苯酰化

Methods Starting from 2-chloro-4-nitrophenol and 2- pyridine hydrochlorid, 3-chloro-4-(pyridin-2-ylmethoxy) aniline was obtained via etherization and reduction. The obtained aniline coupled with N-(4-chloro-3-cyano-7-ethoxyquinolin-6-yl) acetamide to give 4-[3-chloro-4-(2-pyridylmethoxy) phenylamino]-3-cyano-7-ethoxy-6-N-acetylaminoquinoline. And then it was deacetylated, followed by reacting with4- but-2-enoyl chloride to yield the target compound neratinib.

以2-氯－4-硝基苯酚和2-氯甲基吡啶为起始原料，经醚化、硝基还原得到3-氯－4-（吡啶－2-甲氧基）苯胺，3-氯－4-（吡啶－2-甲氧基）苯胺与3-氰基－6-乙酰氨基－7-乙氧基－4-氯喹啉反应得到3-氰基－6-乙酰氨基－4-［3-氯－4-（吡啶－2-甲氧基）苯氨基］－7-乙氧基喹啉，3-氰基－6-乙酰氨基－4-［3-氯－4-（吡啶－2-甲氧基）苯氨基］－7-乙氧基喹啉去乙酰保护基后，与-4-二甲氨基－2-丁烯酰氯经酰化反应得到ner-atinib。

Teflubenzuron was synthesized from 2,4-difluoronitrobenzene and 2,6-dichlobenil as starting reagent through six-step reaction with the yield of 75.3%.3,5-Dichloro-2,4-difluoroaniline was synthesized by chlorination,reduction reaction from 2,4-difluoronitrobenzene,the yield was 84.5%;2,6-difluorobenzamide with the yield of 87.7% was synthesized by fluoridation and hydrolysis from 2,6-dichlobenil.

以2，4-二氟硝基苯和2，6-二氯苯腈为起始原料，经过6步反应合成伏虫隆，总收率为75.3%。以2，4-二氟硝基苯为原料，经过氯化、还原反应合成3，5-二氯-2，4-二氟苯胺，产率为84.5%；以2，6-二氯苯腈为原料，经过氟化和水解，制得2，6-二氟苯甲酰胺，产率为87.7%；将Ⅱ与二碳酸酯酰化，合成2，6-二氟苯甲酰异氰酸酯，产率为91.3%；Ⅲ与Ⅰ加成，得到杀虫剂伏虫隆，产率为95%。

Methods 4-Hydroxybenzonitrile (2) as the starting material was transformed to 4-hydroxy-thiobenzamide (3) via thioformylation. And ethyl 2-(4-hydroxyphenyl)-4-methylthiazole-5-carboxylate (4), which was synthesized via cyclization from 3, was treated with hexamethylenetetramine to generate the intermediate ethyl 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylate (5). The target compound febuxostat (1) was obtained from 5 by etherification, cyanidation, hydrolysis.

以羟基苯腈为原料，经硫代甲酰化得到对羟基硫代苯甲酰胺(3)，3经环合得到2-（4-羟基苯基）－4-甲基－噻唑－5-羧酸乙酯(4)，4与乌洛托品反应，得到中间体2-（3-甲酰基－4-羟基苯基）－4-甲基－噻唑－5-羧酸乙酯(5)，之后再经醚化、氰化、水解得到目标产物(1)。

ABSTRACT Immobilized penicillin acylase (from E.coli) was used to catalyze 7 phenylacetamido 3 E propenyl cephalosporanic acid hydrolyzation into 7 amino 3 E propenyl cephalosporanic acid. Then, trans APRA was acylated with hydroxyethyl ester of 4 hydroxy D phenylglycine to obtain trans cefprozil.

以7 苯乙酰氨基 3 E 丙烯基 3 头孢菌素 4 羧酸为原料，在青霉素酰化酶作用下，首先酶法水解得到3 E 丙烯基 3 头孢菌素 4 羧酸，过滤固相酶，滤液调pH分离得到反式APRA固体；在青霉素酰化酶作用下，反式APRA再与对羟基苯甘氨酸乙二醇酯缩合，得到反式头孢丙烯；酶法合成所得的产品与进口反式头孢丙烯对照品一致。

Bis-(4-bromobenzoyl) benzene as the monomer of poly was synthesized by Friedel-Crafts benzoylation reaction. Poly-Ⅱ synthesized via palladium-catalyzed aryl amination reaction using 1, 4-bis-(4-bromo-benzoyl) benzene and 4, 4'-diaminodiphenyl ether as monomers.

通过傅－克酰基化反应合成了1，4-双－（4'-溴苯酰基）苯，以1，4-双－（4'-溴苯酰基）苯和4'4-二氨基二苯醚为单体，通过钯催化的胺基化缩聚反应合成了高性能聚合物－聚亚胺酮－Ⅱ。

In the fifth chapter, a series of betulin derivatives including 28-acetoxybetulin, 28-tritylbetulin, 28-benzoylbetulin, 3-0-P-D-glucopyranoside of betulin and some betulinic acid conjugate containing amino acid were synthesized and confirmed by MS and NMR.

第五章分别合成得到了乙酰化白桦酯醇、28-苯甲酰化白桦酯醇、28-三苯甲基化白桦酯醇、3-O-β-D-glucopyranoside of betulin和一系列的白桦酯酸苷氨酸的衍生物，并分别对其进行了结构鉴定。

Gemini surfactant, sodium oleoylamidodiphenyl ether disulfonate was synthesized from p-nitrodiphenylether,oleoyl choride and chlorosulphonic acid through nitro-group reduction,acylation and sulphonation.

以对硝基二苯醚、油酸酰氯、氯磺酸为主要原料，通过硝基还原反应、胺基酰化反应、磺化反应，合成了双子表面活性剂油酸酰胺基二苯醚双磺酸钠；并用IR，1HNMR，MS对产品及中间体结构进行了表征。

A process for preparingp-fluo-2-(2-methyl-3-propionyl)-4-oxy-N,3-diphenyl-phenylbutylamide includes such steps as Friedle-Craft acylating of newly prepared phenylacetyl chloride and fluorobenzene under catalysis of AlCl3 to obtain 4-fluoro-phenylbenzyl ketone, brominating at carbonyl alpha position under catalysis of less AlCl3 to obtain alpha-bromo-4-fluo-phenylbenzyl ketone, and condensing with isobutyryl acetanilide under action of sodium ethoxide.

本发明涉及一种制备对氟－2－(2－甲基－3－氧丙基)－4－氧－N，3－二苯基－苯丁酰胺(1)的方法，其包括以下步骤：新制的苯乙酰氯与氟苯在AlCl3催化下进行Friedle－Craft酰化反应，得到对4－氟－苯基苄基酮(4)；化合物(4)在少量AlCl3催化下进行羰基α位溴化，得到α－溴－4－氟－苯基苄基酮(5)；然后(3)异丁酰乙酰苯胺在乙醇钠作用下与化合物(5)进行缩合。

Part I, the Friedel-Crafts acylation on DAA and methyl dehydroabietic acid was carried out with acetyl chloride, benzoyl chloride or phthalic anhydride as acylating regents, anh- ydrous aluminum chloride as catalyst and with different solvents to compare with, we have got t- hree new compounds.

第一部分，分别以脱氢松香酸和脱氢松香酸甲酯为底物，乙酰氯、苯甲酰氯、邻苯二甲酸酐为酰化试剂，无水三氯化铝作催化剂，采用不同的溶剂及反应条件进行傅克酰基化反应，得到3个新化合物。

Methyl phenyl glyoxylate was prepared firstly by reaction of 2-methyl benzoyl chloride with NaCN. The reaction of 2-methyl phenyl glyoxylate with methanol gave the target product methyl 2-methyl phenyl glyoxylate. An improved 3 step synthetic method of methyl 2-methyl phenyl glyoxylate was studied. The optimization conditions were presented.

以2-甲基苯甲酸为原料，酰化后与氰化钠反应生成2-甲基苯甲酰腈，经甲酯化生成2-甲基苯甲酰甲酸甲酯，改进了三步合成2-甲基苯甲酰甲酸甲酯的方法，并对反应时间、反应温度等影响因素进行了优化，确定了合成反应中的最优化条件。

We have no common name for a mime of Sophron or Xenarchus and a Socratic Conversation; and we should still be without one even if the imitation in the two instances were in trimeters or elegiacs or some other kind of verse--though it is the way with people to tack on 'poet' to the name of a metre, and talk of elegiac-poets and epic-poets, thinking that they call them poets not by reason of the imitative nature of their work, but indiscriminately by reason of the metre they write in.

索夫农 、森那库斯和苏格拉底式的对话采用的模仿没有一个公共的名称；三音步诗、挽歌体或其他类型的诗的模仿也没有——人们把&诗人&这一名词和格律名称结合到一起，称之为挽歌体诗人或者史诗诗人，他们被称为诗人，似乎只是因为遵守格律写作，而非他们作品的模仿本质。

The relationship between communicative competence and grammar teaching should be that of the ends and the means.

交际能力和语法的关系应该是目标与途径的关系。