酰化

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)。

Besides,through Arbuzov reaction,Vilsmer-Haack Hydroformylation,Wittig-Horner reaction,nitryl hydrogenation deoxidize,and imidization five steps synthesized another compound which included hole-transporting,electron-transporting and luminescence materials.

此外，又通过Arbuzov反应、Vilsmer-Haack甲酰化反应、Wittig-Horner反应生成二苯乙烯、硝基加氢还原、酰亚胺化5步反应合成了一种集空穴传输-电子传输-发射三位一体的新型苝酰亚胺化合物。

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。

In general, the phosphoamino acid esters were unable to transfer their phosphoryl group to other hydroxyl nucleophiles even with the presence of imidazole, but the N-phosphoserine and threonine esters were two exceptions.

二、测定了部分磷酰化D—氨基酸的磷酰基转移反应速率常数，并对外消旋化合物的酯交换反应进行了旋光度跟踪，发现磷酰化丝、苏氨酸的对映体有明显的区别。

In the study of peptide formation from phosphoryl aspartic acid with ethyl alanine, the N-phosphoryl peptide ester was isolated and identified by 1D and 2D NMR. It was found that only α-dipeptide ester, no β-dipeptide ester, was formed in the reaction.

实验发现N-磷酰化极性氨基酸在没有活化剂、缩合剂的水溶液中能够发生成肽反应，且生成的磷酰化二肽具有方向性：成肽产物的N端氨基酸来自N-磷酰化氨基酸，成肽反应发生在其C端。

Amino to acetyl phenol, in have technology of two kinds of production domestic and internationally, acetic anhydride craft of the United States, acyl changes temperature to have 75 ℃ only, acyl changes mother liquor not apply mechanically, deputy reaction is little, of production thick tasting is kind of white almost, purificatory craft is very simple, activated carbon dosage only 2~3%, the Kun that its product does not have glow material almost in different third alcohol inferior the sealed impurity of amine impurity and minim, settleclear lightness it may not be a bad idea, the product quality that acetic anhydride craft produces is good, but close rate low, cost is high.

对乙酰氨基酚，在国内外有两种生产工艺，美国的醋酐工艺，酰化温度只有75℃，酰化母液不套用，副反应少，生产的粗品几乎是类白色，精制工艺就非常简单，活性炭用量仅2~3%，其产品在异丙醇中几乎无红光物质的醌亚胺杂质及微量的未知杂质，澄明度也好，醋酐工艺生产的产品质量好，但收率低、成本高。

A series of 2-oxocyclododecyl sulfonylurea s have been synthesized from 2-oxocyclododecylsulfonamide via acylation of phenyl chloroformate and amination.

以环十二酮为起始原料，经磺化反应制备得到2-氧代环十二烷基磺酸盐B，B经过氯化和胺解反应制备得到2-氧代环十二烷基磺酰胺C，C经过苯氧酰化与胺解反应后合成了10个新的2-氧代环十二烷基磺酰脲类化合物D，它们的结构通过了1HNMR和IR的确证。

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。

Spiral Spirobifluorene acetylated is oxidated by m-chloroperoxybenzoic acid and hydrolyzed by sodium hydroxide ,obtaining 2,2 '- dihydroxy -9,9'- spiral Spirobifluorene .Through nitrification,Reduced by hydrazine hydrate, we may get the 2,2 '- diamino -9,9'- spiral Spirobifluorene which are characterizated by IR, 1H-NMR !

L-酒石酸和乙醇酯化得到酒石酸二乙酯，将保护羧基保护起来，然后用碘甲烷在2，3-位上两个甲基，得到2，3-二甲氧基-酒石酸二乙酯，再用氢氧化钠将其水解，得到2，3-二甲氧基-酒石酸，用五氯化磷将羧基酰化，得到2，3-二甲氧基- 1，4-丁二酰氯，经过与二环己胺反应，得到拆分配体2，3-二甲氧基–N，N，N'，N'-四环己丁二酰胺。

By the time of its fall, most of the prisoners were writers who had written against the corruptions of the government.

到它被攻陷的时候，里面多数的犯人是写了反对政府贪污文章的作家。

The most obvious variation to ovum morphological character was that the color was changed from light green to sepiaceous in embryonic development, and all the ovums were almost hatched after 96h.

在胚胎发育过程中卵的形态特征最明显的变化是颜色从淡绿到深褐色，卵在发育96h后卵基本全部孵化。