药物合成反应(第三版)第二章课后翻译
药物合成反应课后翻译
1、216-224g(1.62–1.68 moles)的无水三氯化铝。
While the free-flowing catalyst isfunnel 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 easily without being either heated or cooled. The molten mass, in which thebrown.当快滴加完时，团块开始融化，表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。
药物合成反应(第三版)第二章课后翻译
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。
药物合成反应课后翻译
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。
Whilefrom 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 easily without being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。
Bromine (128 g., mole) is added dropwise to the well-stirred mixture over a period of 40 minutes (Note 4). 在40分钟内在搅拌下把溴缓慢滴加到混合物中。
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。
(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。
药物合成反应课后翻译
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。
《药物合成反应》第二章 烃化反应
药物合成反应
• 影响因素 催化剂的影响
有些有旋光活性的醇，如果加金属钠制成醇钠，再与卤代烃 反应，产物比较复杂，如用氢化钠，则可立体专一性地得到相 应的甲醚（ 2 ）或（ 4 ）
药物合成反应
芳香卤化物也可作为烃化剂，生成芳基烷基混合醚。通常情 况下，由于芳卤化物上的卤素与芳环共轭不够活泼，一般不易反 应。但当芳环上在卤素的邻对位有吸电基存在时，可增强卤原子 活性，能顺利地与醇羟基进行亲核取代反应而得到烃化产物
药物合成反应
第一节氧原子上的烃化反应
一 醇的O-烃化
1 卤代烷为烃化剂 2 磺酸酯 3 环氧乙烷类作烃化剂
4 烯烃作为烃化剂 5 醇作为烃化剂 6 其它烃化剂
二 酚的O-烃化
1 烃化剂 2 多元酚的选择性烃化
药物合成反应
第一节 氧原子上的烃化反应
一 醇的O-烃化
1 卤代烷为烃化剂：
• 通式
ROH + B
R'O
C
X
HH
伯卤代烷RCH2X按SN2历程
R'O-CH2R + X 构型翻转
随着与X相连的C的取代基数目的增加越趋向SN1
药物合成反应
第一节 氧原子上的烃化反应
一 醇的O-烃化 1 卤代烷为烃化剂：醇在碱的条件下与卤代烷生成醚
• 影响因素 a RX的影响
i） 当R相同C-X极化度 活性
活性：RI>RBr>RCl>RF 成本：RI>RBr>RCl
（∵卤素的电负性）
药物合成反应
第一节 氧原子上的烃化反应
一 醇的O-烃化 1 卤代烷为烃化剂：醇在碱的条件下与卤代烷生成醚
• 影响因素 a RX的影响
药物合成反应课后翻译
1、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。
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。
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 easily without being eitherranges in color from tan to brown.当快滴加完时，团块开始融化，表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。
Bromine (128 g., 0.80 mole) is added dropwise to the well-stirred mixture over a period of 40 minutes (Note 4). 在40分钟内在搅拌下把溴缓慢滴加到混合物中。
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。
药物合成反应与设计翻译部分
药物合成反应与设计翻译部分（第三版闻韧主编）第一章翻译：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。
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。
药物合成反应(第三版)
Br
Br
Br
Br
(选 择 性 溴 化 试 剂 )
第三节 羰基化合物的卤代反应
一、醛酮α-位氢的卤代反应
选择性溴化剂
O CH3 O Br Br O O Br CH3 CH3 CH3 O CH-Ar Br O CH-Ar
第一节 不饱和烃的卤加成反应
• 加卤素
C C X2 C X C X
概述
X2=Cl2, Br2
• 加卤化氢
C C HX C H C X HX=HCl, HBr, HI
无过氧化物 CH3CH=CH2
CH3CHBrCH3
Markovnikov加 成 反Markovnikov加 成
过氧化物
CH3CH2CH2Br
一、醛酮α-位氢的卤代反应
1,3二羰基化合物
O O H3C C CHCCH3 Cl
O
O
H3C C CH2CCH3
CF3SO2Cl Et3N
第三节 羰基化合物的卤代反应
一、醛酮α-位氢的卤代反应
α-羰基自由基取代
O
游离基反应促进剂 选择性地对烷基取代较多的α -H进行溴代
O Br C R''' R''
E π-络 合 物
X+-X-
H X -H+
σ-络 合 物
CH3 CH3 Cl + CH3 2mol Cl CH3 Br2 /Fe Br + Br CH3 Cl Cl
X
H
CH3
Cl2 /Fe
例
+
第二节 烃类的卤代反应
二、芳烃卤代反应（亲电取代）
OH H2O 3Br2 OH H2O 2Br2 Br