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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%。

According to the theoretic significance and the applications of the complexes, this paper mainly concluded the following work: The ligand, 2-carboxybenzaldehyde-2,4-dinitrophen hydrazone, was synthesized by 2-carboxybenzaldehyde and 2,4-dinitrophenyl hydrazine in absolute alcohol.

中文摘要本文基于芳香腙类化合物的抑菌活性、稀土元素的生物活性以及二者配位后可能的协同效应,主要进行了以下几个方面的工作:在无水乙醇中,利用2-羧基苯甲醛和2,4-二硝基苯肼缩合反应得到了配体2-羧基苯甲醛-2,4-二硝基苯腙(C14H10N4O6)。

DBP and DEHP have the similar photodegradation mechanism. The predominant pathway for DBP and DEHP photodegradation in the Fe -oxalate complexes system is hydroxyl radical extracting H atom in α-position of the aliphatic chain close to the carboxyl group followed by oxidation to produce alcoholized derivatives ROH. ROH then breaks down to phthalic acid and dialcohol that will be further oxidized up to mineralization.

DBP和DEHP的光降解历程相似,主要反应途径是OH自由基提取烷基上与羧基相连的α-H原子,然后被氧化生成醇衍生物,再分解成为酞酸和二醇,酞酸经历开环和进一步脱羧,二醇可以被氧化成为低级烷基羧酸,直至矿化。

From the structural analysis of three praseodymium complexes, we could draw a conclusion that as the dentate arms of carboxyl group on ligands elongating, the coordination numbers of Pr and the coordination modes of ligands increase, and the mean distances between metallic atoms of metallic helices existing in these complexes augment.2. By altering 5-substituting group of isophthalic acid three series of lanthanide complexes 8~19 with 5-methylisophthalic acid and 5-nitroisophthalic acid have been prepared.

从得到的三个配体的镨配合物的结构分析可以看出,随配体的羧基齿臂的增长,Pr的配位数逐渐增大,配体的配位模式增多,配合物中存在的螺旋金属链中的金属间平均距离增大。2、通过改变间苯二甲酸配体的5位取代基,制备了5-甲基间苯二甲酸和5-硝基间苯二甲酸的三个系列稀土羧酸配合物8~19。

In this paper,pyromellitic dianhydride,1,2,3,4-cyclobutanetetracarboxylic dianhydride,4[(4-aminophenyl)-bis(4-methoxyphenyl)methyl]benzeneamine,4-hexyloxy-biphenyl-3′,5′-diaminobenzoate,and additive ADD-34 were used to synthesize four PIs.

文章用均苯四甲酸二酐,4[(4-氨基苯基)-二(4-甲氧基苯基)甲基]苯胺,1,2,3,4-环丁烷四羧酸二酐,4-己烷氧基联苯酚-3′,5′-二胺基苯甲酸酯和不同含量的添加剂制备了聚酰亚胺液晶取向剂。

The present invention concerns the compounds having the formula N-oxides, salts, stereoisomeric forms, racemic mixtures, prodrugs, esters and metabolites thereof, wherein R1 and R8 each are H, optionally substituted C1-6alkyl, C2-6alkenyl, C3-7cycloalkyl, aryl, Het1, Het2; R1 may also be a radical of formula (R11aR11b)NC(R10aR10b)CR9-; t is 0, 1 or 2; R2 is H or C1-6alkyl; L is -C-,-O-C-,-NR8-C-,-O-C1-6alkanediyl-C-,-NR8-C1-6alkanediyl-C-,-S2-,-O-S2-,-NR8-S2 ; R3 is C1-6alkyl, aryl, C3-7cycloalkyl, C3-7cycloalkylC1-4alkyl, or arylC1-4alkyl; R4 is H, C1-4alkylOC, carboxyl, aminoC, mono- or di(C1-4alkyl)aminoC, C3-7cycloalkyl, C2-6alkenyl, C2-6alkynyl or optionally substituted C1-6alkyl; R5 and R6 are H or C1-6alkyl.

本发明涉及右式化合物其N-氧化物、盐、立体异构形式、外消旋混合物、前药、酯及代谢物,其中R 1 及R 8 各是氢、C 1-6 烷基、C 2-6 烯基、C 3-7 环烷基、芳基、Het 1 、Het 2 ;R 1 也可以是式(R 11a R 11b )NC(R 10A R 10b )CR 9 -之基;t是0、1或2;R 2 是氢或C 1-6 烷基;L是-C-、-O-C-、-NR 8 -C-、-O-C 1-6 烷二基-C-、-NR 8 -C 1-6 烷二基-C-、-S 2 -,-O-S 2 -、-NR 8 -S 2 -;R 3 是C 1-6 烷基、芳基、C 3-7 环烷基、C 3-7 环烷基C 1-4 烷基或芳基C 1-4 烷基;R 4 是氢、C 1-4 烷基OC、羧基、氨基C、一-或二(C 1-4 烷基)氨基C、C 3-7 环烷基、C 2-6 烯基、C 2-6 炔基或任选被取代的C 1-6 烷基;R 5 及R 6 是氢或C 1-6 烷基。

A compound of formula wherein R1 is hydrogen, halo or methoxy; R2 is hydrogen, halo, methyl, ethyl or methoxy; R3 is carboxy, tetrazolyl, or -CONHSO2R where R is methyl, ethyl, phenyl, 2,5-dimethylisoxazolyl or trifluoromethyl; T is -CH2- or -SO2-; and ring A is 3-chlorophenyl, 4-chlorophenyl, 3-trifluoromethylphenyl, 3,4-dichlorophenyl, 3,4-difluorophenyl, 3-fluoro-4-chlorophenyl, 3-chloro-4-fluorophenyl or 2,3-dichloropyrid-5-yl; or a pharmaceutically acceptable salt or prodrug thereof, as well as pharmaceutical compositions containing them are described and claimed.

本发明涉及一种式化合物,其中R 1 是氢原子、卤素或甲氧基;R 2 是氢原子、卤素、甲基、乙基或甲氧基;R 3 是羧基、四唑基或-CONHSO 2 R 4 ,其中R 4 是甲基、乙基、苯基、2,5-二甲基异∴唑基或三氟甲基;T是-CH 2 -或-SO 2 -;环A是3-氯苯基、4-氯苯基、3-三氟甲基苯基、3,4-二氯苯基、3,4-二氟苯基、3-氟-4-氯苯基、3-氯-4-氟苯基或2,3-二氯吡啶-5-基;或其药用允许的盐或前药,还包括所阐述和要求权利的含有它们的药用组合物。

A novel method combining a conventional free-radical solution polymerization with a chemical saponification was used to synthesize a, cu-dicarboxyl terminated oligo s with molecular weight below 1500. Here, cn-carboxyl terminated oligo s were firstly synthesized by the free-radical polymerization in THF, where 4,4'-azobis(4-cyanovaleric acid) was used as initiator, thioglycolic acid as chain transfer agent, then CTBMA were transformed into di-CTBMA via saponifying CTBMA in dioxane/H_2O/KOH solution.

利用传统自由基聚合法,在四氢呋喃溶液中自由基引发聚合甲基丙烯酸丁酯单体而得到w-羧基-甲基丙烯酸丁酯低聚物(分子量在1500左右);利用CTBMA 末端酯基的反应特性,在二氧六环/水/KOH混合溶液中皂化CTBMA,使之转化为a ,w-羧基甲基丙烯酸丁酯低聚物;研究了溶剂的类别、反应时间等反应条件对皂化产物结构的影响;利用MALDI-TOF-MS及LSIMS对皂化各阶段产物进行了分析监测。

The latter is chlorinated in the side chains under free-radical conditions to give 2,4-dichloro-5-fluoro-3-dichloromethyl-1-trichloromethylbenzene. The latter is hydrolysed via 2,4-dichloro-5-fluoro-3-dichloromethylbenzoic acid, which can be isolated if necessary, to give 2,4-dichloro-5-fluoro-3-formyl-benzoic acid, the aldehyde group of which is reacted to give 2,4-dichloro-5-fluoro-3-N-hydroxyiminomethyl-benzoic acid, from which, with simultaneous conversion of the carboxyl group into the chlorocarbonyl group, water is eliminated using an acid chloride to give the nitrile 2,4-dichloro-3-cyano-5-fluoro-benzoyl chloride.

随后,在游离基条件下进行侧链的氯化,得到2,4-二氯-5-氟-3-二氯甲基-1-三氯甲基苯、后者被水解,经过2,4-二氯-5-氟-3-二氯甲基苯甲酸(如果需要此化合物可以分离),得到2,4-二氯-5-氟-3-甲酰苯甲酸,将其醛基反应,得到2,4-二氯-5-氟-3-N-羟基亚氨基甲基苯甲酸,用酰氯从其中除去水,同时将羧基转化为碳酰氯,得到一种腈,即2,4-二氯-3-氰基-5-氯-苯甲酰氯。

By synthesizing the hapten LBc starting from the metabolite of bifenthrin (2-methyl-3-phenylbenzyl alcohol), LBs (2-methyl[1,1-biphenyl]-3-ylmethyl 3-carboxyl-2,2-dimethylcyclopropane carboxylate and Lby (2-methyl[1,1-biphenyl]-3-ylcarboxylic acid , Three haptens were praparaed which were used in next step.

利用联苯菊酯的代谢物联苯醇合成了联苯菊酯的半抗原LBc(2-甲基-3-苯基苄基氧基羰基丙酸)、LBs(2-甲基-3-苯基苄基-3-羧基一2,2-二甲基环丙烷羧酸)和LBy(2-甲基-3-苯基苯甲酸)。

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