…Benzimidazo[1,2‐ a ]pyrimidines are an important category of N ‐fused heterocycles containing pyrimidine and benzimidazole rings [23] . Benzimidazopyrimidines have also been reported as pyrimidobenzimidazoles in literature [23–25] . They have widely biological properties such as antibacterial, [26] antiviral, [27] antifungal, [28] antiulcer, [29] anti‐HIV, [30] anticancer, [31,32] antiproliferative [33] and anti‐inflammatory [34] activities.…”