喹唑啉

Goal compound synthesis namely: Take the vanillic acid as outset raw material, obtains 4- hydroxyl - 3- anisole methyl formate with the methyl alcohol reflux conditions, then after the etherification, the nitration, the return to original state, the ring closure response obtains 6- methoxy - 7- animal pen oxygen radical kui zuo lin - 4- alkone, then passes through the chlorination, the substitution aniline, to escape responses again and so on animal pen oxygen radical, etherification to obtain the goal compound; The goal compound and the diethylamine had the amine substitution reaction to obtain TM1, namely 4- benzene amino - 6- methoxy - 7- [2- hydroxyl - 3-(N, N- two ethyl aminos) third oxygen radical] kui zuo lin; Through zuo has the etherification with the Austria niter to respond obtains TM2, namely 4- benzene amino - 6- methoxy - 7- [2- hydroxyl - 3-(2- methyl - 5- nitryl imidazole) third oxygen radical] kui zuo lin.

目标化合物的合成即：以香草酸为起始原料，与甲醇回流条件下得到4-羟基-3-甲氧基苯甲酸甲酯，然后经过醚化、硝化、还原、环合反应得到6-甲氧基-7-苄氧基喹唑啉-4-酮，然后再经氯化、取代苯胺、脱苄氧基、醚化等反应得到目标化合物；目标化合物与二乙胺发生胺取代反应得到了TM1，即4-苯氨基-6-甲氧基-7-[2-羟基-3-丙氧基]喹唑啉；通过与奥硝唑发生醚化反应得到TM2，即4-苯氨基-6-甲氧基-7-[2-羟基-3-(2-甲基-5-硝基咪唑)丙氧基]喹唑啉。

The present paper take the purine synonym kui zuo lin as a parent nucleus, separately in its 4 and 7 introduction structure diverse substituted benzene amino and the flexible side chain, designed a series of 4- substitution anilino-- 6- methoxy - 7-(2- hydroxyl to substitute for third oxygen radical) kui zuo lin a kind of compound.

本论文以嘌呤类似物喹唑啉为母核，分别在其4位和7位引入结构多样的取代苯氨基和柔性侧链，设计了一系列4-取代苯胺基-6-甲氧基-7-(2-羟基取代丙氧基)喹唑啉类化合物。

The most potent quinazolinone and quinazoline had pA2 values of 7.0 and 5.9, respectively.

活性最高的喹唑啉酮和喹唑啉的 pA2值分别为7.0和5.9。

The design, synthesis, and angiotensin Ⅱ antagonist activities of several quinazolinone and quinazoline phenoxyphenylacetic acids are described.

本文设计、合成了一系列喹唑啉酮和喹唑啉苯氧基苯乙酸类化合物，并检测了它们的血管紧张素Ⅱ受体拮抗活性。

Two representative compounds have been determined by X-ray crystallography. The best ratio of reactants, the adequate reaction temperature and solvent have been found by contrast experiments.4. The better photoreaction conditions and irridation times have been confirmed through the different photoreaction results. It is the first time that fifty quinazoline derivatives with biological activity and four photooxidation products with urea functional groups have been obtained by photochemistry method. Two representative compounds, quinazoline derivatives and photooxidation products, have been determined by X-ray crystallography, respectively.

通过实验对比我们找到了较佳的反应物的投料比、反应温度和反应所用的溶剂。4、根据不同条件下的光反应结果，确定了硫脲衍生物的相对较好的光反应条件和光照时间，首次利用光化学手段成功得到50个具有生物活性的喹唑啉衍生物和4个具有脲基官能团的光氧化的产物，测定了两个具有代表性的喹唑啉和光氧化的产物的晶体结构。

Quinazolinone ring was used to replace the quinoline moiety of quinoline phenoxyphenylacetic acids which have been discovered as potent AⅡ antagonists, to give a new series of antagonists, while their quinazoline analogs were obtained as isomers during the synthesis of.

前文报道了一系列喹啉苯氧基苯乙酸类非肽类血管紧张素Ⅱ受体拮抗剂，本文以喹唑啉酮代替化合物的喹啉获得化合物，在合成化合物时，同时还获得了化合物。

Many of the aza quinazolines have showed potent activity, such as pyrido[2,3-d]pyrimidine, pyrido [3,2-d]pyrimidine, pyrido[4,3-d]pyrimidine, pyrido[3,4-d]pyrimidine, and pyrimido [5,4-d]pyrimidine. Moreover, the compounds that the benzene in quinazoline ring was substituted by five-member rings, such as pyrrolo[2,3-d]pyrimidine, pyrazolo[3,4-d]pyrimidine, can also inhibit the EGFR and show bright prospects.

然而喹唑啉环并非EGFR抑制剂所必须的，在随后的研究中，人们发现许多氮杂喹唑啉类也有很好的活性，如吡啶并[2，3-d]嘧啶类、吡啶并[3，2-d]嘧啶类、吡啶并[4，3-d]嘧啶类、吡啶并[3，4-d]嘧啶类、嘧啶并[5，4-d]嘧啶类，也就是在喹唑啉环的5，6，7，8-位都可以氮杂，且都有活性。

Synthesis of target compounds namely: to vanillic acid as the starting material with methanol under reflux conditions for 4 - hydroxy -3 - p-methyl, then ether, and nitration, reduction, cyclization reaction 6 - methoxy -7 - benzyloxy-quinazoline -4 - one, and then by the chloride in place of aniline, benzyloxy-off, such as etherification reaction of the target compounds; target compounds with the second and third occurrence of substitution reactions of amines by the TM1, that is, 4 - amino-benzene -6 - methoxy -7 - [2 - hydroxy -3 -(N, N-diethyl amino) oxy c] quinazoline; with ether occurred Ornidazole reaction of TM2, namely, 4 - amino-benzene -6 - methoxy -7 - [2 - hydroxy -3 -(2 - methyl -5 - nitroimidazole) C oxy] quinazoline.

本论文以嘌呤类似物喹唑啉为母核，分别在其4位和7位引入结构多样的取代苯氨基和柔性侧链，设计了一系列4-取代苯胺基-6-甲氧基-7-(2-羟基取代丙氧基)喹唑啉类化合物。目标化合物的合成即：以香草酸为起始原料，与甲醇回流条件下得到4-羟基-3-甲氧基苯甲酸甲酯，然后经过醚化、硝化、还原、环合反应得到6-甲氧基-7-苄氧基喹唑啉-4-酮，然后再经氯化、取代苯胺、脱苄氧基、醚化等反应得到目标化合物；目标化合物与二乙胺发生胺取代反应得到了TM1，即4-苯氨基-6-甲氧基-7-[2-羟基-3-丙氧基]喹唑啉；通过与奥硝唑发生醚化反应得到TM2，即4-苯氨基-6-甲氧基-7-[2-羟基-3-(2-甲基-5-硝基咪唑)丙氧基]喹唑啉。

Quinazolin-4(3H)-ones(1) were conveniently synthesized from anthranilic acids and amidines,which could be chloridized with POCl_3 to obtain 4-chloroquinazolines (2).The reaction of 2 and 1H-pyrazol-3-amine would give two types of products.In the presence of acid or base,the C-N bond would be formed between the 4-position carbon of 2 and the NH_2 of 1H-pyrazol-3-amine.While the C-N bond between the 4-position carbon of 2 and the NH of 1H-pyrazol-3-amine would be formed when Pd catalyst was utilized.

以邻氨基苯甲酸类化合物和脒为原料，可方便地获得喹唑啉-4(3H)-酮类产物(1)，1经POCl_3氯化可到4-氯代喹唑啉化合物(2)。2与3-氨基-1H-吡唑化合物反应可得到两种类型的产物，在酸、碱条件下2的4位碳和3-氨基-1H-吡唑化合物的NH_2发生C-N成键反应；在Pd催化条件下，2的4位碳则和3-氨基-1H-吡唑化合物的环内NH发生C-N成键反应。

Quinazolinone alkaloids are the active components contained in the plants of Rutaceae. Many investigators have indicated that quinazolinones have anti-tumor activity. However, the reasons why the molecular mechanisms of quinazolinones produced their biological effects remain unknown.

喹唑啉酮类生物碱是芸香科植物中所含的活性成分，虽然已有许多研究者证实喹唑啉酮类缘物具有抗癌活性，然而，其真正的抗癌作用机制仍然未被厘清。2-(Naphthalene-1-yl)-6-pyrrolidinyl-4-quinazolinone（HL66）是合成的喹唑啉酮类缘物。

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。