药物合成反应课后翻译
药物合成反应第五章(翻译题)
药物合成反应第五章作业1)翻译通过Cu r ti u s 重排，从反-2，4-戊二烯酸合成苄基，反-1，3-丁二烯-氨基甲酸一个干燥的，配备磁性搅拌棒和温度计和压力平衡轴承氮入口滴液漏斗的，250毫升三口圆底烧瓶。
烧瓶用氮冲洗后，称取49克（0.50摩尔）的反-2,4 -戊二烯酸、80克（0.62摩尔）的N，N -二异丙基和300毫升的丙酮放于烧瓶中。
这个溶液被搅拌并用冰盐浴冷却至0℃。
55克（0.51m o l）氯甲酸乙酯的150毫升的丙酮溶液加入到烧瓶中，保持温度低于0℃超过30分钟。
把65g （1.0m o l）叠氮化钠的170ml的水冷冻溶液加到烧瓶中，在温度低于0°下保持20分钟，之后在0℃下继续搅拌30分钟。
这个烧瓶被额外在0℃下被搅拌10~15分钟，然后倒倒装有500m l冰水的2L的分液漏斗中。
用6份250m l的甲苯提取酰基叠氮。
结合提取得到的甲苯，用无水硫酸镁干燥，集中到一个体积约300毫升的水浴温度40-50℃旋转蒸发器中。
当甲苯溶液浓缩时，同时组装一个干燥的带有压力平衡滴液漏斗、一个简单的蒸馏头、一个加热地幔的和装有机械搅拌器的2L三口圆底烧瓶和称取43克（0.40摩尔）苯甲醇、250m g4 - 叔丁基邻苯二酚和200m l苯。
大约30m l的甲苯通过蒸馏除去微量的水份，蒸馏头用冷凝和有氮气保护的代替。
搅拌并加热氮气保护下，酰基叠氮的甲苯溶液被添加，超过30分钟。
红外线分析证实了，酰基叠氮化物和异氰酸酯的消失。
通过冰浴迅速把溶液冷却至温，在这之后，在10-30分钟全部转换成氨基甲酸酯类。
甲苯通过40-50℃水浴旋转蒸发仪迅速去除，产生一个黄色的固体残渣，将其溶解在95％的乙醇中，并可以在-25℃冷冻几个小时结晶。
得到的两种淡黄色晶体，熔点69-72℃，减压干燥，得到39-46g。
母液浓缩得到了一个油性残留物，放置在6× 80厘米，装有500克的硅胶和1:9（V/V）的洗脱乙酸乙酯- 正己烷的容器中。
第四版药学英语课后翻译（节选）
第四版药学英语课后翻译（节选）药学英语课后翻译Organic Chemistry Translation1. 没有化学的帮助，现代医学所取得的令人瞩目的进展是不可能的。
The remarkable advances made in modern medicine would not have been possible without the aid of chemistry.2. 既然人体从本质上讲是一台化学机器，那么，有人体功能的化学知识对医生来说就显得至关重要了。
Since the body is essentially a chemical machine, a knowledge of the chemistry of bodily functions seems essential to the physician.3. 通过植物和动物生产食品涉及到分子中原子的重新排列问题。
The production of food by plants and animals involves the rearrangement of atoms in molecules.4. 幸运的是，很少有其他工作能像研究化学那样更能激励人们去取得成功。
Fortunately, few kinds of work seem to urge people on to success more effectively than does the pursuit of chemistry.5. 迄今为止，寻求合成制品背后的动机便是祈盼以更少的钱为更多的人生产更好的东西。
So far the motive behind the search for synthetics has been a wish to produce better things for less money, and for more people.6. 人们从活体分离出越来越多的纯净物质，并认识到它们都含有碳元素，这样便诞生了有机化学Isolation of increasing numbers of purified materials from living forms and recognition of the fact that all contained carbon gave birth to organic chemistry.7. 煤与氧结合在炉中燃烧，生成二氧化碳——一种在成分和化学性质上都不同于煤和氧的全新物质。
(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》-闻韧主编第三章酰化反应-知识点总结
#2.11打卡# 完成学习目标第三章酰化反应Acylation Reaction1 定义：有机物分子中O、N、C原子上导入酰基的反应.2 分类：根据接受酰基原子的不同可分为：氧酰化、氮酰化、碳酰化3 用途：药物本身有酰基活性化合物的必要官能团结构修饰和前体药物羟基、胺基等基团的保护。
酰化机理：加成-消除机理加成阶段反应是否易于进行决定于羰基的活性：若L的电子效应是吸电子的，不仅有利于亲核试剂的进攻，而且使中间体稳定；若是给电子的作用相反。
根据上述的反应机理可以看出，作为被酰化物质来讲，无疑其亲核性越强越容易被酰化。
具有不同结构的被酰化物的亲核能力一般规律为；RCH2－＞R—NH－＞R—O－＞R—NH2＞R—OH。
在消除阶段反应是否易于进行主要取决于L的离去倾向：L-碱性越强，越不容易离去，Cl- 是很弱的碱，-OCOR的碱性较强些，OH-、OR-是相当强的碱，NH2-是更强的碱。
RCOCl＞(RCO)2O＞RCOOH 、RCOOR′ ＞RCONH2＞RCONR2′R: R为吸电子基团利于进行反应；R为给电子基团不利于反应R的体积若庞大，则亲核试剂对羰基的进攻有位阻，不利于反应进行酸碱催化碱催化作用是可以使较弱的亲核试剂H-Nu转化成亲核性较强的亲核试剂Nu-，从而加速反应。
酸催化的作用是它可以使羰基质子化，转化成羰基碳上带有更大正电性、更容易受亲核试剂进攻的基团，从而加速反应进行。
氧原子的酰化反应是一类形成羧酸酯的反应，是羧酸和醇的酯化反应，是羧酸衍生物的醇解反应醇的结构对酰化反应的影响伯醇(苄醇、烯丙醇除外）＞仲醇＞叔醇1) 羧酸为酰化剂：提高收率：(1)增加反应物浓度(2)不断蒸出反应产物之一(3)共沸除水、添加脱水剂或分子筛除水。
（无水CuSO4，无水Al2(SO4)3，(CF3CO)2O，DCC。
）加快反应速率:(1)提高温度(2)催化剂(降低活化能)催化剂(1)质子酸催化法: 无机酸：浓硫酸,氯化氢气体,有机酸：苯磺酸，对甲苯磺酸等。
药物合成反应(第三版_闻韧)第二章烃化反应
O C -CN -COOR' -COOH
O C3H7OH + CH3CH=CHCH
NaOH
CH3 C3H7OCHCH2CHO
CH3OCH2CH2CN
CH3OH+CH2=CHCN
NaOCH3 90℃ 1h
Organic Reactions for Drug Synthesis
(3)烷氧鏻盐为烃化剂
醇（伯醇、仲醇）+三苯基膦+偶氮二羧酸酯→ 烷氧鏻盐(R3P+OR′X-)
ArOH + ROH Ph3P/EtOOCN=NCOOEt
ArOR
EtOOCNHNHCOOEt+Ph3PO
Organic Reactions for Drug Synthesis
ii）当X相同时 卤代丙烯, 卤苄 > 卤代烷 > 卤芳烃ArX OEt Cl NaOH + EtOH 非那西丁中间体 NO2 NO2
当卤代烃为叔卤代烃时，不能在强碱下反应， 易消除HX，可在中性或弱碱性下反应。 CH3 CH2 B CH3 C + CH3-C CH3
Organic Reactions for Drug Synthesis
反应机理：b 碱催化
R'O R-CH-CH2 O O R-CH-CH R'OH
OR'
RCHCH2OR' O
RCHCH2OR'+ R'O OH
SN2 双分子亲核取代，立体位阻原因为
主，反应发生在取代较少的碳原子上。
药物合成反应(第三版)第一,二 三章课后翻译
第二章课后翻译Preparation of cyclopropane 1,1- dicarboxylic acid环丙烷1,1-二甲酸的制备(1). To a 1-L solution of aqueous 50% sodium hydroxide(Note 1), mechanically stirred in a 2-L, three-necked flask, was added, at 25°C, 114.0 g (0.5 mol) of triethylbenzylammonium chloride（TEBA三乙基苄基氯化铵）(Note 2).1L的50%氢氧化钠加入到2L的三口烧瓶中，加入TEBA三乙基苄基氯化铵114.0g（0.5mol）在25℃机械搅拌。
To this vigorously stirred suspension was added a mixture of 80.0 g (0.5 mol) of diethyl malonate and 141.0 g (0.75 mol) of 1,2-dibromoethane all at once.充分搅拌至混悬状，一次性加入丙二酸二乙酯80.0g（0.5mol）和1,2-二溴乙烷141.0个（0.75mol）的混合物。
The reaction mixture was vigorously stirred for 2 hr (Note 3).反应混合物强烈搅拌2小时。
The contents of the flask were transferred to a 4-L Erlenmeyer flask by rinsing the flask with three 75-mL portions of water.把烧瓶中的物质转移到4L的锥形瓶中，并用75ml清水洗涤烧瓶三次。
The mixture was magnetically stirred by dropwise addition of 1 L of concentrated hydrochloric acid.混合物在磁力搅拌下缓慢滴加浓盐酸。
药物合成反应(第三版_闻韧)第一章卤化反应
Organic Reactions for Drug Synthesis
例1.
C6H5 H
CC
H
COOC2H5
Br2 / CCl4
Br
C6H5
C
H C
H Br COOC2H5
C6H5 H CC
H Br COOC2H5
1. 卤素与烯烃的亲电加成反应
（1）反应历程： 第一步：卤正离子向π 键进攻，形成三员环卤正离子 或开放式碳正离子的过渡态。
R1 R3
R2
R4
δ +δ XX
Organic Reactions for Drug Synthesis
R1 R3 CC
R2 X R4
(1)
R1 R3
CC
R2
X R4
(2)
第二步：
反应类型
亲电加成 亲电取代 亲核取代 自由基反应
Organic Reactions for Drug Synthesis
常用的卤化剂 卤素（X2）：Cl2、Br2
次卤酸（HOX）：HOCl、HOBr
N-卤代酰胺：
如 N-溴（氯）代乙酰胺（ NBA，NCA） N-溴（氯）代丁二酰亚胺（NBS，NCS）
Ph H CC
H CH3
NBS / DMSO / H2O
OH
Ph
H
CC
H
Br CH3
NBS / 干燥的DMSO
O H
Ph C C Br CH3
Organic Reactions for Drug Synthesis
五、卤化氢与烯烃的加成
药物合成反应(第三版)第一章课后翻译
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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1、216-224g(1.62–1.68 moles)的无水三氯化铝。
While the free-flowing catalyst is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。
Near the end of the addition, the mass becomes molten and can be stirred easilygrams of heavy dark residue by distillation at reduced pressure. 乙醚在常压下蒸馏，微量的溴苯乙酮通过减压蒸馏的方法从大量深色残渣中被分离出来。
The colorless distillate is carefully fractionated to obtain 94–100 g.通过分馏，得到无色的流出液94-100g2、反应式：3、2-Methyl-4-ethoxalylcyclopentane-1,3,5-trione. A solution of sodium ethoxide is prepared in a 2-l. three-necked, round-bottomed flask fitted with amercury-sealed stirrer, a reflux condenser carrying a drying tube, and a stopper by the addition of 69.0 g. (3 moles) of sodium to 950 ml. of absolute ethanol. 69.0g （3mol）钠和950ml无水乙醇在配有干燥回流冷凝管和汞封搅拌器的2L三口圆底烧瓶中制备乙醇钠。
The solution is cooled to 0–5° in an ice bath and stirred.溶液在0-5℃下冰浴搅拌。
The stopper is replaced by a dropping funnel, and a cold mixture (5–15°) of 108 g. (1.50 moles) of freshly distilled 2-butanone and 482 g. (3.30 moles) of diethyl oxalate (Note 1) is added gradually over a period of 30 minutes.瓶塞用分液漏斗取代，108g（1.5mol）的丁二酮和482g（3.3mol）的乙二酸二乙酯在5-15℃下低温混合，在30分钟内逐步滴加到溶液中。
After the addition is complete, the thick, orange-red mixture is allowed to warm with continued stirring to room temperature, heated under reflux for 30 minutes, and cooled again to 0° in an ice bath. 完全加入后，橘红色的粘稠物继续搅拌至室温，加热回流30分钟后在冰浴中冷却至0℃。
The mixture is decomposed by stirring with 165 ml. of sulfuric acid (1:1 by volume) added in portions.将165ml浓硫酸（体积比1:1）在搅拌加入，分解混合物。
The sodium sulfateconcentrated by evaporation .合并滤液和洗涤液后蒸发浓缩。
The yellowish brown product which accumulates by slow crystallization is collected by filtration, washed with small quantities of ice-cold water, and dried in air. 过滤缓慢析出的棕黄色产品用小剂量的冰水洗涤后在空气中干燥。
The crude product weighs 140–150 g.粗产品140-150g。
Further evaporative concentration of the mother liquor followed by cooling furnishes an additional 40–50 g. of the keto ester, 此外将母液用冷冻蒸发浓缩后又得到40-50g的酮酯。
bringing the total yield to 180–200 g. (53–59%)产品总共180-200g（产率53-59%）(Note 2). This crude material (m.p. 120–130°) is used in the next step.粗品（熔点120–130℃）用于下一步中A pure sample can be obtained byThe procedure for 2- pyrrolealdehyde 2-吡咯甲醛In a 3-l. three-necked round-bottomed flask, fitted with a sealed stirrer, a dropping funnel, and a reflux condenser, is placed 80 g. (1.1 moles) of dimethylformamide (Note 1).在配有封闭搅拌器、滴液漏斗和冷凝回流装置的三口圆底烧瓶中放入80g（1.1mol）的二甲基甲酰胺。
The flask is immersed in an ice bath, and the internal temperature is maintained at 10–20°, while 169 g.(1.1 moles) of phosphorus oxychloride is added through the dropping funnel over a period of 15 minutes. 烧瓶浸入冰浴中，内部温度保持在10-20℃，169g（1.1mol）的磷酰氯通过滴液漏斗在15分钟内滴加。
An exothermic reaction occurs with the formation of the phosphorus oxychloride - dimethylformamide complex. 放热反应生成磷酰氯二甲基甲酰胺化合物。
The ice bath is removed, and the mixture is stirred for 15 minutes (Note 2). 移去冰浴，在搅拌15分钟。
The ice bath is replaced, and 250 ml. of ethylene dichloride is added to the mixture. 重新再冰浴下加入250ml的二氯乙烯。
When the internal temperature has been lowered to 5°, a solution of 67 g. (1.0 mole) of freshly distilled pyrrole in 250 ml. of ethylene dichloride is added through a clean dropping funnel to the stirred, cooled mixture over a period of 1 hour. 当内部温度降到5度时，把67g（1.0mol）新蒸馏的吡咯加入到250二氯乙烯中，通过滴液漏斗在1小时内低温下边搅拌边滴加。
After the addition is complete, the ice bath is replaced with a heating mantle, and the mixture is stirred at the reflux temperature for 15 minutes, during which time there is copious evolution of hydrogen chloride.滴加完后，用加热装置取代冰浴，搅拌回流15分钟，直到有大量氯化氢产生。
The mixture is then cooled to 25–30°, and to it is added through the dropping funnel a solution of 750 g. (5.5 moles) of sodium acetate trihydrate (Note 3) in about of water, cautiously at first, then as rapidly as possible. 当混合物降温到25-30℃后，通过滴液漏斗加入750g（5.5mol）的三水醋酸钠溶液，开始要小心，然后要尽可能地快。
The reaction mixture is again refluxed for 15 minutes, vigorous stirring being maintained all the while (Note 4). 反应物在充分搅拌下重新回流15分钟。