酰氨基

Odoquinazolin-4(3H)-one,7-methyl-4(3H)-quinazolinone,7-bromoquinazolin-4(3H)-one were synthesized by using anthranilic acid、2-amino-5-nitrobenzoic acid、2-amino-4-nitrobenzoic acid,6-nitro--4(3H)-quinazoline-one、o-amino-terephthalic acid, 2-amino-4-hydroxy benzoic acid、2-amino-5-bromo-benzoic acid、2-amino-5-iodine acid,1、4-butynediol、L-glutamine、isatin anhydride、formamide as starting materials and utilizing microwave-assisted synthetic approach.

本文利用微波辅助合成的方法，以邻氨基苯甲酸、2-氨基-5-硝基苯甲酸、2-氨基-4-硝基苯甲酸、邻氨基对苯二甲酸、2-氨基-4-羟基苯甲酸、2-氨基-5-溴苯甲酸、2-氨基-5-碘苯甲酸、5-甲基-2-氨基苯甲酸等为原料与甲酰胺反应，以及以1，4-丁炔二醇、L-谷氨酰胺与靛红酸酐反应，共合成了13个喹唑啉酮衍生。。。

The famciclovir was synthesized from purine by a series of steps by Acylation, Decarboxylation, Reduction ,and so on; Derivatives of these intermediates is described from the 6-chloro- 9H- purin-2-amine as raw materials in different conditions when the iodine and bromide were synthesized with the addition of two intermediate 6-bromo-9H-purin-2-amine and 6-iodo-9H-purin-2-amine; There is elaborated from the main part of a acetophenone, urineaminohydrochloride, phenylhydrazine, ethyl acetoacetate as raw material through a series of reactions to synthetic 3-phenyl-4-formylphenyl pyrazole and 5-chloro-3-methyl-1-phenyl-1H-pyrazole-4-aldehyde two pyrazole aldehyde, and then with 2-amino-6-chlorine-9-(2-methicillin-oxo-co-methyl-4-yl) purine reaction of the two new pyrazole purine Schiff bases.

本论文主是采用以鸟嘌呤为原料，经过一系列的酰基化，脱羧，还原等反应作用下最终得到了产物2-氨基-9-(4-乙酰氧基-3-乙酰氧基甲基丁基)嘌呤；其中的中间体衍生物主要是阐述从以2-氨基-6-氯鸟嘌呤为原料通过在不同的条件下进行溴代与碘代分别合成了另外两种中间体2-氨基-6-溴鸟嘌呤及2-氨基-6-碘鸟嘌呤；还有一部分主要是阐述从以苯乙酮，盐酸氨基脲，苯肼，乙酰乙酸乙酯为原料通过一系列的反应先合成3-苯基-4-醛基吡唑及5-氯-3-甲基-1-苯基-1H-吡唑-4-甲醛这两个吡唑醛，然后再与2-氨基-6-氯-9-(2-甲氧羰基丁酸甲酯-4-基)嘌呤反应得到了两个新型的吡唑嘌呤席夫碱

In the first part, five new 4-acyl pyrazolone 4-ethyl-thiosemicarbazones compounds: 1-Phenyl-3-methyl-4-(4-bromo)benzal-pyrazol-5-one N(4)-ethyl-thiosemicarbazone (PM4Br BP-ETSC), 1-Phenyl-3-methyl-4-(4-methyl)benzal-pyrazol-5-one N(4)-ethyl-thiosemicarbaz -one (PM4MBP-ETSC), 1-Phenyl-3-methyl-4-benzal-pyrazol-5-one N(4)-ethyl-thiosemicarba -zone, 1,3-diphenyl-4-benzal-pyrazol-5-one N(4)-ethyl-thiosemicarbazone and 1-Phenyl-3-methyl-4-phenylacetyl-pyrazol-5-one N(4)-ethyl-thiosemi -carbazone have been synthesized and characterized by elemental analyses, IR, 1H NMR spectra and single-crystal XRD.

第一部分合成了五个4-酰基吡唑啉酮缩4-乙基-氨基硫脲化合物：1-苯基-3-甲基-4-（4-溴）苯甲酰基-5-吡唑啉酮缩4-乙基-氨基硫脲(PM4BrBP-ETSC)，1-苯基-3-甲基-4-(4-甲基)苯甲酰基-5-吡唑啉酮缩4-乙基-氨基硫脲(PM4MBP-ETSC)，1-苯基-3-甲基-4-苯甲酰基-5-吡唑啉酮缩4-乙基-氨基硫脲，1，3-二苯基-4-苯甲酰基-5-吡唑啉酮缩4-乙基-氨基硫脲和1-苯基-3-甲基-4-苯乙酰基-5-吡唑啉酮缩4-乙基-氨基硫脲，其中前四个具有光致变色性质。

The preliminary bioassays indicated that, at 500 g/mL, 1-(o-tolyl-4-(4-chloro-3-ethyl-1-methylpyrazol-5-ylcarbonyl)semicarbazide (4g) and 1-(2,4-dimethyl- phenyl)-4-(4-chloro-3-ethyl-1-methylpyrazol-5-ylcarbonyl)semicarbazide (4k) showed inhibitory activities 90% and 80% against Blumeria graminis, respectively; and at 25 g/mL, 4-phenyl-4-(4-chloro-3-ethyl-1- methylpyrazol-5-ylcarbonylsemicarbazide (4c) showed inhibitory activity 70.1% against Botrytis cinerea and 1-2-nitro-phenyl-4-(4-chloro-3-ethyl-1-methylpyrazol-5-ylcarbonylsemicarbazide (4d) showed inhibi-tory activitiy 51.3% against Pyricularia oryzae.

初步生物活性实验结果表明，在500 mg/mL浓度下，化合物1-(4-氯-3-乙基-1-甲基-1H-吡唑-5-甲酰基)-4-(2-甲基苯基)氨基脲(4g)， 1-(4-氯-3-乙基-1-甲基-1H-吡唑-5-甲酰基)-4-(2，4-二甲基苯基)氨基脲(4k)对小麦白粉病菌的抑制率分别达到90%和80%；在25 mg/mL浓度下，化合物1-(4-氯-3-乙基-1-甲基-1H-吡唑-5-甲酰基)-4-苯基氨基脲(4c)对黄瓜灰霉病菌的抑制率达到70.1%；化合物1-(4-氯-3-乙基-1-甲基-1H-吡唑-5-甲酰基)-4-苯基氨基脲(4c)和1-(4-氯-3-乙基-1-甲基-1H-吡唑-5-甲酰基)-4-(2-硝基苯基)氨基脲(4d)对稻瘟病菌的抑制率均达到51.3%。

The results of biological tests indicated that, at 25 g/mL, 1-(4-bromo-3-ethyl-1-methyl-pyrazol-5'-ylcarbonyl-4-(2-nitrophenyl) semicarbazide (4d) showed inhibitory activities (52.6%) against Pyricularia oryzae. 1-(4-bromo-3-ethyl-1-methyl-pyrazol-5'-ylcarbonyl)-4-(3-chlorophenyl) semicarbazide (4j), 1-(4-bromo-3-ethyl-1-methyl-pyrazol-5'-ylcarbonyl)-4-(2,4-dimethylphenyl) semicarbazide (4k), 1-(4-bromo-3-ethyl-1-methyl-pyrazol-5'-ylcarbonyl)-4-(3,4-dimethyiphenyl) semicarbazide (41) and 1-(4-bromo-3-ethy-1-methyl-pyrazo1-5'-ylcarbonyl)-4-(2,4-difluorophenyl) semicarbazide (4m) showed inhibitory activities (45.6%) against Pyricularia oryzae, repestively.

初步生物活性实验结果表明，在25μg/mL浓度下，1-（1-甲基－3-乙基－4-溴－5-吡唑甲酰基）－4-（2-硝基苯基）氨基脲(4d)对水稻稻瘟病菌Pyricularia oryzae抑制活性达到52.6%；1-1-甲基－3-乙基－4-溴－5-吡唑甲酰基）－4-（3-氯苯基）氨基脲(4j，1-（1-甲基－3-乙基－4-溴－5-吡唑甲酰基）－4-（2，4-二甲基苯基）氨基脲(4k)，1-（1-甲基－3-乙基－4-溴－5-比唑甲酰基）－4-（3，4-二甲基苯基）氨基脲(41)和1-（1-甲基－3-乙基－4-溴－5-吡唑甲酰基）－4-（2，4-二氟苯基）氨基服(4m)对水稻稻瘟病菌Pyricularia oryzae抑制活性达到45.6%。

The kinetics of reconstitution of apoacylase with either 〓 or 〓 and the inactivation of the 〓 reconstituted enzyme by 1, 10-phenanthroline has been studied by following the substrate reaction continuously in presence of the metal ion or OP respectively. Although the native 〓-containing and the 〓-reconstituted enzymes have closely similar Michaelis constants and maximal velocities, the kinetics for both the inactivation by OP and the reconstitution of the apoenzyme with the metal ions differs considerably.

虽然钴重组的氨基酰化酶与天然含锌的氨基酰化酶在催化活性上比较相近，但两种酶在去金属失活动力学机制以及去金属失活的氨基酰化酶与两种金属离子重组复活的动力学过程均存在较大的差异，说明锌在氨基酰化酶中的作用比较复杂，并不能完全由钴替代。

This method is accurate, realiable and can be used for the determination of Paracetamol Tablets.

该方法准确、可靠，与标准法比较，结果较为满意，可用于对乙酰氨基酚片的含量测定。

Results:Paracetamol Injection solution of 25% was produced through the study on technology.

目的：对低浓度的对乙酰氨基酚注射剂进行改进。

Paracetamol can also be taken to bring down the fever.

对乙酰氨基酚也可以采取以降低发热。

Simple painkillers such as aspirin and paracetamol may help.

简单的止痛药如阿司匹林和对乙酰氨基酚可能的帮助。

The split between the two groups can hardly be papered over.

这两个团体间的分歧难以掩饰。

This approach not only encourages a greater number of responses, but minimizes the likelihood of stale groupthink.

这种做法不仅鼓励了更多的反应，而且减少跟风的可能性。