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氨磺酰

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Dichloro-5-sulfamoylbenzoic acid(1)was synthesized by sulfochlorination , ammoniation and hydrolysis with 2,4-dichlorobenzoic acid as raw materials, and the reaction conditions were optimized.

2,4-二氯苯甲酸为原料,经氯磺化、氨解、水解酸化三步反应制备了2,4-二氯-5-磺酰氨基苯甲酸(1)。

The results indicate that the optimized sulfonylation reaction time is 4 h, the materiel rate of chlorosulfonic acid and 2-chloroimidazo[1,2-α]pyridine is 1.2 : 1, with ethylamine the yield increasing from 15.4% to above 70%; the optimized ammonolysis reaction time is 3 h and the reaction temperature is 27℃, with the acetonitrile yield increasing from 60.1% to above 79.6%.

实验结果表明,磺酰化反应的最佳反应时间为4 h,氯磺酸与2-氯咪唑并[1,-α]吡啶的用量比为1.2:1,加入三乙胺可将收率由15.4%提高到70%以上;氨解反应的最佳反应时间为3 h,反应温度为27 ℃,加入乙腈可将收率由60.1%提高到79.6%;方案经改进后,总反应时间缩短3 h,收率提高了5.5%。

Synthesis of novel sulfonamide-prolinols and their application on the asymmetric addition of diethylzinc to benzaldehyde.

三、研究了脯氨酸衍生的新型手性磺酰胺-氨基醇的合成及其催化二乙基锌对苯甲醛的不对称加成反应 1。

Ophenyl phenol,ophenyl phenol sodium salt tetrahydrate,7ADCA,2ethyl phenyl hydrazine hydrochloride,2,3dihydrofuran,7ethyl3(2hydroxy ethyl)indole,methyl ester of etodolac; 1,8diethyl1,3,4,9tetrahydropyrano[3.4b] indole1acetic acid methyl ester,5chloro2methoxy benzoic acid,4(2aminoethyl)benzene sulfonamide,5cyano phthalide,phthalhydrazide,9thioxanthenone,n[(1,4benzodioxane2yl)carboxyl]piperazine HCL,2chloro4amino6,7dimethoxyquinazoline,2chloro benzimidazole,1(4fluorobenzyl)2chlorobenzimidazole,2methylthio4pyrimidone,5amino4imidazole carboxamide HCL,6chloro2hexanone,11oxo6.11hydrodibenzothiepin,6,11dihydrodibenzooxepin11one,10,11dihydrodibenzocyclohepten5one;dibenzosuberone,dibenzo cyclohepten5one;dibenzosuberenone,3,5dihydroxy benzoic acid,3,5dihydroxy benzyl alcohol,2mercapto benzimidazole,3,4dihydroxy benzaldehyde,3,4dihydroxy benzonitrile,2amino5chloro benzonitrile,2(4chlorophenoxy)ethyl chloride,2(4chloro phenoxy)tert,butane,ditrimethylol propane;DTMP,2,2bis(4hydroxyphenyl)butane; bisphenol B,1,1'bis(4hydroxyphenyl)cyclohexane;bisphenol Z,tetrabromobisphenolS,3,5ditertbutyl salicylic acid,3,4,5trihydroxy benzoic acid stearyl ester,1,2,4trimethoxybenzene.

华业公司产品:邻苯基苯酚,邻苯基苯酚钠盐,7氨基3去乙酰氧基头孢烷酸,邻乙基苯肼盐酸盐,2,3二氢呋喃,7乙基色氨醇,依托度酸甲酯,5氯2甲氧基苯甲酸,4(2氨乙基)苯磺酰胺,5氰基苯酞,双酮酞嗪,9噻吨酮,N〔(1,4苯并二恶烷2基)羰基〕哌嗪盐酸盐,2氯4氨基6,7一二甲氧基喹唑啉,2氯苯并咪唑,1(4氟苄基)2氯苯并咪唑,2甲硫基4嘧啶酮,5氨基咪唑4 甲酰胺盐酸盐,6氯2已酮,11氧6.11二氢苯并〔b.c〕虑平,11氧代6,11二氢二苯并氧杂卓,10,11二氢二苯并环庚烯5酮,二苯并环庚烯5酮,3,5二羟基苯甲酸,3,5二羟基苯甲醇,2巯基苯并咪唑,3,4二羟基苯甲醛,3,4二羟基苯腈,2氨基5氯苯腈,2(4氯苯氧基)1氯乙烷,2(4氯苯氧基)叔丁烷,双丙烷,2,2二(4羟基苯基)丁烷;双酚B,1,1'双(4羟基苯基)环己烷;双酚Z,2[3,5二溴4(2,3二溴丙氧基)]苯砜,3,5二叔丁基水杨酸,3,4,5三羟基苯甲酸十八烷基脂,1,2,4三甲基氧基苯。

Methods the all cells were divided into four groups: control group, p-tosyl-l-phenylalanine chloromethyl ketone group, dexamethasone group, cotreatment group.

分组:对照组、对甲苯磺酰-l-苯丙氨酸甲基甲酮组、地塞米松组、tpck+dex组。mtt比色分析法测定细胞生长抑制率,流式细胞术测定细胞凋亡率。

The analysis of SAR reveals that the activities of target compounds are closely associated with the electron-withdrawing substituents at the para position of 1-aryl-1, 2, 4 -triazoles as well as with the substituents such as sulfonyl and methylthio groups at the 3 position of 1, 2, 4 -triazoles; And the introduction of sulfamoyl moiety at the para position of 5-aryl-1,2,4-triazoles also has significant influence on the anti-inflammatory activity of these compounds.

构效关系分析发现,在三唑环1位芳基的对位引入F、Cl、Br吸电子基团以及3位引入磺酰基和甲硫基,对抗炎活性有重要的意义;在三唑环5位芳基的对位引入氨磺酰基,对抗炎活性有较大影响。

SA catalyzed the amidation of benzhydryl alcohol in good to excellent yields under solvent-free condition.

加热条件下磺氨酸可以催化磺酰胺和酰胺类化合物与二苯甲醇的取代反应,生成新的取代胺类化合物。

Synthesis process of 2,6-dichloro-3-methylaniline was investigated 3-methylaniline was first N-acetylated with acetic anhydride,then treated with chlorosulphonic acid and ammonia yielding the 2-methyl-4--benzenesulfonic amide,which wasin turn deacetylated,chlorinated and hydrolyzed to the title compound.Hydrochloric acid was used instead of sodium hydroxide in deacetylation and sodium chlorate instead of hydrogen peroxide as oxidant in chlorination.

合成工艺2,6-二氯-3-甲基苯胺调查3-甲基首次N-乙酰与醋酸酐,然后与氯磺酸和氨产量 2-甲基-4--苯磺酰胺基,而擅转乙酰,氯化和水解的标题compound.hydrochloric酸代替氢氧化钠乙酰氯酸钠代替双氧水为氧化剂,加氯。

This dissertation is mainly focused on the reactivity of methylenecyclopropanes and comprises six parts. 1 The reactions of methylenecyclopropanes with phenylsulfenyl chloride, phenylselenyl chloride and diphenyl diselenide; 2 The coupling reactions of the ring-opening products derivated from methylenecyclopropanes; 3 The palladium-catalyzed ring-enlargement of mono-aryl group substituted methylenecyclopropanes to cyclobutenes. 4 The gold-catalyzed domino ring-opening and ring-closing hydroamination of methylenecyclopropanes with sulfonamides; 5 The Lewis acid-catalyzed reactions of mono-aryl group substituted methylenecyclopropanes with diethyl ketomalonate in the presence of water; 6 The iodobenzene diacetate mediated novel 1,3-dipolar cycloaddition of methylenecyclopropanes, vinylidenecyclopropanes, and methylenecyclobutane with phthalhydrazine.

本论文主要研究了亚甲基环丙烷类化合物的一些化学反应性能,共由以下六部分组成:1、亚甲基环丙烷类化合物与苯硫氯、苯硒氯及二苯基二硒的反应;2、亚甲基环丙烷类化合物开环产物的偶联反应;3、单芳基取代的亚甲基环丙烷类化合物在钯催化剂作用下的扩环反应;4、金化合物催化磺酰胺对亚甲基环丙烷类化合物的串联开环关环氨氢化反应;5、路易斯酸催化亚甲基环丙烷类化合物与丙酮二羧酸二乙酯在有水存在下的反应;6、醋酸碘苯促进的亚甲基环丙烷类化合物、亚乙烯基环丙烷类化合物及亚甲基环丁烷类化合物与邻苯二甲酰肼的新型1,3-偶极环加成反应。

Herein, using grafting strategy we have developed a new kind of sulfamide-amine alcohol ligands by grafting a activator to the traditional aminoalcohols, which led to more rigid tridentate coordination model and benefit to the control of chiral surrounding.

本文提出一种嫁接策略设计新的手性配体,即在传统的氨醇配体上嫁接上一个活化剂就可以得到一类新型的手性磺酰胺-氨醇配体。

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