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moneyhost: 金币+10, 翻译EPI+1, ★有帮助 2013-04-09 19:24:59
phu_grassman: 金币+1, 翻译EPI-1, 杜绝机器翻译。 2013-04-14 09:15:10
Optimization of the synthesis conditions of the chiral genetically targeted drugs polyamide build their critical dimer
Abstract: Currently, the synthesis of polyamides (PAS), mainly taken two ways: the liquid phase synthesis and solid phase synthesis. This article aims to research and technology improvements in the liquid phase synthesis, polyamides (PAS), a synthetic low yield and long routes, complicated operation, building the key pieces required for polyamides. Take the fragment coupling the strategy to explore a method is simple, short routes, efficient, high-yield, green synthetic route. By N-methyl pyrrole, N-methyl imidazole as a starting material, after the acylation reaction to FC, nitration, haloform reaction, reduction, hydrolysis, Fmoc-amino protection reaction step was designed and synthesized four key dimerized body (dimer) fragments and monomer synthesis technology available on the market to improve and optimize, simplify the synthetic steps, shortening the synthesis time, greatly improving the yield and purity; solid-phase synthesis for subsequent manual pyrrole - imidazole polyamide provides the necessary raw materials. Article also by the (S) - - hydroxy - - amino butyric acid as a the chiral recognition element, the synthesized key dimer fragment (dimer) is designed as a basic building element, by manual solid-phase synthesis method of building 2 the strip has a chiral pyrrole - imidazole polyamide modified. This method overcomes the manual solid phase synthesis Cheng Zhongfu electronic heterocyclic acid and the nucleophilic imidazole amine coupling of electron-deficient difficult problem, while saving agents to improve the yield and efficiency of solid-phase synthesis and yield, and to reduce the environmental contamination. For further research polyamide research in cell and molecular biology, animal models of applications in the future, until the development to lay the foundation for a new generation of targeted gene drugs. |
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