药物合成第七章翻译

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药学英语(化学工业出版社)课文翻译

药学英语(化学工业出版社)课文翻译

药学英语课文翻译Unit1药品依据他们的产品或来源药物能够被分为三种:Ⅰ、全合成Ⅱ、天然产物和Ⅲ、由局部合成产物〔半合成产物〕本书的重点是关于最重要化合物Ⅰ和Ⅲ——这类药物合成。

然而,这并不意味天然产物和其他的药物就不重要。

它们能够被用作有价值的先导化合物,同时它们通常被用作起始原料或作为重要合成产物的中间体。

而更加经济的。

在过往的几年里发酵,即微生物工程,差不多变得极其重要。

通过现代技术和基因的选择结果,导致了微生物高突变体演变的产生,发酵差不多变成了对物质广泛围的选择方式。

真核细胞〔酵母和霉菌〕和原核细胞〔单细菌细胞和放线菌〕都被用作微生物。

以下为可获得的生产形式:1.细胞原料〔单细胞蛋白质〕2.酶3.初级的落解产物〔初级酶代谢物〕4.次级的落解产物〔次级的代谢物〕在次级代谢物中,必先提起的是抗生素,以下五种药代表了每年世界范围内价值170亿美元的药物:青霉素,头孢菌素,四环素,红霉素,氨基糖苷类。

大约有5000种抗生素差不多从微生物中不离出来了,但在这些中仅有那些少于100种用于治疗使用。

然而,一定明白,那些衍生物通过局部合成被先进用于治疗。

在过往十年中,单单从β-内酰胺半合成的就有五万种药物。

发酵在容积大于400m3的不锈钠发酵罐中进行,防止了微生物噬菌体的污染等等,整个过程必须在无菌条件下进行。

〔倒数第五段开始〕大量使用的试剂不仅仅是酸〔盐酸、硫酸、硝酸、醋酸〕,还有无机和有机碱〔氢氧化钠、氢氧化钾、碳酸钾、重碳酸钾、铵碱、三乙胺、吡啶〕。

还有辅助化学物质包括活性炭和催化剂。

所有这些补充的化学物质〔比方中间体〕在最终产物中可能是杂志的来源。

在1969年,世界卫生组织出版了关于“药品平安质量保卫〞的论述。

名目2是有关“药品赔偿和平安保卫质量的规定〞〔世界卫生组织,1969年第418号技术报告,名目2;1975年第567号名目1A〕这同时变为众所周知的“药品质量治理标准〞或GMP标准,同时这些规定在现在药品生产中也应遵守。

药物合成反应课后翻译.

药物合成反应课后翻译.

1、About 216–224 g. (1.62–1.68 moles) of powdered anhydrous aluminum chloride is added to a 1Lthree-necked flask.在1L的三口烧瓶中加入大约216-224g(1.62–1.68 moles)的无水三氯化铝。

While the free-flowing catalyst is stirred (Note 3), 81 g. (0.67 mole) of acetophenone is added from the dropping funnel in a slow stream over a period of 20–30 minutes. 自由流动的催化剂边搅拌边用滴液漏斗缓慢滴加81g苯乙酰。

Considerable heat is evolved, and, if the drops of ketone are not dispersed, darkening or charring occurs. 放热反应,假如滴加的酮不能被分散,就会变黑或是碳化。

When about one-third of the acetophenone has been added, the mixture becomes a viscous ball-like mass that is difficult to stir.当三分之一的乙酰苯被滴加,反应混合物变成一个很难搅拌的粘性的球状团块。

Turning of the stirrer by hand or more rapid addition of ketone is necessary at this point. 在这时,改用手动搅拌或快速滴加酮是非常必要的。

The addition of ketone, however, should not be so rapid as to produce a temperature above 180°. 然而,速度不能太快,当反应温度超过180℃时。

药物合成之缩合反应翻译

药物合成之缩合反应翻译

药物合成反应——缩合反应翻译一、In a 3L round-bottomed flask with a reflux condenser are placed 625mL of 95 percent alcohol, 500mL of water, 500g (476ml, 4.7mol) of pure benzaldehyde, and 50g of sodium cyanide (96-98 percent). The mixture is then heated and kept boiling for one-half hour. In the course of about twenty minutes, crystals begin to separate from the hot solution. At the end of thirty minutes, the solution is cooled, filtered with suction, and washed with a little water. The yield of the dry crude benzoin, which is white or light yellow, is 450-460g (90-92 percent of the theoretical amount). In order to obtain it completely pure, the crude substance is recrystallized from 95 percent alcohol. 90g of crude material being dissolved in about 700ml of boiling alcohol; upon cooling, a yield of 83g of white, pure benzoin which melts at 129℃is obtained.二、In a 1L three-necked round-bottomed flask equipped with mechanical stirrer, short reflux condenser, and bent glass tube reaching below the surface of the liquid for the introduction of hydrogen chloride, are placed 50g(0.36mol) of p-nitrophenol, 650ml of concentrated hydrochloric acid, 5ml concentrated sulfuric acid, and 76g(1mol) of methylal. The mixture is stirred while the temperature is maintained at 70±2℃for 4-5 hours by means of a water bath. During this time hydrogen chloride is bubbled into the reaction mixture through the bent glass tube, and the excess gas is carried away through the refluxcondenser to a hood or gas absorption trap. The 2-hydroxy-5-nitrobenzyl chloride begins to separate as a solid about 1 hour after the beginning of the reaction. At the end of the mixture is cooled in ice for 1 hour whereby more crystals separate, after which the acid liquors are either filtered or decanted from the crystal. The 2-hydroxy-5-nitrobenzyl chloride is purified by recrystallization from 125ml of hot benzene. The yield is 46g (69% based on p-nitrophenol) of a white product melting at 129-130.翻译为:一、在一个3L圆底烧瓶中加入650mL 95%的乙醇,500mL水,476mL苯甲醛,50gNaCN(96-98%)并装上冷凝回流装置.混合物保持沸腾1个半小时,正常情况下大约20分钟有晶体从溶液中析出来。

药物合成反应(闻韧第三版)课后翻译

药物合成反应(闻韧第三版)课后翻译

1、About 216–224 g. (1.62–1.68 moles) of powdered anhydrous aluminum chloride is added to a 1Lthree-necked flask.在1L的三口烧瓶中加入大约216-224g(1.62–1.68 moles)的无水三氯化铝。

While the free-flowing catalyst is stirred (Note 3), 81 g. (0.67 mole) of acetophenone is added from the dropping funnel in a slow stream over a period of 20–30 minutes. 自由流动的催化剂边搅拌边用滴液漏斗缓慢滴加81g苯乙酰。

Considerable heat is evolved, and, if the drops of ketone are not dispersed, darkening or charring occurs. 放热反应,假如滴加的酮不能被分散,就会变黑或是碳化。

When about one-third of the acetophenone has been added, the mixture becomes a viscous ball-like mass that is difficult to stir.当三分之一的乙酰苯被滴加,反应混合物变成一个很难搅拌的粘性的球状团块。

Turning of the stirrer by hand or more rapid addition of ketone is necessary at this point. 在这时,改用手动搅拌或快速滴加酮是非常必要的。

The addition of ketone, however, should not be so rapid as to produce a temperature above 180°. 然而,速度不能太快,当反应温度超过180℃时。

(完整word版)药物合成反应(闻韧_第三版)课后翻译(word文档良心出品)

(完整word版)药物合成反应(闻韧_第三版)课后翻译(word文档良心出品)

1、About 216–224 g. (1.62–1.68 moles) of powdered anhydrous aluminum chloride is added to a 1Lthree-necked flask.在1L的三口烧瓶中加入大约216-224g(1.62–1.68 moles)的无水三氯化铝。

While the free-flowing catalyst is stirred (Note 3), 81 g. (0.67 mole) of acetophenone is added from the dropping funnel in a slow stream over a period of 20–30 minutes. 自由流动的催化剂边搅拌边用滴液漏斗缓慢滴加81g苯乙酰。

Considerable heat is evolved, and, if the drops of ketone are not dispersed, darkening or charring occurs. 放热反应,假如滴加的酮不能被分散,就会变黑或是碳化。

When about one-third of the acetophenone has been added, the mixture becomes a viscous ball-like mass that is difficult to stir.当三分之一的乙酰苯被滴加,反应混合物变成一个很难搅拌的粘性的球状团块。

Turning of the stirrer by hand or more rapid addition of ketone is necessary at this point. 在这时,改用手动搅拌或快速滴加酮是非常必要的。

The addition of ketone, however, should not be so rapid as to produce a temperature above 180°. 然而,速度不能太快,当反应温度超过180℃时。

药物合成反应闻韧第三版课后翻译

药物合成反应闻韧第三版课后翻译

1、About 216–224 g. –moles) of powdered anhydrous is added to a 1Lthree-necked flask.在1L的三口烧瓶中加入大约216-224g– moles)的无水三氯化铝。

While the free-flowing catalyst is stirred , 81 g. mole) of is added from the dropping funnel in a slow stream over a period of 20–30 minutes. 自由流动的催化剂边搅拌边用滴液漏斗缓慢滴加81g苯乙酰。

Considerable heat is evolved, and, if the drops of ketone are not dispersed, darkening or charring occurs. 放热反应,假如滴加的酮不能被分散,就会变黑或是碳化。

When about one-third of the has been added, the mixture becomes a viscous ball-like mass that is difficult to stir.当三分之一的乙酰苯被滴加,反应混合物变成一个很难搅拌的粘性的球状团块。

Turning of the stirrer by hand or more rapid addition of ketone is necessary at this point. 在这时,改用手动搅拌或快速滴加酮是非常必要的。

The addition of ketone, however, should not be so rapid as to produce a temperature above 180°. 然而,速度不能太快,当反应温度超过180℃时。

制药工程专业英语详细Unit1.3.6详细翻译

制药工程专业英语详细Unit1.3.6详细翻译

Unit 1 Production of Drugs根据其生产或来源不同药物制剂可以分为三类:Ⅰ。

人工合成材料(全合成材料)Ⅱ。

天然产物,和Ⅲ.半合成天然产物(半合成药物).本书的重点是这些第一组和第三组化合物都是合成药物。

然而这并不意味着那些天然药物和其他药物就不重要.他们可以作为很有价值的先导结构,并经常被用为重要合成药物的原料或中间体。

表1概述了获取药物制剂的不同方法。

Table 1 Possibilities for the preparation of drugs表1药物制备的可能性几种最初来自于天然原料有治疗意义天然产物如今用更有效也就是经济的全合成法制备。

这样的例子包括L—氨基酸,氯霉素,咖啡因,多巴胺,肾上腺素,左旋多巴,肽类激素,前列腺素,D —青霉胺,长春蔓胺,以及几乎所有的维生素.在过去的几年里发酵(即微生物处理)变得极其重要。

通过现代技术和遗传选择的结果产生了高效能微生物突变株,发酵已成为广泛的底物(物质)都可以选择的一种方法.真核微生物(酵母菌和霉菌)和原核微生物(单细胞细菌和放线菌)用于微生物。

可以得到以下产品类型:1.细胞原料(单细胞蛋白)2.酶3.主要降解产物(初级代谢物)4.次要降解产物(次级代谢物).除了某些微生物(如肠膜明串珠菌)的黏膜所合成葡萄糖以外第2类和第3类都是与药物的制备相关的物质。

分子量为5万到10万的葡萄糖可以作为血浆替代品。

在这些初级代谢物中谷氨酸棒状杆菌和黄色短杆菌的突变体产生的L —氨基酸是特别有意义的。

利用这些生物体大约可以生产35万吨味精(食物添加剂)和7万吨L —赖氨酸(用于植物蛋白补充)。

更重要的初级代谢产物有嘌。

呤核苷酸,有机酸,乳酸,柠檬酸和维生素,例如谢曼丙酸杆菌产生的维生素12其中首先要提到的次级代谢物是抗生素.以下五类抗生素每年全球销售额170亿美元:青霉素(黄青霉)头孢菌素(假头状孢子头枝顶孢属)四环素(金色链霉菌)红霉素(红霉素链霉菌)氨基糖苷类抗生素(灰色链霉菌)微生物已经分离出大约5000种抗生素的,但其中只有不到100种应用于临床治疗。

制药工程专业英语unit 1、2、3、4、5、16、17、18、19、20中文翻译(庄永思,吴达俊版)

制药工程专业英语unit  1、2、3、4、5、16、17、18、19、20中文翻译(庄永思,吴达俊版)

1、生产的药品其生产或出身不同药剂可以分为三类:Ⅰ.完全(合成纤维)合成材料,Ⅱ.天然产物,和Ⅲ.产品从(半合成产品)的部分合成。

本书的重点是团体的最重要的化合物Ⅰ和Ⅲ一所以药物合成。

这并不意味着,但是,天然产品或其他代理人并不太重要。

它们可以作为有价值的领导结构,他们常常为原料,或作为重要的合成中间体产品的需要。

表1给出了获取药剂的不同方法的概述。

(表1对药物的可能性准备)方法举例1、全合成,超过75%的药剂(合成纤维)2、分离(天然产物)天然来源:2.1植物-生物碱;酶;心甙,多糖,维生素E;类固醇的前体(薯蓣皂素,sitosterin),柠檬醛(中间产品维生素A,E和K)2.2动物器官一酶;肽激素;胆酸从胆;胰岛素)从胰脏;血清和疫苗2.3从角蛋白和明胶L -氨基酸;三一胆固醇从羊毛油脂的其他来源水解3.一抗生素发酵; L -氨基酸,葡聚糖,对类固醇有针对性的修改,例如11 -羟基化;也胰岛素,干扰素,抗体,肽激素,酶,疫苗4。

部分合成修改(半合成剂)天然产品: 一生物碱化合物;半合成/ 3-内酰胺类抗生素;类固醇;人胰岛素其中几个重要的治疗作用最初是从天然产品天然来源获得更有效的今天,我。

大肠杆菌更经济的准备..由全合成。

这样的例子包括L-氨基酸,氯霉素,咖啡因,多巴胺,肾上腺素,左旋多巴,肽类激素,前列腺素,D -青霉胺,长春胺,以及几乎所有的维生素。

在过去的几年里发酵-岛大肠杆菌微生物过程变得极其重要。

通过现代技术和基因选择的结果导致了突变体的微生物创造高性能,发酵,已成为首选方法各种各样的物质。

这两个Eukaryonts(酵母菌和霉菌)和Prokaryonts(单细胞细菌,放线菌和)用于微生物。

下列产品类型可以得到:1.细胞的物质(单细胞蛋白),2.酶,3.主要降解产物(主要代谢物),4.二级降解产物(次生代谢物)。

不顾来自某些微生物,大肠杆菌粘膜生产的葡聚糖克明串珠mesenteroides,2和3级是毒品有关的准备工作。

制药工程专业英语课文翻译1 5 11 13 16单元原文加翻译

制药工程专业英语课文翻译1 5 11 13 16单元原文加翻译

Unit 1 Production of DrugsDepending on their production or origin pharmaceutical agents can be split into three groups:I .Totally synthetic materials (synthetics),Ⅱ.Natural products,andⅢ.Products from partial syntheses (semi-synthetic products).The emphasis of the present book is on the most important compounds of groups I and Ⅲ一thus Drug synthesis. This does not mean,however,that natural products or other agents are less important. They can serve as valuable lead structures,and they are frequently needed as starting materials or as intermediates for important synthetic products.Table 1 gives an overview of the different methods for obtaining pharmaceutical agents.1单元生产的药品其生产或出身不同药剂可以分为三类:1。

完全(合成纤维)合成材料,Ⅱ。

天然产物,和Ⅲ。

产品从(半合成产品)的部分合成。

本书的重点是团体的最重要的化合物Ⅰ和Ⅲ一所以药物合成。

这并不意味着,但是,天然产品或其他代理人并不太重要。

它们可以作为有价值的领导结构,他们常常为原料,或作为重要的合成中间体产品的需要。

药物合成反应课后翻译

药物合成反应课后翻译

四次把深色的油从混合物中用 150ml 萃取岀来。

The extracts are combined, washedto produce a temperature above 180° .然而,速度不能太快,当反应温度超过either heated or cooled. The molte n mass, in which the acet ophenon e is complexed with aluminum chloride, ranges in color from tan to brown.明苯乙酰已经和三氯化铝混合完全,颜色也逐渐从黄褐色变为棕色。

混合均匀。

Part of the cold aqueous layer is added to the reacti on flask to deco mposewhatever part of the reactionmixture remains there, and the resultingmixture is addedto the beaker.把部分的冰水层加入到烧瓶中洗涤残留物,然后合并到烧杯中。

that settles out is extracted from the mixture with four 150-ml. p orti ons of etherAbout 216 — 224 g. — moles) of po wdered an hydrous aluminum chloride is added to a1Lthree-necked flask.在1L 的三口烧瓶中加入大约 216-224g - moles)的无水三氯化铝。

While the freeflow ing catalyst is stirred (Note 3), 81 g. mole) of acet ophenone is added from the dropping funnel in a slow stream over a p eriod of 20 -30 minutes. 自由流动 的催化剂边搅拌边用滴液漏斗缓慢滴加 81g 苯乙酰。

药物合成第七章翻译

药物合成第七章翻译

本次翻译由【谭扬】一人独立完成,考虑到很多人应该没有翻译,所以提供大家共享哈哈~~ 注:红色部分为翻译不出或者有问题等。

In a 500mL modified Claisen flask are placed 250g (4 moles) of ammonium formate, 150 g. (1.25 moles) of acetophenone, and a few chips of porous plate.在一个500mL的改良克氏烧瓶中加入250g(4moles)的甲酸铵和150g(1.25moles)的乙酰苯以及几片多孔板。

The flask is fitted with a cork carrying a thermometer extending nearly to the bottom, and the side arm is connected to a small condenser set for distillation.烧瓶口装有携带温度计的软木塞延伸近烧瓶底部,在其侧壁连接有一个蒸馏用的小型冷凝器。

On heating the flask with a small flame the mixture first melts to two layers and distillation occurs; at 150–155° it becomes homogeneous and reaction takes place with moderate foaming.当用小火加热烧瓶时,先将混合物融化并分成两层随即开始蒸馏;当温度达到150-155°时,液体将均匀混合并发生反应伴有温和发泡。

The heating is continued, more slowly if necessary, until the temperature reaches 185°.持续加热,若有必要可以更加缓慢,直到温度达到185°。

(完整word版)药物合成反应(闻韧_第三版)课后翻译(word文档良心出品)

(完整word版)药物合成反应(闻韧_第三版)课后翻译(word文档良心出品)

1、About 216 -224 g. (1.62 —.68 moles) of powdered an hydrous alumi numchloride is added to a 1Lthree-necked flask. 在1L 的三口烧瓶中加入大约216-224g(1.62 —.68 moles) 的无水三氯化铝。

While the free-flowi ng catalyst isstirred (Note 3), 81 g. (0.67 mole) of acetophenone is added from the droppingfunnel in a slow stream over a period of 20 -30 min utes. 自由流动的催化剂边搅拌边用滴液漏斗缓慢滴加81g 苯乙酰。

Considerable heat is evolved, and, if the drops of ketoneare not dispersed, darke ning or charri ng occurs. 放热反应,假如滴加的酮不能被分散,就会变黑或是碳化。

When about on e-third of the acetophe none has bee n added, themixture becomes a viscous ball-like mass that is difficult to stir. 当三分之一的乙酰苯被滴加,反应混合物变成一个很难搅拌的粘性的球状团块。

Turning of the stirrer by hand ormore rapid additi on of ket one is n ecessary at this point. 在这时,改用手动搅拌或快速滴加酮是非常必要的。

The additi on of ket one, however, should not be so rapid as toproduce a temperature above 180 .然而,速度不能太快,当反应温度超过180 C时。

药物合成方程式+名词解释+反应机理 石皮 石...

药物合成方程式+名词解释+反应机理 石皮 石...

药物合成反应方程式第一章:卤代反应1.2.3.4.5.6.第二章:烃化反应1.盐酸普萘洛尔的合成:2.盐酸氯丙嗪的合成:构型保持构型反转4.第三章:酰化反应 1. 2. 3. 4第四章:缩合反应 1. 2. 3 4.6.7.8.9.10.11. 13.第五章:重排反应1.2.3.4.5.7.8.9. 11.12.13.14.15.17.第六章:氧化反应 一、完成下列反应: 1. 2. 3. 4. 5. 6. 7. 8. 9. 10.℃℃11.12.13.14.二、写出下列反应的主要试剂和反应条件:1.2. 3.4.5.6.7.8.9.第七章:还原反应 一、完成下列反应: 1. 2. 3. 4. 5. 6. 7. 8. 9. 10. 11.二、写出下列反应的化学试剂和反应条件: 1.2.3.4.5. 其他:1.在利尿药氯噻酮的中间体对氯苯甲酸的制备中,为什么1mol的邻苯二甲酸酐要用2.4mol的AlCl3为催化剂?若傅克酰化反应中用酰氯为酰化剂,催化剂AlCl3的用量如何?反应结束后,产物如何从反应中分离?2.下列两种甾醇以鉻酸氧化时,哪一种速度快,为什么?药物合成名词解释1.Adams’ catalyst (Adams催化剂):将氯铂酸铵与硝酸钠混合均匀后灼热熔融,氧化过程中有大量二氧化氮放出,经洗涤等处理后即得二氧化铂催化剂。

2.Arndt-E istert reaction (Arndt-E istert重排):Arndt-Eistert等用酰氯与重氮甲烷反应得α-重氮酮,再经Wollf重排,生成比原酰氯多一个碳的羧酸,该反应环称Arndt-Eistert反应。

3.Baeyer-Villiger oxidation (Baeyer-Villiger氧化反应):在酸催化下,醛或酮与过氧酸作用,在烃基与羰基之间插入氧生成酯的反应称为Baeyer-V illiger氧化重排。

4.Beckmann rearrangement (Beckmann重排):醛肟或酮肟在酸性催化剂作用下重排成取代酰胺的反应称Beckmann重排。

药学英语Unit7 Text A 注释及译文

药学英语Unit7 Text A 注释及译文

Unit SevenText A BiopharmaceuticsBefore the reader can appreciate the meaning and clinical significance of biopharmaceutics, it is necessary to introduce the concept of drug bioavailability.1. appreciate [ə'pri:ʃ ieit] vt.欣赏;感激;领会;鉴别vi.增值;涨价2. bioavailability ['baiəuə,veilə'biləti] n.生物利用度;生物药效率为了使读者能够理解生物药剂学的含义和其对于药物临床应用的重要意义,有必要先给大家介绍一下药物生物利用度的概念。

BioavailabilityThe therapeutic response of a drug is normally dependent on an adequate concentration of the drug being achieved and then maintained at the site or sites of action of the drug. In the case of systemically acting drugs ( i. e. drugs that reach these sites via the systemic circulation) it is generally accepted for clinical purposes that a dynamic equilibrium exists between the concentration of drug at its site(s) of action and the concentration of drug in blood plasma. An important consequence of this dynamic equilibrium is that it permits a therapeutically effective concentration of drug to be achieved at its site(s) of action by adjustment of the concentration of drug in blood plasma. Strictly speaking, the concentration of drug in plasma water (i. e. protein-free plasma) is a more accurate index of drug concentration at the site(s) of action than the concentration of drug in whole plasma since a drug may often bind in a reversible manner to plasma protein. Only drug which is unbound (i. e. dissolved in plasma water) can pass out of the plasma through the capillary endothelium and reach other body fluids and tissues and hence its site(s) of action. Drug concentration in whole blood is also not considered to be an accurate indirect index of the concentration of drug at its site(s) of action since drug can bind to and enter blood cells. However, to measure the concentration of an unbound drug in plasma water requires more complex and sensitive assay methods than to measure the total concentration of both unbound and bound drug in total plasma. Thus, for clinical purposes, drug concentration in blood plasma is usually measured and is regarded as an index of drug concentration at the site(s) of action of the drug and of the clinicaleffects of the drug. However, it should be realized that this is a simplification and may not always be valid. Indeed one should not draw inferences about the clinical effects of a drug from its plasma concentration until it has been established that the two are consistently correlated. It has been assumed that the plasma drug concentration is directly proportional to the clinical effect of that drug.1. systemically [ sistə'mætikəli ] adv.有系统地,有组织地,有条理地,全身地systemic [si'stemik; -'sti:-] adj.系统的;体系的;全身的2. purpose ['pə:pəs] n.目的;用途;意志vt. 决心;企图;打算3. dynamic equilibrium [dai'næmik] [,i:kwi'libriəm] 动态平衡;动力平衡4. plasma ['plæzmə] n.等离子体;血浆5. reversible [ri'və:səbl] adj.可逆的;可撤消的;可反转的n. 双面布料6. capillary endothelium [kə'piləri, 'kæpi-] [,endəu'θi:liəm] 毛细血管内皮7. assay [ə'sei] n.化验;试验vt.分析;化验;尝试vi.鉴定;经检验证明内含成分8. simplification [,sɪmpləfə'keʃən] n.简单化;单纯化9. valid ['vælid] adj.有效的,有根据的;正当的10. draw inferences ['infərəns] 作出推论11. consistently [kən'sistəntli] adv.一贯地;一致地;坚实地12. proportional to [prə'pɔ:ʃənəl] 与……相称,与……成比例通常情况下,药物达到其作用部位、并维持足够的药物浓度,才能发挥疗效。

药物合成反应(闻韧第三版)课后翻译

药物合成反应(闻韧第三版)课后翻译

1、About 216–224 g. (1.62–1.68 moles) of powdered anhydrous aluminum chloride is added to a 1Lthree-necked flask.在1L的三口烧瓶中加入大约216-224g(1.62–1.68 moles)的无水三氯化铝。

While the free-flowing catalyst is stirred (Note 3), 81 g. (0.67 mole) of acetophenone is added from the dropping funnel in a slow stream over a period of 20–30 minutes. 自由流动的催化剂边搅拌边用滴液漏斗缓慢滴加81g苯乙酰。

Considerable heat is evolved, and, if the drops of ketone are not dispersed, darkening or charring occurs. 放热反应,假如滴加的酮不能被分散,就会变黑或是碳化。

When about one-third of the acetophenone has been added, the mixture becomes a viscous ball-like mass that is difficult to stir.当三分之一的乙酰苯被滴加,反应混合物变成一个很难搅拌的粘性的球状团块。

Turning of the stirrer by hand or more rapid addition of ketone is necessary at this point. 在这时,改用手动搅拌或快速滴加酮是非常必要的。

The addition of ketone, however, should not be so rapid as to produce a temperature above 180°. 然而,速度不能太快,当反应温度超过180℃时。

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本次翻译由【谭扬】一人独立完成,考虑到很多人应该没有翻译,所以提供大家共享哈哈~~ 注:红色部分为翻译不出或者有问题等。

In a 500mL modified Claisen flask are placed 250g (4 moles) of ammonium formate, 150 g. (1.25 moles) of acetophenone, and a few chips of porous plate.
在一个500mL的改良克氏烧瓶中加入250g(4moles)的甲酸铵和150g(1.25moles)的乙酰苯以及几片多孔板。

The flask is fitted with a cork carrying a thermometer extending nearly to the bottom, and the side arm is connected to a small condenser set for distillation.
烧瓶口装有携带温度计的软木塞延伸近烧瓶底部,在其侧壁连接有一个蒸馏用的小型冷凝器。

On heating the flask with a small flame the mixture first melts to two layers and distillation occurs; at 150–155° it becomes homogeneous and reaction takes place with moderate foaming.
当用小火加热烧瓶时,先将混合物融化并分成两层随即开始蒸馏;当温度达到150-155°时,液体将均匀混合并发生反应伴有温和发泡。

The heating is continued, more slowly if necessary, until the temperature reaches 185°.
持续加热,若有必要可以更加缓慢,直到温度达到185°。

During this process water, acetophenone, and ammonium carbonate distil; about three hours is required and little attention is necessary(这一句没搞懂).
在这个过程中,水、乙酰苯、和碳酸铵被蒸出;大约须要三小时并且要注重细节。

At 185° the heating is stopped and the upper layer of acetophenone is separated from the distillate and returned, without drying, to the reaction flask.
在185°时停止加热,上层的苯乙酮馏分被分离并未经干燥返回烧瓶中。

The mixture is then heated for three hours at 180–185°.
然后在180-185°加热混合物3小时。

The distillate is extracted with 25–30mL of benzene to recover acetophenone, and the aqueous portion is discarded.
蒸馏物与25-30mL的苯反应恢复成苯乙酮,而水层被丢弃。

The reaction mixture is cooled and then shaken in a 500mL separatory funnel with 150–200mL of water to remove ammonium formate and formamide.
反应混合物冷却之后与150-200mL的水在一个500mL的分液漏斗中震荡除去氨甲酸和甲酰胺。

The crude α-phenylethylformamide is drawn off into the original flask, and the water layer is extracted with two 30mL portions of benzene and discarded.
粗品苯基乙基甲酰胺抽出到原烧瓶中,水提取层和两份30mL苯合并后丢弃。

The benzene extracts are united with the main portion, and 150 mL of concentrated hydrochloric acid is added, together with a few pieces of porous plate.
苯提取物与主要成分联合在一起,并加入150mL浓盐酸,之后加入几片多孔板。

The mixture is cautiously heated until the benzene has distilled and then boiled gently for forty to fifty minutes longer.
谨慎地加热混合物直到苯被蒸馏出来,然后温和的加热40-50分钟。

Hydrolysis proceeds rapidly, and the mixture becomes homogeneous except for a small layer of acetophenone and other neutral substances.
水解的收益迅速,且混合物变得均匀除了有一小层苯乙酮和其他中立物质。

The mixture is cooled and extracted first with 50 mL of benzene and then with three or four 25mL portions of the solvent.
混合物冷却后并首次用50mL的苯萃取,然后用3或4次其他溶剂萃取。

The extracts are saved for the recovery of acetophenone.
保存该提取物为了之后恢复苯乙酮。

The aqueous acid solution is transferred to a 1L round-bottomed flask provided with a separatory funnel and equipped for steam distillation.
酸溶液会转移到一个1L的配有分液漏斗和蒸馏装置的圆底烧瓶中。

A solution of 125g of sodium hydroxide in 250 mL of water is added through the funnel, and the mixture is distilled with steam.
125g的氢氧化钠水溶液通过漏斗加入到250mL水中,蒸馏得到混合物。

The first liter of distillate contains most of the amine, but the distillate should be collected until it is only faintly alkaline.
第一升蒸馏物包含了大多数胺类,但是馏分要收集起来直到它有一点碱性时。

A small residue containing di-(α-phenylethyl)-amine and neutral substances remains in the flask and may be discarded.
包含次苯乙胺和中性物质的小部分残渣遗留在烧瓶中很有可能被遗弃。

The distillate is extracted with five 50mL portions of benzene, and the benzene solution is dried thoroughly with powdered sodium hydroxide and distilled.
提取物用5个50mL的苯萃取,苯溶液用粉末状氢氧化钠彻底干燥并蒸馏。

Most of the amine distils at 184–186°, but the fraction distilling at 180–190° is sufficiently pure for most purposes.
大多数胺类在184-186°被提炼出,但是小部分在180-190°提炼出的对于大多数用途来说已经足够纯净了。

The yield of this fraction is 80–88g By combining the benzene fore-run with the distillation residue, extracting with dilute acid, and recovering the amine as above, an additional 10–12g of material can be obtained, making the total yield 90–100g (60–66 per cent of the theoretical amount based on the acetophenone taken).
这一小部分产量大约在80-88g,通过结合苯的初馏物和残渣、用稀酸萃取、和恢复上述的胺类、还有额外的10-12g物料包括在内可使得总收率达到90-100g(60%-66%理论上的量是基于乙酰苯的消耗量)。

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