苯酰胺

They are 4-(2- hydroxy-3-butynlenoxy) benzoic acid (1, WA), 5-chloro-7, 8-dihydroxy-7-methyl- 6-oxo-3- [ -3, 4-dihydroxy-3, 5-dimethyl-l-heptylene] -1H-8, 8a-dihydrobenzo [2, 3-c] pyran (2, WB),-2-(2-methyl-2-dibutene diamido)-2-butenoic acid (3, B5262), 3, 4-dihydro-9, 10-dihydroxy-7-methoxy-3-methyl-1H-naphtho [2, 3- c] pyran-1-one (4, A73 semi-Vioxanthin), 8, 8'-bis (6, 9-dioxo-3,4-dihydro-10- hydroxy-7-methoxy-3-methyl-1H-naphtho [2, 3-c] pyran-1-one)(5, A122 Xanthomegnin), 2, 5-dioxo-3a-hydroxymethyl-3, 3a, 6, 6a-tetrahydro-furo [2, 3-b] furan (6, 1003-2), 7-acety1-5-chloro-6, 8-dioxo-7-methyl-3- [ -3, 5-dimethyl-1, 3- diheptylene] -4aH-benzo [2, 3-c] pyran (7, M2-2 sclerotiorin), respectively.

它们分别被命名为4-（2-羟基-3-丁炔氧基）苯甲酸（1，WA）、5-氯-7，8-二羟基-7-甲基-6-氧代-3-[-3，4-二羟基-3，5-二甲基-1-庚烯基]-1H-8，8a-二氢苯并[2，3-c]吡喃（2，WB）、-2-（2-甲基-2-丁烯二酰亚胺基）-2-丁烯酸（3，B5262）、3，4-氢-9，10-二羟基-7-甲氧基-3-甲基-1H-萘并［2，3-c］吡喃-1-酮（semi-Vioxanthin，4，A73）、8，8'-双（6，9-二氧代-3，4-二氢-10-羟基-7-甲氧基-3-甲基-1H-萘并［2，3-c］吡喃-1-酮）（Xanthomegnin，5，A122）、2，5-二氧代-3a-羟甲基-3，3a，6，6a-四氢-呋喃并［2，3-b］呋喃（6，1003-2），7-乙酰基-5-氯-6，8-二氧代-7-甲基-3-［-3，5-二甲基-1，3-庚二烯基］-4aH-苯并2，3-c］吡喃（Sclerotiorin，7，M2-2）。

Study on an efficient process for the preparation of trifloxystrobin starting from 2-methylacetophenone bypartial oxidation,esterification,reaction with methoxyamine,bromization and condensation with 3'- acetophenone oxime.

以邻甲基苯乙酮为原料，经过高锰酸钾的碱性氧化，甲醇酯化，再与甲氧基胺盐酸盐肟化后，用N-溴丁二酰亚胺溴化，最后和间三氟甲基苯乙酮肟缩合得到目标产物肟菌酯。

Our company supply raw materials and related intermediates as follows: Second dibutyryl cAMP calcium, voriconazole, terbinafine, vecuronium amines, cAMP, thiamphenicol, a chlorophenol hydrochloride esters, card network sodium phosphate tilmicosin, foscarnet, lornoxicam, Tilmicosin, Cephalosporium aspirin acid, ceftiofur hydrochloride, ceftiofur sodium, Ozagrel, ondansetron hydrochloride ketones, hydroxyurea, ticarcillin sodium, telmisartan, esmolol hydrochloride, hydrochloric acid Daguan Nikkomycin, adefovir dipivoxil, buflomedil hydrochloride, granisetron hydrochloride, warfarin sodium,-methyl gabexate acid, nicergoline, pantoprazole sodium,·, tegafur, cefepime hydrochloride, vecuronium bromide, hydrochloric acid meclofenoxate, sertraline hydrochloride, Cefonicid amine salt, aztreonam, ticarcillin, cefdinir, cefodizime sodium, sodium ferulate, colloidal pectin secretion, 2,3 - cyclopentene and pyridine, Piperacillin acid, cefetamet US-acid, hydrochloride Cefmenoxime ,3-TZ, 2 - deoxy-D-glucose, two-amidine urea benzene, sodium Cefonicid, Cefonicid intermediates, ester Cefamandole sodium, Cefalotin acid, intermediates cefpirome, cefepime sulphate, cefepime intermediate nucleus of cefepime, cefpirome nucleus, Cefamandole sodium, ceftriaxone new active ester, oxaliplatin, cyclophosphamide vary gland amines, polyene match him.

我公司供应的原料药及相关中间体为：二丁酰环磷腺苷钙、伏立康唑、盐酸特比萘芬、维库溴胺、环磷腺苷、甲砜霉素、盐酸甲氯酚酯、卡络磺钠、磷酸替米考星、膦甲酸钠、氯诺昔康、替米考星、头孢匹胺酸、头孢噻呋盐酸盐、头孢噻呋钠、奥扎格雷、盐酸恩丹西酮、羟基脲、替卡西林钠、替米沙坦、盐酸艾司洛尔、盐酸大观霉素、阿德福韦酯、盐酸丁咯地尔、盐酸格拉司琼、华法林钠、甲磺酸加贝酯、尼麦角林、泮托拉唑钠、普拉洛芬、替加氟、盐酸头孢吡肟、维库溴铵、盐酸甲氯芬酯、盐酸舍曲林、头孢尼西胺盐、氨曲南、替卡西林、头孢地尼、头孢地嗪钠、阿魏酸钠、胶体果胶泌、2，3-环戊烯并吡啶、哌拉西林酸、头孢他美酸、头孢甲肟盐酸盐、3-TZ、2-脱氧-D-葡萄糖、双脒苯脲、头孢尼西钠、头孢尼西中间体、头孢孟多酯钠、头孢噻吩酸、头孢匹罗中间体、头孢吡肟硫酸盐、头孢吡肟中间体、头孢吡肟母核、头孢匹罗母核、头孢孟多钠、头孢曲松新型活性酯、奥沙利铂、异环磷腺胺，多烯他赛。

Synthesis of Antidote of N-Dichloroacetyl-2-methyl-1-oxa-4-aza-spiro-4.4-nonane BI Hong-mei, ZHANG Jin-yan, LIANG Ying, SHEN Yong (College of Arts and Sciences Heilongjiang August First Reclamation University, Daqing 163319, Heilongjiang, China) Abstract: N-Dichloroacetyl-2-methyl-1-oxa-4-aza-spiro-4.4-nonane was synthesized by one pot method with isopropanolamine, cyclopentanone and dichloroacetyl chloride. The optimum reaction conditions obtained are as follows:the proportion in moles of the above materials is 1∶1∶1.2, reaction solvent is toluene, reaction temperature is -15 to -10 ℃,reaction time is 3 h, under the optimum condition, the yield of the compound is 50.0%.

除草剂解毒剂N-二氯乙酰基-2-甲基-1-氧杂-4-氮杂-螺[4.4]壬烷的合成毕洪梅，张金艳，梁英，沈勇(黑龙江八一农垦大学文理学院，黑龙江大庆 163319)摘要：以33%的氢氧化钠水溶液为缚酸剂，异丙醇胺、环戊酮和二氯乙酰氯为原料，采用&一锅法&合成了N-二氯乙酰基-2-甲基-1-氧杂-4-氮杂-螺[4.4]壬烷，采用正交实验法得到最佳反应条件：反应原料摩尔比为1∶1∶1.2，苯作溶剂，反应的温度为-15 ℃~-10 ℃，搅拌时间为3 h，产率达到50.0%。

Tetrachloroterephthalic acid was prepared by chlorinating terephthalic acid, oleumsolvent and iodine catalyst. Tetrachloroterephthalic acid was acylated by sulphurous oxychloride in the presence of DMF to form tetrachloroterephthaloyl chloride. The acyl chloride product was fluorinated by potassium fluoride and esterified by methanol to synthesize dimethyl tetrafluoroterephthalate. The ester was reduced with potassium borohydride and lithium chloride to give tetrafluoroterephthalyl alcohol. The above product was bromated in the hydrobromic acid to obtain 4-bromomethyl-2,3,5,6-tetrafluoro-benzene methanol. 4-Methyl-2,3,5,-6-tetrafluorobenzene ethanol was obtained by reducing the bromide with magnesium. In the exist of DCC and DMAP, tefluthrin was got by the condensation reaction between 4-methyl-2,3,5,6-tetrafluoro-benzene methanol and-(1RS,3RS)- 3-(2- chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cycolpropanecar-boxylate acid.

对苯二甲酸与氯气在碘存在下以发烟硫酸为溶剂进行氯化制备四氯对苯二甲酸；再以DMF为催化剂与二氯亚砜反应生成四氯对苯二甲酰氯；以氟化钾为氟化剂，环丁砜为溶剂置换氟化，再与甲醇酯化得到四氟对苯二甲酸甲酯；以KBH4-LiCl为还原剂二甲醚为溶剂反应制得四氟对苯二甲基苄醇；以氯苯为溶剂在溴化氢溶液中溴化得到溴化产物；在乙醇溶液中经镁粉还原得到4-甲基-2，3，5，6-四氟苄醇；甲基苄醇与功夫酸在催化剂二环己基碳二亚胺和4-二甲氨基吡啶作用下缩合得到七氟菊酯，总收率达43.6%。

NOBS PAG , can obviously activate hydrogen peroxide thus , the efficiency of hydrogen peroxide bleaching can be advanced greatly .

研究结果初步表明，此类有机酰化剂类如：四乙酰乙二胺，四乙酰甘脲，异壬酰氧基苯磺酸钠，五乙酰葡萄糖等有着非常明显的活化过氧化氢的作用，从而能在很大程度上提高纸浆过氧化氢漂白的效率。

The intermediate which obtained from oximation of 7a-e reacted withmethyl N-(2-bromomethylphenyl)-N-methoxycarbamate to synthesize oxime ether methyl carbamate 3a-e.

以邻位卤代苯甲醛和3-丁烯-2-醇为原料通过钯催化&一锅法&反应合成了2-乙酰基茚7a-e，7a-e 肟化之后和N-(2-溴甲基苯基)-N-甲氧基氨基甲酸甲酯反应合成了肟醚类氨基甲酸甲酯3a-e，进一步胺解之后得到了肟醚类氨基甲酰甲胺3f-j。

Afterwards, N-(6-chloro-3-pyridinemethyl) phthalimide is prepared by using potassium phthalimide, as nucleophilic reagent, condensation reacting with 2-chloro-5-methylpyridine at a temperature of 70℃.

然后在70℃条件下，以邻苯二甲酸亚胺钾作为亲核试剂，与2-氯－5-氯甲基吡啶发生缩合反应，制备了N-（6-氯－3-吡啶甲基）邻苯二甲酰亚胺。

The synthetic route starts from penicillin G, peroxyacetic acid(8.5%) as Oxidizing Agent to get penicillin G sulfoxide; esterifided with p-nitrobenzyl bromine to synthesize penicillin G sulfoxide ester; we synthesize 3-exomethylenecepham sulfoxide ester with phthalimide potassium and 4A molecular sieve as acid scavenger to open the ring, SnCl_4 as catalyzation to close the ring. The yield is over 60%.

本研究采用的合成路线为：以青霉素G钾盐为原料，选用工业过氧化氢制备的过氧乙酸(22.3%)稀释至8.5%为氧化剂，氧化得青霉素亚砜；采用对硝基溴苄为酯化试剂，制备青霉素亚砜酯；以NCP(N-氯代邻苯二甲酰亚胺)为开环试剂，酞酰亚胺钾和4A型分子筛为酸清除剂，顺利开环；再经无水SnCl_4催化闭环得3-环外亚甲基头孢亚砜酯，最终产率在60%以上。

In the third step, when the ratio of racemic ester to benzenesulfonyl chloride to triethylamine to catalyst 4-DMAP is 1:1:1:0.1 in 10℃, the yield is 82.9% and high purity is obtained by crystallisation.

在第三步磺酰化反应中，得到合成消旋2-苯磺酸基-2(2-氯苯基)乙酸甲酯的较佳反应条件为邻氯扁桃酸甲酯：苯磺酰氯：三乙胺=1：1：1，催化剂4-DMAP用量为摩尔反应物的10%，反应温度为10℃，收率为82.9%，同时用结晶方法获得高纯度的产物。

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Yang yinshu、Wang xiangsheng、Li decang,The first discovery of haemaphysalis conicinna.

1〕 杨银书，王祥生，李德昌。安徽省首次发现嗜群血蜱。