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The synthesis of several drugs and intermediates

Author: LiDianQing
Tutor: ShiZhiQiang
School: Shandong Normal University
Course: Organic Chemistry
Keywords: Dimethy1-β-Propiothetin Acid Dithiophosphate derivatives Sertaconazole nitras Nifuroxazide Nifursol
CLC: TQ460.1
Type: Master's thesis
Year: 2008
Downloads: 233
Quote: 1
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Abstract


The present paper prime task involves the medicine and the intermediate synthesis research, mainly includes the following content:1、A efficient Synthesis of Dimethy1-β-Propiothetin AcidDimethy1-β-Propiothetin Acid (DMPT) is the most intense olfactory nerves stimulant. To many kinds of fishes and shrimps’s growth and takes in food that it has the varying degree promoter action. Enhance a fish’s resistivity to poor surroundings. This article has designed one new highly efficient synthesis of dimethy1-β-propiothetin acid. Factors such as raw materials, temprerature and time were dicussed and the optimum process conditions were as follows: n(crylic acid) : n(dimethyl sulfide) : n(halogenic acid) = 1∶0 .5～4∶1～6. the purity is high, and the production rate can reaches above 99%. Only one step, specially simple technical process , and raw materials can get easyly, Very suitable for industrial production.2、Dithiophosphate derivatives synthesis researchWe mainly have done the thorough research to its derivatives synthesis, This method can divides three steps to carry on. First take the phosphoric sulfide and the alkyl alcohol as raw material, obtains O, O-dialkyl-S-hydrogen phosphorodithioate. Then take the maleic anhydride and the alkyl alcohol as raw material under the catalyst function, obtains the dialkyl maleate after the esterification. Finally passes through the two addition reaction to obtain a terms of dithiophosphate derivatives. About this method,its purification is simple, the cost is low, security and the product purity are high. Very suitable for industrial production.3、Sertaconazole nitras synthesis researchThe Sertaconazole is a new pyrrole ring anti-fungus medicine. Its security is good, and the economic efficiency is remarkable. We have conducted a comprehensive thorough research to the sertaconazole nitras, absorpted original reasonable steps. Through the improvement innovation, we proposed a more simple, more lower cost and more easily controlled synthesis method. Have made the significant development. (1) If outset raw materials have bene reported in the literature, production yield is not lower than the literature value’s 85%;(2) The reagent and raw materials are the domestic product, and low in price;(3) Low pollution, low energy consumption;(4) Operated simply, suitably for industrial production, and internationallly the technology to be in the lead.4、Nifuroxazide with Nifursol’s high production yield synthesis researchThe Nifuroxazide and Nifursol are all the new highly effective feed additive (the European Economic Community only legal animal special-purpose). It can promote the animal to grow fast, and has the special effect in the prevention of animal respiratory tract and the intestinal tract disease aspect. Animal’s medicine sensitive effect is higher than other antibiotics far in the water.In view of the fact that the overseas patent soon expires, we have conducted a deep research to it. We also hoped that they could be made industrially as soon as possible. The synthesis method contains three steps, obtained the product through the esterification, the acylation and the condensation. Its purity is high, each yield can reach 75%. Raw material can get easily, operated easily, suitablly for the industrial production.

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