硫酰胺

In this thesis, a convenient and efficient synthesis of highly functionalizeddihydropyrido[2,3-d]pyrimidines via a double [5 + 1] annulation strategy startingfrom easily available α-alkenoyl-α-carbamoyl ketene--acetals 1 and cheapreagents (NH4OAc, DMF, and POCl3) has been developed.

本论文探索了一种简便有效的合成高度官能化的二氢吡啶并[2，3-d]嘧啶的方法，此方法由易得的α-乙酰基-α-氨基乙酰基二硫缩烯酮1和便宜的试剂(醋酸铵，二甲基甲酰胺和三氯氧磷)通过两步[5 + 1]加成而实现。

Methods 4-Hydroxy- benzonitrile was treated with sodium hydrogen sulfide and anhydrous magnesium chloride in dimethyl formamide to give thioamide, which was then directly cyclized with ethyl 2-chloroacetoacetate without separation to give ethyl 2-(4-hydroxyphenyl)-4-methylthiazole-5-carboxylate(2) in one-pot; then 2 was formylated with Duff reaction adopting hexamethylenetetramine in trifluoroacetic acid to give ethyl 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylate(3); finally, the target compound was obtained by the treatment of 3 with hydroxylamine hydrochloride and sodium formate in formic acid.

采用"一勺烩"方法，以4-羟基苯甲腈为起始原料，首先与硫氢化钠和无水氯化镁在N，N-二甲基甲酰胺中反应，所得中间体不经分离，直接加入2-氯乙酰乙酸乙酯进行环合反应，得到2-(4-羟基)苯基-4-甲基-5-噻唑甲酸乙酯（2）；然后通过六亚甲基四胺/三氟乙酸进行Duff反应，得到2-(3-甲酰基-4-羟基)苯基-4-甲基-5-噻唑甲酸乙酯（3）；再经盐酸羟胺/甲酸/甲酸钠体系脱水得到目标化合物。

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。

Chapter two 4-Hydroxybenzoic acid is connected with PEG6000 through defoliant DCC at rooom temperature, then the product is refluxed with chloroacetic acid in acetone to afford PEG-bound phenyloxyacetic acid, which is reacted with thionyl chloride, ammonium thiocyanate and arylamines in turn to give PEG-bound disubstituded thioureas. After the cleavage with sodium methoxide in methanol, the eleven disubstituted thioureas are obtained.

第二章 利用PEG6000作载体，通过脱水剂DCC在室温下将对羟基苯甲酸以酯键连接在PEG6000上，再与氯乙酸在较温和的条件下生成PEG6000支载的芳氧乙酸，然后，依次与亚硫酰氯、硫氰酸铵、芳胺反应，生成PEG6000支载的硫脲，最后用甲醇钠的甲醇溶液切割PEG，得到了十一种1，3-二取代硫脲。

Methods 4-Hydroxybenzonitrile (2) as the starting material was transformed to 4-hydroxy-thiobenzamide (3) via thioformylation. And ethyl 2-(4-hydroxyphenyl)-4-methylthiazole-5-carboxylate (4), which was synthesized via cyclization from 3, was treated with hexamethylenetetramine to generate the intermediate ethyl 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylate (5). The target compound febuxostat (1) was obtained from 5 by etherification, cyanidation, hydrolysis.

以羟基苯腈为原料，经硫代甲酰化得到对羟基硫代苯甲酰胺(3)，3经环合得到2-（4-羟基苯基）－4-甲基－噻唑－5-羧酸乙酯(4)，4与乌洛托品反应，得到中间体2-（3-甲酰基－4-羟基苯基）－4-甲基－噻唑－5-羧酸乙酯(5)，之后再经醚化、氰化、水解得到目标产物(1)。

Methods: Uses carbon tetrachloride (CC14) 2ml/kg, thioacetamide 200mg/kg, the abdominal cavity to inject separately, Establish model which the rat acute liver damages; Guarantees the liver profit stomach mixture, the polyene phosphatide acid radical choline capsule, the glycyrrhizic acid diamidogen capsule fills the stomach.

分别用四氯化碳(CC14)2mL/kg，硫代乙酰胺200mg/kg，腹腔注射，建立大鼠急性肝损伤的模型；保肝益胃合剂，多烯磷脂酰胆碱胶囊，甘草酸二胺胶囊灌胃治疗。

Methods 4-Hydroxy- benzonitrile was treated with sodium hydrogen sulfide and anhydrous magnesium chloride in dimethyl formamide to give thioamide, which was then directly cyclized with ethyl 2-chloroacetoacetate without separation to give ethyl 2-(4-hydroxyphenyl)-4-methylthiazole-5-carboxylate(2) in one-pot; then 2 was formylated with Duff reaction adopting hexamethylenetetramine in trifluoroacetic acid to give ethyl 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylate(3); finally, the target compound was obtained by the treatment of 3 with hydroxylamine hydrochloride and sodium formate in formic acid.

采用&一勺烩&方法，以4-羟基苯甲腈为起始原料，首先与硫氢化钠和无水氯化镁在N，N-二甲基甲酰胺中反应，所得中间体不经分离，直接加入2-氯乙酰乙酸乙酯进行环合反应，得到2-(4-羟基)苯基-4-甲基-5-噻唑甲酸乙酯（2）；然后通过六亚甲基四胺/三氟乙酸进行Duff反应，得到2-(3-甲酰基-4-羟基)苯基-4-甲基-5-噻唑甲酸乙酯（3）；再经盐酸羟胺/甲酸/甲酸钠体系脱水得到目标化合物。

The chemical deposition method was applied to prepare bismuth sulfide through reaction of bismuth salt complexed by triethanolamine or EDTA with an aqueous solution containing a sulfur sourse such as thioacetamide, thiourea, sodium thiosulphate, geseous H2S.

化学沉积方法用于准备硫化铋铋盐络合的反应，通过乙醇胺水溶液或edta一个含有硫源为硫代乙酰胺等，硫、硫代硫酸钠、硫化氢geseous。

Research result indicated that the cooperative effect between swell and precursor is main factor for the nanoparticle loaded in Nafion, and moreover, polarity of solvent and water content in Nafion also affects the load largely. To improve away the surface concentration of CdS nanocrystal on two side of membrane for general preparation, thioacetamide was first used as a precursor instead of inorganic sulfur source(H2S and Na2S) in synthesis of CdS nanocrystal. The assembly mechanism for several sulfur source had been studied, and CdS/Nafion with the character of homogeneous disperse had been prepared, which is fit for mass transmission in photocatalitic reaction. Following the investigation of several crystallizing way, simple and reliable hydrothermal-crystallizing was found. According to this way, maximal TiO2 load in Nafion achieved 43%. Activity of TiO2/Nafion or CdS/Nafion as a photocatalyst was explored initially for disintegrating liquid contamination. Maximal decompose rate achieved 86% under condition of this research.

研究结果表明：Nafion膜对纳米粒子负载量的主要影响因素是溶胀作用与前驱体协同效应，同时溶剂极性和薄膜含水量对负载量也影响相当大；本课题首次使用硫代乙酰胺代替传统无机硫源（H2S、Na2S）合成CdS纳晶，研究了各种硫源的组装机理，克服了常规技术存在的CdS纳晶趋于膜表面富集的缺点，得到了有利于光催化传质需要的体相均匀分布CdS/Nafion；研究了多种Nafion膜内纳米粒子晶化途径，找到了简单可靠的水热晶化法，TiO2纳晶最高负载量达43％；初步探索了TiO2/Nafion、CdS/Nafion作为光催化剂降解水中模拟污染物的活性，在本实验条件下最高降解率达86％。

85 And 119486/79. They are a novel type of antibiotic having both the wide antibacterial spectrum and high safety of penicillin and cephem antibiotics belonging to beta -lactam antibiotics, as well as the potent antibacterial activity and high beta -lactamase stability of carbapenem antibiotics.Sodium-(5R, 6S)-6-[-1-hydroxyethyl]-7-oxo-3- [-2-tetrahydrofuryl]-4-thia-1-azabicyclo [3.2.0] hept-2-ene-2-carboxylate 5/2 hydrate (faropenem sodium, hereinafter referred to as compound 1) is currently used as an oral drug for various infectious diseases and is reported to show potent antibacterial activity against not only methicillin-sensitive Staphylococcus aureus, Streptococcus pyrogenes and Streptococcus pneumoniae but also gram-positive bacteria for which conventional beta -lactam drugs have proved ineffective such as penicillin-resistant pneumococci, oral staphylococci and enterococci, also showing a wide antibacterial spectrum covering gram-negative bacteria such as Haemophilus influenzae and anaerobic bacteria such as the genus Bacteroides, which activity is due to its novel skeleton penem ring (Kagaku Ryoho no Ryoiki The Field of Chemotherapy, Vol.

他们是一种新型的抗生素都具有广泛的抗菌谱和高度的安全青霉素和cephem抗生素，属于β-内酰胺类抗生素，以及作为强大的抗菌活性和高β-内酰胺酶稳定的碳青霉烯类antibiotics.sodium -（ 5 R ， 6 S ）-6 -[ - 1 -羟乙基] - 7 -氧- 3 - [ - 2 - t etrahydrofuryl] - 4 -硫杂- 1 -氮杂双环[ 3 。2.0]庚- 2 -节能- 2 -羧酸5 / 2水合物（法罗培南钠，以下简称为化合物1 ）是目前用来作为口服药物，为各种传染病和报道，以显示强大的抗菌活性，不仅对甲氧敏感的金黄色葡萄球菌，链球菌pyrogenes和肺炎链球菌，但也克阳性菌为常规β-内酰胺类药物已证明无效，如青霉素耐药pneumococci ，口腔葡萄球菌和肠球菌，也显示出广泛的抗菌谱，包括革兰阴性菌如流感嗜血杆菌和厌氧菌如属杆菌，这活动是由于其新颖的骨架青霉烯环（（化学ryoho没有ryoiki领域的化疗），第13卷，第10号，第74-80 ， 1997年）。

This one mode pays close attention to network credence foundation of the businessman very much.

这一模式非常关注商人的网络信用基础。

Cell morphology of bacterial ghost of Pasteurella multocida was observed by scanning electron microscopy and inactivation ratio was estimated by CFU analysi.

扫描电镜观察多杀性巴氏杆菌细菌幽灵和菌落形成单位评价遗传灭活率。