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Environmentally Friendly Syntheses of Biological Active Azaheterocycles Valentina Yu 1, Assel Ten 1 and Lyailya Bahktybaeva 2 1 Instutite of Chemical Sciences, Kazakhstan 2 al-Farabi Kazakh National University, Kazakhstan yu_vk@mail.ru 1. Relevance: It is not a secret that in society there is a negative attitude towards chemistry as industry giving a high contribution to the pollution of the environment. On another hand, chemistry is capable of creating and indeed creates new reagents, drugs, catalysts and various materials necessary for humans. The development of modern chemistry is characterized by the tendency of tightening environmental regulations and transition to the safe and efficient technologies. This tendency reflects the essence of green chemistry: techniques of which allow not only obtaining the desired substance but performing it without damage to the environment at every stage of production. 3. Methods: For the synthesis and construction of desired molecules a wide range of the organic reactions is used. The main criterion for selection of structural units is giving the complete molecule a specific biological function as well as reduction of its toxicity. Desired molecule must “works” as a plant hormones– provide bioeffect in very small concentrations. 2. Aims & Objectives: There had been found analgesics, cardiac anti-arrhythmics, immunomodulators, geroprotectors, plant growth stimulants among synthesized by us compounds. The studied azaheterocycles family refers to the organic compounds of complex structure. The synthesis of these is multi stage, sometimes with low yields and long reaction time. The environmental risks from the production are big but the demand for them is very high. The aim is to demonstrate the benefits of green synthesis methods of azaheterocycles in comparison with classical ones. 5. Conclusions: It is well known that “bad” environment is harmful for the health, especially of children and women, therefore the resulting green methods will help switch to the ecologically friendly strategies of the search and synthesis of biologically active substances. 4. Results: It was found that the use of MW-radiation in the Williamson alkylation of azaheterocyclic alcohols and oximes with bromides in the presence of phase transfer catalyst – tetrabutylammonium bromide, reduces the reaction time from few days to few minutes and increases the yield of ethers by 20%. In addition, the formation of the by-product in the reaction of phenoxyalkylbromides with DMF (classical alkylation solvent) is avoided. MW-radiation is required for Mannich aminomethylation of azaheterocyclic ethynyls with aromatic aldehydes and cyclic amines in the presence Cu 2 Hal 2 to obtain propargyl derivatives with sufficiently good yield (up to 60%). Ionic liquids correspond to the concept of “green” chemistry due to their recyclability, non- flammability and non-volatility. In the alkylation of initial carbo- and heterocyclic alcohols and oximes with alcoxy- and phenoxyalkylbromides the IL - [BMIM]Br appeared to be a good alternative to DMF, acetone, benzene, etc., as well as alkylation promoter. The Favorskii ethynylation of cyclic ketones, where hydroxyl containing acetylenes in diethyl ether, dioxane or benzene were taken turned to be unsatisfying. The use of [BMIM]Br sufficiently solves the problem.
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