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二氯甲基苯

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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 general formula of said soluble fluorine- containing aromatic medlin is as follows: the substituent group on side phenyl group in diamine monomer Ar includes methyl, trifluoromethyl, two trifluoromethyls or chlorine and trifluoromethyl.

可溶性含氟芳香聚酰亚胺具有如下通式:二胺单体Ar中苯侧基上取代基为甲基、三氟甲基、两个三氟甲基或者氯和三氟甲基。

Object: A specific and sensitive liquid chromatography tandem mass spectrometry method was developed for the multiresidue determination of sulfisomidine, sulfapyridine, sulfamerazine, sulfamethoxazole, sulfisoxazole, sulfadiazine, sulfamethizole, sulfachlorpyridazine, sulfamethoxypyridazine, sulfadimethoxine, sulfamonomethoxine, sulfathiazole, sulfadoxine, sulfaquinoxaline, sulfanilamide, sulfaguanidine, sulfamoxole, sulfameter, sulfadimidine, sulfacetamide, sulfaphenazole, sulfanitran, sulfabenzamide and a potentiator, trimethoprim, in meat.

目的:建立猪肉中磺胺及其增效剂多残留检测的液相色谱-串联质谱法,包括磺胺二甲异嘧啶、磺胺吡啶、磺胺甲基嘧啶、磺胺甲基异噁唑、磺胺二甲异噁唑、磺胺嘧啶、磺胺甲噻二唑、磺胺氯哒嗪、磺胺甲氧哒嗪、磺胺间二甲氧嘧啶、磺胺-6-甲氧嘧啶、磺胺噻唑、磺胺邻二甲氧嘧啶、磺胺喹噁啉、磺胺、磺胺脒、磺胺噁唑、磺胺甲氧嘧啶、磺胺二甲嘧啶、磺胺醋酰、磺胺苯吡唑、磺胺硝苯、磺胺苯酰和甲氧苄氨嘧啶。

In this paper, 2,6-dimethyl-1,4-phenylene oxidel was modified by trimethyl chlorosilane and triphenyl chlorosilane, and a serfes of silyl-substituted PPO were synthesized.

讨论了聚2,6-二甲基-1,4-苯撑氧与三甲基氯硅烷和三苯基氯硅烷的反应,合成了一系列取代含量不同的三甲基硅取代PPO和三苯基硅取代PPO。

Methyl-2,3,5,6-tetrafluoro-benzene methanol was synthesized by chlorination, acylation, fluorination, esterifica- tion, reduction, bromization, reduction from terephthalic acid. Tefluthrin was obtained from-(1RS,3RS)-3-(2-chloro-3,3,3-trifluoro-1-propenyl)-2,2-dimethyl cycolpropa-necarboxylate acid by reacting with 4-methyl-2,3,5,6-tetrafluoro-benzene methanol.

以对苯二甲酸为原料,经氯化、酰氯化、氟化、酯化、还原、溴化、还原七步反应合成了4-甲基-2,3,5,6-四氟苄醇,甲基苄醇与-(1RS,3RS)-3-(2-氯-3,3,3-三氟丙-1-丙烯基)-2,2-二甲基环丙甲酸一步酯化合成了七氟菊酯。

In a similar way, using N,N\'-dibenzyl tartamide as auxiliary,-(2-methyl)allyl-2-chloro-phenyl-methyl azide, a vital intermediate of Repaglinide, can be prepared via asymmetric allylation of o-chlorobenzaldehyde in

产物经氧化和碘加成内酯化反应得到阿伐他汀中间体(3R,5S)-3-羟基-5-碘甲基戊内酯(10);将N-苄基酒石酸二酰胺用于邻氯苯甲醛的不对称烯丙基化反应以较高光学收率得-甲基烯丙基-2-氯苯基-甲基醇

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。

They are insoluble in water, ethanol, methanol, acetone, chloroform and benzene, but soluble in DMA, DMF and DMSO.

它们溶于N,N-二甲基甲酰胺、N,N-二甲基乙酰胺和二甲基亚矾等溶剂,但不溶于水、乙醇、甲醇、丙酮、氯仿和苯。

Cellulose benzoate,the degree of substitution of which was calculated from the content of C determined by element analysis,was prepared from microcrystalline celluloseand benzoyl chloride under heterogeneous condition and characterized by FT-IR and~1H-NMR.

研究了微晶纤维素和苯甲酰氯在多相条件下合成制备纤维素苯甲酸酯的反应,通过元素分析所得碳的质量百分含量计算了产物的取代度,并系统研究了吡啶与N,N-二甲基乙酰胺或与三乙胺混合反应溶剂、苯甲酰氯与纤维素羟基的摩尔比r、反应温度和反应时间对D S的影响,用FT-IR和1H-NM R对产物进行了表征。

The effects and mechanism of GABAergic neurons, NOergic neurons, opioid peptide and cyclic adenosine monophosphate in the nucleus reticularis thalami on sleep-wakefulness cycle of rats and the effects and mechanism of the 5-HTergic nerve fibers project from the nucleus raphes dorsalis to RT on sleep-wakefulness cycle of rats were investigated with the methods of brain stereotaxic, nucleus spile, microinjection and polysomngraphy.1. The effects of GABAergic neurons in RT on sleep-wakefulness cycle of rats1.1 Microinjection of 3-mercaptopropionic acid (3-MP, a kind of glutamate decarboxylase inhibitor) into RT. On the day of microinjection, sleep only decreased a litter. On the second day, sleep marked decreased and wakefulness marked increased. On the third and fourth day, sleep and wakefulness stages resumed to normal.1.2 Microinjection of gamma-amino butyric acid (GABA 1.0μg) into RT enhanced sleep and reduced wakefulness compared with control; while microinjection of L-glutamate (L-Glu, 0.2μg) decreased sleep and increased wakefulness; microinjection of bicuculline (BIC, 1.0μg), a GABAA receptor antagonist, enhanced wakefulness and reduced sleep; microinjection of baclofen (BAC, 1.0μg), GABAB receptor agonist, had the same effects as GABA.2. The effects of NOergic neurons in RT on sleep-wakefulness cycle of rats2.1 Microinjection of L-arginine (L-Arg, 0.5μg) into RT decreased sleep compared with control, but there were on statistaical difference between L-Arg group and control; while microinjection of sodium nitroprusside (SNP, 0.2μg), a NO donor into RT, sleep marked decreased and wakefulness marked increased. Microinjection of nitric oxide synthase inhibitor, N-nitro-L-arginine (L-NNA, 2.0μg) into RT enhanced sleep and reduced wakefulness.2.2 After simultaneous microinjection of L-NNA (2.0μg) and SNP (0.2μg) into RT, SNP abolished the sleep-promoting effect of L-NNA compared with L-NNA group; after simultaneous microinjection of L-NNA (2.0μg) and L-Arg(0.5μg) into RT, we found that L-NNA could not blocked the wakefulness-promoting effect of L-Arg.3. The effects of opioid peptide in RT on sleep-wakefulness cycle of rats3.1 Microinjection of morphine sulfate (MOR, 1.0μg) into RT increased wakefulness and decreased sleep compared with control; while microinjection of naloxone hydrochloride (NAL, 1.0μg), the antagonist of opiate receptors, into RT, enhanced sleep and reduced wakefulness.3.2 After simultaneous microinjection of MOR (1.0μg) and NAL (1.0μg) into RT, the wakefulness-promoting effect of MOR and the sleep-promoting effect of NAL were not observed compared with control.4. The effects of cAMP in RT on sleep-wakefulness cycle of rats Microinjection of cAMP (1.0μg) into RT increased sleep and decreased wakefulness compared with control; microinjection of methylene blue (MB,1.0μg) into RT enhanced sleep and reduced wakefulness compared with control.5. The effects of the 5-HTergic nerve fibers project from DRN to RT on sleep-wakefulness cycle of rats5.1 When L-Glu (0.2μg) was microinjected into DRN and normal sodium (NS,1.0μg) was microinjected into bilateral RT. We found that sleep was decreased and wakefulness was increased compared with control; when L-Glu (0.2μg) was microinjected into DRN and methysergide (MS,1.0μg), a non-selective 5-HT antagonist, was microinjected into bilateral RT, We found that sleep was enhanced and wakefulness was reduced compared with L-Glu group.5.2 When p-chlorophenylalanine (PCPA, 10μg) was microinjected into DRN and NS (1.0μg) was microinjected into bilateral RT, We found that sleep was increased and wakefulness was decreased compared with control; microinjection of 5-hydroxytryptaphan (5-HTP, 1.0μg), which can convert to 5-HT by the enzyme tryptophane hydroxylase and enhance 5-HT into bilateral RT, could block the effect of microinjection of PCPA into DRN on sleep-wakefulness cycle.

本研究采用脑立体定位、核团插管、微量注射、多导睡眠描记等方法,研究丘脑网状核(nucleus reticularis thalami,RT)中γ-氨基丁酸(gamma-amino butyric acid ,GABA)能神经元、一氧化氮(nitrogen monoxidum,NO)能神经元、阿片肽类神经递质、环一磷酸腺苷(cyclic adenosine monophosphate,cAMP)及中缝背核(nucleus raphes dorsalis,DRN)至RT的5-羟色胺(5-hydroxytryptamine,5-HT)能神经纤维投射对大鼠睡眠-觉醒周期的影响及其作用机制。1 RT内GABA能神经元对大鼠睡眠-觉醒周期的影响1.1大鼠RT内微量注射GABA合成关键酶抑制剂3-巯基丙酸(3-MP,5μg),注射当天睡眠时间略有减少,第二日睡眠时间显著减少,觉醒时间明显增多,第三、四日睡眠和觉醒时间逐渐恢复至正常。1.2大鼠RT内微量注射GABA受体激动剂GABA( 1.0μg)后,与生理盐水组比较,睡眠时间增加,觉醒时间减少;而RT内微量注射L-谷氨酸(glutamic acid, L-Glu, 0.2μg)后,睡眠时间减少,觉醒时间增加;RT内微量注射GABAA受体阻断剂荷包牡丹碱(bicuculline,BIC,1.0μg)后,睡眠时间减少,觉醒时间增加;RT内微量注射GABAB受体激动剂氯苯氨丁酸(baclofen,BAC,1.0μg)后,产生了与GABA相似的促睡眠效果。2 RT内NO能神经元对大鼠睡眠-觉醒周期的影响2.1大鼠RT内微量注射NO的前体L-精氨酸(L-Arg,0.5μg)后,与生理盐水组对比,睡眠时间略有减少,但无显著性意义;而RT内微量注射NO的供体硝普钠(Sodium Nitroprusside,SNP,0.2μg)后可明显增加觉醒时间,缩短睡眠时间;微量注射一氧化氮合酶抑制剂L-硝基精氨酸(L-arginine,L-NNA,2.0μg)后,引起睡眠时间增多,觉醒时间减少。2.2大鼠RT内同时微量注射L-NNA(2.0μg)和SNP(0.2μg)后与L-NNA组比较发现SNP逆转了L-NNA的促睡眠作用;RT内同时微量注射L-NNA(2.0μg)和L-Arg(0.5μg)后,与L-NNA(2.0μg)组比较发现L-Arg可以增加觉醒而缩短睡眠,其促觉醒作用未能被NOS的抑制剂L-NNA所逆转。3 RT内阿片肽对大鼠睡眠-觉醒周期的影响3.1大鼠RT内微量注射硫酸吗啡(morphine sulfate,MOR,1.0μg)后与生理盐水组对比,睡眠时间减少而觉醒时间增加; RT内微量注射阿片肽受体拮抗剂盐酸纳洛酮(naloxone hydrochloride,NAL,1.0μg)后与生理盐水组比较,睡眠时间增加而觉醒时间减少。3.2大鼠RT内同时微量注射MOR(1.0μg)和NAL(1.0μg)后,与生理盐水组对比,原有的MOR促觉醒效果和NAL的促睡眠效果都没有表现。4 RT内环一磷酸腺苷信使对大鼠睡眠-觉醒周期的影响大鼠RT内微量注射cAMP(1.0μg)后与NS(1.0μg)组比较,睡眠时间增多而觉醒时间减少;RT内微量注射亚甲蓝(methylene blue,MB,1.0μg)后,与NS组比较,睡眠时间增多而觉醒时间减少。5中缝背核投射到丘脑网状核的5-羟色胺能神经纤维对大鼠睡眠-觉醒周期的影响5.1大鼠DRN内微量注射L-Glu(0.2μg),同时在双侧RT内微量注射NS (1.0μg)后,与对照组(DRN和双侧RT注射NS, 0.2μg)比较,睡眠时间减少,觉醒时间增多;大鼠DRN内微量注射L-Glu(0.2μg),同时在双侧RT内微量注射二甲基麦角新碱(methysergide, MS, 1.0μg )后,与对照组(DRN注射L-Glu 0.2μg,双侧RT注射NS 1.0μg)比较,睡眠时间增多,觉醒时间减少。5.2大鼠DRN内微量注射对氯苯丙氨酸(p-chlorophenylalanine,PCPA,10μg),同时在双侧RT内微量注射NS (1.0μg)后,与对照组(DRN和双侧RT注射NS, 1.0μg)比较,睡眠时间增多,觉醒时间减少;大鼠DRN内微量注射PCPA(10μg),产生睡眠增多效应后,在双侧RT内微量注射5-羟色胺酸(5-hydroxytryptaphan , 5-HTP, 1.0μg )后,与对照组(DRN注射PCPA 10μg,双侧RT注射NS 1.0μg)比较,睡眠时间减少,觉醒时间增多。

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Now, however, all children continue in "comprehensive" schools, and the eleven-plus determines which courses of study the child will follow.

然而现在,所有的孩子都要在综合学校继续学习,所以这次考试只是决定他们将要学习哪些课程。

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