天堂国产午夜亚洲专区-少妇人妻综合久久蜜臀-国产成人户外露出视频在线-国产91传媒一区二区三区

米格列奈的合成工藝改進(jìn)

發(fā)布時(shí)間:2018-01-25 22:36

  本文關(guān)鍵詞: 米格列奈 丁二酸二乙酯 苯甲醛 全合成 工藝優(yōu)化 出處:《青島科技大學(xué)》2014年碩士論文 論文類型:學(xué)位論文


【摘要】:米格列奈是一種非磺脲類胰島素促分泌的藥物,對(duì)于治療糖尿病具備作用時(shí)間快、藥效高、給藥?kù)`活和安全性能高等優(yōu)點(diǎn)。本文中針對(duì)以往制備米格列奈路線操作復(fù)雜、花費(fèi)高、效率低的問(wèn)題,對(duì)其合成方法進(jìn)行了改進(jìn),,并根據(jù)每步實(shí)驗(yàn)反應(yīng)機(jī)理及重要影響因素,對(duì)反應(yīng)條件和操作進(jìn)行了研究探討,尋找優(yōu)化方法,確定了各步反應(yīng)的最佳工藝條件,得出一條簡(jiǎn)單高效的工藝流程。大致包括以下內(nèi)容: 文章中首先介紹了米格列奈的結(jié)構(gòu)、性質(zhì)、藥物作用機(jī)制及以往的制備方法;并參照文獻(xiàn)合成路線進(jìn)行了對(duì)比和改進(jìn),設(shè)計(jì)了新的合成路線;另外,還對(duì)米格列奈的合成條件及影響產(chǎn)率因素進(jìn)行了一系列實(shí)驗(yàn)探索,得到本路線最優(yōu)的合成工藝。綜合目前的研究結(jié)果和現(xiàn)狀,我們確定了本課題研究?jī)?nèi)容與方向:米格列奈的合成及其工藝優(yōu)化研究。 本文的實(shí)驗(yàn)部分主要介紹了以丁二酸二乙酯和苯甲醛作為原料,通過(guò)Stobbe縮合、烯烴鍵加氫還原、外消旋體拆分、酰胺化、酯鍵水解和成鹽六步反應(yīng)制得所需的終產(chǎn)物。通過(guò)1H-NMR、旋光度、熔點(diǎn)和HPLC分析檢測(cè)鑒定,確定最終產(chǎn)物結(jié)構(gòu),實(shí)驗(yàn)表明,經(jīng)優(yōu)化后,本路線米格列奈合成的終產(chǎn)率為14.01%,工藝條件溫和,實(shí)驗(yàn)步驟簡(jiǎn)單,經(jīng)濟(jì)成本低,易于轉(zhuǎn)為工業(yè)化生產(chǎn)。
[Abstract]:Mieglinide is a non-sulfonylurea insulin secretion drug, which has a rapid effect and high efficacy in the treatment of diabetes. In order to solve the problems of complex operation, high cost and low efficiency, the synthesis method of Mieglinide was improved in this paper. According to the reaction mechanism of each step experiment and the important influencing factors, the reaction conditions and operation were studied and discussed, the optimization method was found, and the optimum process conditions of each step reaction were determined. A simple and efficient process has been developed. It includes the following: In this paper, the structure, properties, drug action mechanism and previous preparation methods of mieglinide were introduced. A new synthetic route was designed by comparing and improving the synthetic route of literature. In addition, a series of experiments were carried out on the synthetic conditions and the factors affecting the yield of Mieglinide, and the optimum synthetic process was obtained, which synthesizes the current research results and the present situation. We have determined the research content and direction of this subject: the synthesis and process optimization of miglinide. In the experimental part of this paper, diethyl succinate and benzaldehyde were used as raw materials, condensation of Stobbe, hydrogenation of olefins, resolution of racemes and amidation of racemes were introduced. The final product was obtained by hydrolysis of ester bond and six steps of salt formation. The structure of the final product was determined by 1H-NMRR, optical rotation, melting point and HPLC analysis. The experimental results showed that the final product was optimized. The final yield of mieglinide is 14.01, the technological conditions are mild, the experimental steps are simple, the economic cost is low, and it is easy to be converted to industrial production.
【學(xué)位授予單位】:青島科技大學(xué)
【學(xué)位級(jí)別】:碩士
【學(xué)位授予年份】:2014
【分類號(hào)】:R914.5

【參考文獻(xiàn)】

相關(guān)期刊論文 前10條

1 翁建平;2型糖尿病對(duì)社會(huì)造成的負(fù)擔(dān)不容忽視[J];廣東醫(yī)學(xué);2003年10期

2 信建峰;馬吉海;張樹(shù)芬;陳韶蕊;李海于;;酰氯制備方法綜述[J];河北化工;2006年11期

3 張德義;加快我國(guó)加氫工藝和技術(shù)的發(fā)展[J];煉油設(shè)計(jì);2002年03期

4 鄭德強(qiáng);劉文濤;毋立華;孫利民;王長(zhǎng)斌;;米格列奈鈣的合成[J];食品與藥品;2007年11期

5 沈洪兵,俞順章,徐耀初;我國(guó)糖尿病的發(fā)病變化及其經(jīng)濟(jì)負(fù)擔(dān)研究[J];上海預(yù)防醫(yī)學(xué)雜志;1998年09期

6 吳元民,邵寶蓉,顧惠琳,袁杏生,劉紹芳,賈偉平,項(xiàng)坤三;上海市華陽(yáng)社區(qū)糖尿病、高血壓、血脂紊亂及代謝綜合征基線調(diào)查[J];上海醫(yī)學(xué);2001年04期

7 寧光;糖尿病──肆虐全球的流行病[J];世界科學(xué);1999年11期

8 陳慕華;秦曉靜;儲(chǔ)偉;洪景萍;;載體對(duì)鈀基選擇加氫催化劑性能的影響[J];石油學(xué)報(bào)(石油加工);2006年02期

9 南軍,謝海峰,劉晨光;貴金屬選擇性加氫催化劑Pd/Al_2O_3的研究[J];石油煉制與化工;2004年08期

10 唐玲,陳興寶,陳慧云,趙魯勇,胡善聯(lián);中國(guó)城市2型糖尿病及其并發(fā)癥的經(jīng)濟(jì)負(fù)擔(dān)[J];中國(guó)衛(wèi)生經(jīng)濟(jì);2003年12期



本文編號(hào):1463883

資料下載
論文發(fā)表

本文鏈接:http://www.sikaile.net/yixuelunwen/yiyaoxuelunwen/1463883.html


Copyright(c)文論論文網(wǎng)All Rights Reserved | 網(wǎng)站地圖 |

版權(quán)申明:資料由用戶65ac8***提供,本站僅收錄摘要或目錄,作者需要?jiǎng)h除請(qǐng)E-mail郵箱bigeng88@qq.com