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According to the synthetic methods study of the quinolones, it is found that the synthetic method of parent ring is of wide use by the condensation from α-substituted aryl formyl-β-substituted aminoacrylic acid and the inner molecular nucleophilic substitution reaction, which is almost suitable for the quinolones preparation of different rings or different substituted groups in 〓-position.

然后，对其合成方法进行了归纳，发现：由α-取代芳甲酰基-β-取代氨基丙烯酸缩合，经分子内亲核取代反应形成喹诺酮母环的合成方法用途非常广，几乎适用于所有不同环系或〓-位是不同取代基的喹诺酮类衍生物的制备。

In previous work of helicid's structure modification show that 4 substituted groups of helicid are some ordinary acyclic and substituted aniline group, and it had no heptad heterocyclic substituted group.

在前期的豆腐果苷结构修饰工作中，豆腐果苷4位取代基多为一些简单的脂肪族、取代苯胺基等，尚无七元杂环作为取代基的此类化合物。

This invention provides compounds of Formula; wherein: R is a moiety selected from the group: and n is an integer of 1 or 2; R is selected from hydrogen, amino,-NRR, alkyl of 1 to 12 carbon atoms optionally substituted, aryl of 6, 10 or 14 carbon atoms optionally substituted, alkenyl of 2 to 12 carbon atoms optionally substituted, alkynyl of 2 to 12 carbon atoms optionally substituted, halogen, and a 5 to 10 membered heteroaryl ring optionally substituted, having 1 to 4 heteroatoms independently selected from N, O and S; R is selected from hydrogen, alkyl of 1 to 12 carbon atoms optionally substituted, aryl of 6, 10 or 14 carbon atoms optionally substituted, alkenyl of 2 to 12 carbon atoms optionally substituted, vinyl, alkynyl of 2 to 12 carbon atoms optionally substituted and halogen; R is H, alkyl of 1 to 12 carbon atoms optionally substituted, cycloalkyl of 3 to 8 carbon atoms, bicycloalkyl of 5 to 10 carbon atoms or aralkyl optionally substituted; R is OH or -OH; R and R are each independently H or alkyl of 1 to 12 carbon atoms or when optionally taken together with the nitrogen atom to which each is attached form a 3 to 8 membered saturated heterocyclyl ring; R is alkyl of 1 to 12 carbon atoms optionally substituted; or a tautomer or pharmaceutically acceptable salts thereof.

本发明提供式的化合物；其中：R 1 为选自基团和的部分；n为整数1或2；R 2 选自氢、氨基、-NR 6 R 7 、具有1到12个碳原子的视情况经取代的烷基、具有6个、10个或14个碳原子的视情况经取代的芳基、具有2到12个碳原子的视情况经取代的烯基、具有2到12个碳原子的视情况经取代的炔基、卤素和具有1到4个独立地选自N、O和S的杂原子的视情况经取代的5元到10元杂芳基环；R 3 选自氢、具有1到12个碳原子的视情况经取代的烷基、具有6个、10个或14个碳原子的视情况经取代的芳基、具有2到12个碳原子的视情况经取代的烯基、乙烯基、具有2到12个碳原子的视情况经取代的炔基和卤素；R 4 为H、具有1到12个碳原子的视情况经取代的烷基、具有3到8个碳原子的环烷基、具有5到10个碳原子的双环烷基或视情况经取代的芳烷基；R 5 为OH或-OH 8 ；R 6 和R 7 各自独立地为H或具有1到12个碳原子的烷基，或当视情况与其所连接的氮原子连接在一起时形成3元到8元饱和杂环基环；R 8 为具有1到12个碳原子的视情况经取代的烷基；或其互变异构体或医药学上可接受的盐。

Experimental results show that the different substituted location and different substituted group on benzene cycle would result in the diversity of reduction properties of substituted aryl nitrobenzene. Substituted nitrobenzenes with withdrawing group will be reduced at more positive potential, while those with repelling group will be reduced at more negative potential. In addition, the reduction potential of nitro group of o-nitrobenzene shifts more negative due to the effect of space resistance.

结果表明，芳族硝基化合物在苯环上的取代基位置不同以及在相同位置上取代基的种类不同均可使各芳族硝基化合物的电还原性能发生较大差异：吸电子取代基在电还原过程中电位较正，推电子取代基的电还原电位较负：邻位取代基在反应过程中由于空间位阻效应，苯环上的硝基在电还原时电位往负方向移动。

The second route firstly studied the tautomerization of the key intermediate from spirostane to cholestane 3-O-substituted kryptogenin,then formed a direct access used Zn/KI/HOAc reduction,which supplied a better synthetic method of MPD and other furostanol saponins.

第二条路线则首先研究了由螺甾到胆甾结构的关键中间体3-O-substituted kryptogenin的异构化现象，建立起以Zn/KI/HOAc还原反应直接合成该中间体的过程，这提供了一个更好的合成甲基原薯蓣皂苷及其他呋甾皂苷的方法。

The present invention relates to compounds of formula wherein R is hydrogen, lower alkyl, lower alkoxy, halogen or lower alkyl substituted by halogen; R is hydrogen or halogen; or R and R are together with the carbon atom to which they are attached -CH=CH-CH=CH-; R is hydrogen, lower alkyl, phenyl optionally substituted by halogen, or is hetaryl, optionally substituted by lower alkyl; R is hydrogen, lower alkyl, phenyl, benzyl, lower alkenyl, lower alkoxy, phenyloxy, benzyloxy, S-lower alkyl, halogen, CN, lower alkyl substituted by halogen or O-lower alkyl substituted by halogen; R is hydrogen or lower alkyl, aryl is phenyl or naphthyl; n is 1, 2 or 3; m is 1 or 2; and pharmaceutically acceptable acid addition salts and tautomeric forms thereof.

本发明涉及式化合物及其可药用的酸加成盐和互变异构形式，其中R 1 是氢、低级烷基、低级烷氧基、卤素或被卤素取代的低级烷基；R是氢或卤素；或R 1 和R与它们连接的碳原子一起是-CH＝CH-CH＝CH-；R 2 是氢、低级烷基、任选被卤素取代的苯基或者是任选被低级烷基取代的杂芳基；R 3 是氢、低级烷基、苯基、苄基、低级链烯基、低级烷氧基、苯氧基、苄氧基、S-低级烷基、卤素、CN、被卤素取代的低级烷基或被卤素取代的O-低级烷基；R 4 是氢或低级烷基，芳基是苯基或萘基；n是1、2或3；m是1或2。

The general formulas of these compounds are as follows:The strobilurin derivatives were synthesized from substitutedβ-keto esters (2) as starting material which were prepared from substituted ketones (1) and dimethyl carbonate. The ester (2) and methyl hydrazine or substituted amidine were dissolved in methanol and the mixture was heated to reflux to obtain the substituted 5-hydroxy-1H-pyrazole (3) or 4-hydroxy-pyrimidine (4). The title compounds were prepared by reacting the intermediates (3 and 4) with substituted halomethylphenyls which contain four active group under basic conditions.

本论文所合成的strobilurin化合物均是以β-酮酸酯类化合物(2)为起始原料合成的，该中间体(2)是由酮类化合物(1)与碳酸二甲酯在碱性条件下反应生成的，中间体(2)与甲基肼或取代脒类化合物在甲醇中回流制得取代的1H-5-羟基吡唑(3)或4-羟基嘧啶(4)，中间体(3和4)再与包含四种活性基的苄卤中间体在碱性条件下制得目标化合物。

The genera formulas of these compounds are as follows:The strobilurin derivatives were synthesized from substitutedβ-keto esters (2) as starting material which were prepared from substituted ketones (1) and dimethyl carbonate. The ester (2) and methyl hydrazine or substituted amidine were dissolved in methanol and the mixture was heated to reflux to obtain the substituted 5-hydroxy-1H-pyrazole (3) or 4-hydroxy-pyrimidine (4). The title compounds were prepared by reacting the intermediates (3 and 4) with substituted halomethylphenyls which contain four active group under basic conditions.

本论文所合成的strobilurin化合物均是以β-酮酸酯类化合物(2)为起始原料合成的，该中间体(2)是由酮类化合物(1)与碳酸二甲酯在碱性条件下反应生成的，中间体(2)与甲基肼或取代脒类化合物在甲醇中回流制得取代的1H-5-羟基吡唑(3)或4-羟基嘧啶(4)，中间体(3和4)再与包含四种活性基的苄卤中间体在碱性条件下制得目标化合物。

The results of bioassay suggest that 2-methylthio-6-methyl-4-substituted pyrimidine and 4, 6-dimethoxy-2-substituted pyrimidine derivatives show herbicidal activity. In these target compounds, 4, 6-dimethoxy-2-substituted pyrimidine benzylamine and 4, 6-dimethoxy-2-Substituted pyrimidine benzylidene amine exhibit good herbicidal activity, and the herbicidal will be affected by the substituents in the benzene ring.

对分子库中的目标分子进行了生物活性筛选研究，发现其中的2-甲硫基-6-甲基-4-取代嘧啶衍生物和4，6-二甲氧基-2-取代嘧啶类化合物显示出除草活性，其中4，6-二甲氧基-2-取代嘧啶苄胺类化合物和4，6-二甲氧基-2-取代嘧啶亚苄胺类化合物具有较好的除草活性，而且其活性和苯环上的取代基有关。

The major products were methane, ethylene, propylene, butylene, butadiene, cyclopentadiene, benzene, toluene, styrene, vinyl-substituted cyclopentene derivatives and C5/C6 isomers (pentadiene, methyl-substituted cyclopentene derivatives, cyclohexene, hexadiene and methyl-substituted cyclopentadiene derivatives), and the main primary products were determined to be C1～C4 compounds, cyclopentadiene, benzene, toluene and vinyl-substituted cyclopentene derivatives.

热裂解主要产物为甲烷、乙烯、丙烯、丁烯、丁二烯、环戊二烯、苯、甲苯、苯乙烯、环戊烯的乙烯基取代物及C5， C6异构体(戊二烯、环戊烯的甲基取代物、环己烯、己二烯和环戊二烯甲基取代物)，其中， C1～C4、环戊二烯、苯、甲苯、乙烯基取代环戊烯为初始产物。

In the United States, chronic alcoholism and hepatitis C are the most common ones.

在美国，慢性酒精中毒，肝炎是最常见的。

If you have any questions, you can contact me anytime.

如果有任何问题，你可以随时联系我。