羧基化

Ethyl 4-[(1-hydroxy-1-methyl)ethyl]-2-propyl-1H-imidazole-5-carboxylate,the key intermediate of Olmesartan ,was synthesized from butanoic acid and o-phenylenediamine via condensation under microwave-irradiation,oxidation,esterification and the Gringard reaction.

用正丁酸与邻苯二胺为原料，在微波照射下缩合成2-丙基苯并咪唑，再氧化开环制得2-丙基咪唑二羧酸，再经酯化、Gringard反应制得抗高血压药物奥美沙坦的关键中间体2-丙基-4-[(1-羟基-1-甲基)乙基]-1H-咪唑-5-羧酸乙酯，总收率32.2%。

For developing an immunoassay for multiple residues of pyrethroid pesticides, the hapten N-2- carbanmoyl-(3"-phenoxyphenyl) methyl 3-(2"-Cldoro-3",3",3"-trifluoropropenyl)-2, 2-dimethylcyclopropane- carboxylate was synthesized from cyanohydrin and 3-(2"-Chloro-3",3",3- trifluoropropenyl)-2, 2-dimethylcyclopropanecarboxylic acid via hydrolysis and esterification. The synthesis of the hapten was foundation of preparaing anti- cyhalothrin polyclonal antibodies.

为了制备对单一拟除虫菊酯高特异性的抗体，以菊酸和氰醇为起始原料，通过水解、酯化反应合成了半抗原N-2-氨甲酰-(3-苯氧基苄基)甲基-3-(2-氯-3，3，3-三氟丙烯基)-2，2-二甲基环丙烷羧酸酯，为进一步制备抗三氟氰菊酯的特异性抗体奠定基础。

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。

Purified protein samples were separated by 2-DE with 17 cm IPG strips, and the protein spots were detected by fast silver staining. Six protein spots were randomly excised from the silver stained gel for primary analysis by MALDI-TOF MS. Four proteins were identified, and they were 1-aminocyclopropane-1-carboxylate synthase 2, ribulose-1, 5-bisphosphate carboxylase/oxygenase large subunit, F11O4.2 and Rubisco small subunit.

根据预实验结果，选用17 cm IPG预制干胶条对纯化的蛋白样品进行2-DE实验，采用快速银染法进行染色，随机挖取银染胶上6个蛋白点进行MALDI-TOF MS分析和数据库检索，鉴定了3个蛋白，它们是：1-氨基环丙烷-1羧酸合酶2，核酮糖-1，5-二磷酸羧化酶/加氧酶大亚基和F11O4.2。

It was found the levels of both large and small subunits were low at the albescent stage and became normal after leaves recovered to green, which corresponded with the enzyme activity change.

发现安吉白茶在返白与复绿过程中叶片可溶性蛋白的主要变化是RuBP羧化酶大、小亚基含量上的差异，这种差异与RuBP羧化酶活性的变化是相一致的。

The variation of large and small subunits of RuBPcase from temperature-sensitive mutant of Anjibaicha during its stage albescent process was investigated as well as the changes of the enzyme activities.

利用SDS-PAGE电泳分析了返白和复绿过程中各阶段叶片可溶性蛋白组分，尤其是RuBP羧化酶大、小亚基的变化，并利用同位素法测定了此过程中RuBP羧化酶活性的变化。

The same time to early albescent stage; FA: The same time to fully albescent stage;FG: The same time to fully green stage;LS: The large subunit of RuBPcase; SS: The small subunit of RuBPcase

相当于白茶返白初期； FA：相当于白茶全白时期；FG：相当于白茶全复绿时期；LS：RuBP羧化酶的大亚基；SS：RuBP羧化酶的小亚基

Firstly, 3-ethylthiobutanal was prepared from crotonaldehyde reacting with ethanehiol in triethylamine with high yield. Secondly, methyl acetoacetate was converted to 6-ethylthiohept-3-en-2-one by three steps via hydrolysis, condensation with 3-ethyltio-butanal and dehydration, then 6-ethylthiohept-3-en-2-one was cycloco ndensed with dimethyl malonate by Michael addition and Claisen condensation, followed by saponification and decarboxylation to give the intermediate of 5-(2-ethylthiopropyl)-cyclohexane-1,3-dione.

首先，以巴豆醛与乙硫醇为原料，在三乙胺的催化作用下高收率制得3-乙硫基丁醛；然后从乙酰乙酸甲酯出发，通过碱水解、与3-乙硫基丁醛缩合、脱水三步反应合成6-乙硫基-3-烯-2-庚酮，接着6-乙硫基-3-烯-2-庚酮与丙二酸二甲酯通过Michael加成和Claisen缩合成环，再通过皂化和脱羧反应生成中间体5-[2-丙基]-1，3-环己二酮；再与丙酸酐反应丙酰化，最后与0-3-氯-2-丙烯基羟胺肟化，得到目标化合物烯草酮。

In this report, half-esterification between these pendent hydroxyl groups of hydroxyl-PU and maleic anhydride could lead to new pendent groups, carboxylic groups. These highly polar carboxylic groups in the side chain of PU could play the role of internal emulsifier. They had self-dissociation ability in the water or were neutralized first by appropriate amount of base. Then, PU bearing carboxylic group could dispersed steadily in the water, named aqueous-based polyurethane dispersion.

在本论文中，利用原来亲油性Hydroxyl PU主链段上悬挂的羟基经由与琥珀酸酐的半酯化(Half-esterification Reaction)反应后，使PU在侧链上悬挂具有强极性的羧酸基，其可作为聚胺酯分子中的内乳化剂，羧酸基能在水相中自身解离产生离子或加入适量碱使之中合，使聚氨酯高分子能够稳定分散於水中，即所谓水性PU分散液(Aqueous-based Polyurethane Dispersion)。

Do you know, i need you to come back

你知道吗，我需要你回来

Yang yinshu、Wang xiangsheng、Li decang,The first discovery of haemaphysalis conicinna.

1〕 杨银书，王祥生，李德昌。安徽省首次发现嗜群血蜱。