Isoxazole derivatives R 0240Synthesis and Biological Evaluation of 3-(Phthalimidomethyl)-4-(5-substituted isoxazoline and pyrazoline) Substituted Benzanilides. -A variety of phthalimidomethyl derivatives of isoxazoline (IX) (20 examples) and pyrazoline (X) is synthesized and evaluated for antibacterial and antifungal, anthelmintic and hypoglycemic activities. -(SAHU*, S. K.; AZAM, M. A.; BANERJEE, M.; CHOUDHURY, P.; SUTRADHAR, S.; PANDA, P. K.; MISRO, P. K.; J. Indian Chem. Soc. 84 (2007) 10, 1011-1015; Univ. Dep. Pharm. Sci., Utkal Univ., Bhubaneswar 751 004, India; Eng.) -H. Toeppel 33-137
Transition metal catalysed formation of Csp2-S bond through cross-coupling reaction stands important and powerful tools in synthetic organic chemistry. The reaction constitutes an important strategy for the synthesis of thioethers that possess diverse biological activities in medicine and agriculture. Nonetheless, maintaining reaction temperature during Csp2-S crosscoupling reaction decides fate of desired product along with possibility of by-product and disulfides. The economy of process, safety and environmental issue demands thioether synthesis at mild condition and room temperature. Only very few reactions were successful under mild condition using Pd, Cu, Ni, NiÀ Ir and Ir catalyst. The current prospective summarizes the best protocols used for efficient Csp2-S cross-coupling reactions by transition metal catalyst under mild condition.
Presence of multi‐stereo centre in the antimalaria artemisinin molecules makes difficult to chemist for diastereoselective synthesis. This diastereoselectivity is the main hurdle for low yield of product in the reported synthesis. Though, artemisinin‐based drugs are in the frontline treatment of malaria and effective medicine that kills malarial parasites. Due to insufficient production of artemisinin (qinghaosu), millions of people lost their lives in past years worldwide. The current review will summarize the strategy developed so far for synthesis of antimalaria artemisinin and problems encountered during the synthesis. The combined insight of different methods may allow finer approaches capable of delivering efficient synthetic approaches for developing artemisinin and their hybrid analogues for further drug discovery.
This prospective summarizes the stereochemical out comes of [3+2] cycloaddition of allene molecules with 1,3-dipolar carbonyl ylides derived from rhodium carbene mediated diazo decomposition for formation highly daistereoselective poly oxacarbocycle....
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