10.1007/BF01146184
The research focuses on the synthesis and pharmacological activity of certain 2,3-dihydroimidazo[1,2-a]benzimidazoles and their intermediates. The purpose of the study was to explore the potential hypotensive and hypoglycemic properties of these compounds, which contain a common nitrogen atom and an imidazoline ring, and have been found to exhibit a broad spectrum of pharmacological activity. The researchers synthesized new derivatives of 9H-2,3-dihydroimidazo[1,2-a]benzimidazole and investigated their pharmacological properties, including their effects on blood sugar levels and arterial pressure in rats, as well as their influence on the enzymatic activity of cyclic AMP phosphodiesterase (cAMP PDE) and acetylcholine esterase (ACE). The chemicals used in the synthesis process included various alkyl- and aralkyl-substituted benzimidazoles, chloroethylaminobenzimidazoles, and methoxyethylaminobenzimidazoles, among others. The conclusions drawn from the study indicated that some of the synthesized imidazo[1,2-a]benzimidazole derivatives showed promising hypoglycemic and hypotensive effects, and certain compounds demonstrated inhibitory activity against cAMP PDE and ACE, suggesting potential therapeutic applications. However, the overall effectiveness of these compounds was found to be less than that of some reference preparations, such as adebite (a quinidine derivative).
10.1021/jo00015a036
The research focuses on the synthesis of advanced intermediates of Cinchona alkaloids using silicon-directed reactions. The purpose of the study is to develop a more efficient and scalable synthetic route for these alkaloids, which are historically significant therapeutic agents, particularly quinine and quinidine. The key chemicals used in the research include benzylamine, 2-(2-bromoethyl)-1,3-dioxolane, 3-(trimethylsilyl)-2(E)-propenoyl chloride, 1-(triphenylphosphoranylidene)-2-propanone, and various other reagents such as lithium aluminum hydride, sodium borohydride, and ceric ammonium nitrate (CAN). The study concludes that a silicon-directed Baeyer-Villager oxidation is an effective method to achieve the desired transformation, yielding N-benzylmeroquinene aldehyde in good yield. The researchers also successfully synthesized alcohols 23a,b and acetates 24a,b, which are advanced intermediates for the Cinchona alkaloids. The research demonstrates the utility of silicon-directed reactions in the synthesis of complex natural products, providing a potentially more accessible route for the production of these valuable compounds.
10.1016/S0040-4020(01)96074-0
The research focuses on the chemical transformation of the Y-lactonic function of quinide into a keto-2 d-lactone through the addition of a-thiocarbanione, as an approach to synthesize enterocine, an antibiotic active against both gram-positive and gram-negative bacteria. The study also investigates the addition of acetophenone anion on the keto group of a α-keto ester. The conclusions drawn from the research indicate that while several pathways were explored, the transformation to the desired keto-2 d-lactone was challenging, with many attempts leading to either unchanged or degraded products.
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