酰胺化

In this paper, acetanilide used as start material was chlorosulfonated, then reacted with alkylamines with different length of carbon chain to prepare 4 p-acetylaminophenylsulfonylalkylamine.

本文以乙酰苯胺为起始原料，经氯磺化后分别和不同碳链的正烷基胺反应制得4种不同碳链长度的对乙酰氨基苯磺酰烷基胺，将其水解后制得了对氨基苯磺酰正丁胺、对氨基苯磺酰正辛胺、对氨基苯磺酰正十二胺和对氨基苯磺酰正十八胺。

Part 2. Annulation reaction of 3, 4-dichlorocoumarin (1) and 3, 4-dichloromaleimide (8) by a new general annulation strategy developed in this group with 2-phenylbenzofuran (15), 3-phenylbenzofuran (16), 2, 5-diphenyloxazole (17), 2, 5-diphenylthiazole (18), 2-methyl-4-phenylthiazole (19) and 2, 3-dimethoxy-1, 3-butadiene (40) were investigated.

二。在本课题组前一阶段提出的从二氯代环烯酮与1，1-二芳基乙烯的光化反应以及光化反应中得到的环丁烷产物的连续电环化反应对3，4-二氯马来酰亚胺以及3，4-二氯香豆素进行增环反应的工作基础上，研究了3，4-二氯香豆素（1）和3，4-二氯马来酰亚胺（8）与5个α-苯基取代的环烯烃2-苯基苯并呋喃（15），3-苯基苯并呋喃（16），2，5-二苯基噁唑（17），2，5-二苯基噻唑（18），2-甲基-4-苯基噻唑（19），以及一个丁二烯——2，3-二甲氧基丁二烯（40）进行的芳香族增环反应。

Both the protection and deprotective group methods for the amino-group on side chain of a new N-pivot lariat crown ether were studied comparatively.

研究了一种新的氮支套素冠醚侧链上氨基的保护和脱保护基方法，结果表明，由过量乙二胺与对甲苯磺酰氯反应得到的单保护乙二胺（N－对甲苯磺酰基乙二胺4a），经N－烷基化环化反应，然后在氢化铝锂存在下脱除保护基，即可制得最佳产率的N－（2－氨基已基）单氮杂－12－冠－4（1）。

DDS was used as test drug for determination of acetylator phenotype employing HPLC.The results showed that both the occupational and non-occupational exposed group were predominantly slow acetylators(52.2％and 45.5％),higher than that in the exposed controls(13.0％)(0 05).The risks for bladder cancer with the slow ace...

结果表明。无论有无2－萘胺职业接触史，膀胱癌病人中慢型乙酰化者所占比例（52.2％和45.5％）均高于对照组（13.0％），且差异有显著性（P＜0.05），比值比0R分别为5.56（95％可信限＝1.02～30.3）和7.25（95％可信限＝1.70～30.3），提示慢型乙酰化者若暴露于2－萘胺更易患膀胱肿瘤，乙酰化慢表型是膀胱癌的一个遗传易感因素。

Firstly, 3-ethylthiobutanal was prepared from crotonaldehyde reacting with ethanehiol in triethylamine with high yield. Secondly, methyl acetoacetate was converted to 6-ethylthiohept-3-en-2-one by three steps via hydrolysis, condensation with 3-ethyltio-butanal and dehydration, then 6-ethylthiohept-3-en-2-one was cycloco ndensed with dimethyl malonate by Michael addition and Claisen condensation, followed by saponification and decarboxylation to give the intermediate of 5-(2-ethylthiopropyl)-cyclohexane-1,3-dione.

首先，以巴豆醛与乙硫醇为原料，在三乙胺的催化作用下高收率制得3-乙硫基丁醛；然后从乙酰乙酸甲酯出发，通过碱水解、与3-乙硫基丁醛缩合、脱水三步反应合成6-乙硫基-3-烯-2-庚酮，接着6-乙硫基-3-烯-2-庚酮与丙二酸二甲酯通过Michael加成和Claisen缩合成环，再通过皂化和脱羧反应生成中间体5-[2-丙基]-1，3-环己二酮；再与丙酸酐反应丙酰化，最后与0-3-氯-2-丙烯基羟胺肟化，得到目标化合物烯草酮。

Was synthesized from succimide by bromination with bromine,methylation with dimethyl sulfate and the reaction of indolyl magnesium bromide with 2,3-dibromoN-methylmaleimide.

以琥珀酰亚胺为起始原料，经过溴化、甲基化后再与吲哚溴化镁加成反应合成了2-溴-3-(1H-吲哚-3)-N-甲基马来酰亚胺，总收率44.8%，其结构经1H NMR和IR确证。

Seven of them have not been reported.Their structures were confirmed by IR,~1HNMR,MS,and element analysis. 4.Meanwhile,the green methylation procedure of imides was developed by using dimethyl carbonate as methylation reagent.A series of imides,for example,phthalimide,3,4-dibromo-maleimide and succincide were used for substrates.The effects of DABCO(1,4-diazabicyclo [2.2.2]octane)and DBU(1,8-diazabicyclo[5.4.0]undec-7-ene)as a catalyst in this kind of reactions were investigated.2-Bromo-3-(1-methylindolyl-3-yl)-1-methyl-1H-pyrrole-2,5-dione was prepared by using dimethyl carbonate,which further expanded the use of dimethyl carbonate,as a green agent in organic synthesis.

在以硫酸二甲酯为甲基化试剂对3，4-二溴马来酰亚胺进行N-甲基化反应合成3，4-二溴-N-甲基马来酰亚胺的同时，以碳酸二甲酯为甲基化试剂，对3，4-二溴马来酰亚胺、邻苯二甲酰亚胺、琥珀酰亚胺等酰亚胺类化合物的N-甲基化反应进行了研究；考察了1，4-二氮杂双环[2.2.2]辛烷，1，8-二氮杂双环[5.4.0]十一碳-7-烯、碳酸钾和四丁基溴化铵等作为催化剂对碳酸二甲酯N-甲基化反应的反应时间和收率等的影响，并应用碳酸二甲酯为甲基化试剂，合成了N-甲基-3-溴-4-(1-甲基-吲哚-3)-马来酰亚胺。

In this paper, the improvement of synthetic method of 2-acetylaminotropone is introduced. 3-Acetyltropolone reacted with low concen-tration methylamine solution and solvent was directly evaporated in reduce pres-sure to give 2-acetyl-7 -methylaminotropone in good yield. The compound reacted with phenyltrimethylammonium tribromide to give two new compounds.

本文介绍2-乙酰基-7-甲胺基酮合成方法的改进——用挥发性小的低浓度甲胺溶液与3-乙酰基酚酮反应；和采用直接减压蒸除溶剂法分离产品，得到较好产率的2-乙酰基-7-甲胺基酮；用化合物与三溴化苯基三甲铵反应，得到两种至今未见文献报道的新化合物。

Neoformans via the tail vein）, CTX group and controls. The expres- sion of BDNF and bFGF was detected by immunohistochemical technique. Results: Lots of C.

48只C57BL／6雌性小鼠随机分为对照组、环磷酰胺组和试验组，免疫组化法检测大脑皮质BDNF和bFGF的表达。

Optimum conditions are as follows: DMF is used as solvent, compound quaternary ammonium salt as catalyst, n(p-nitrochloro benzene):n=1: 1.2, m:m(p-nitrochloro benzene)=4%, m:m(p-nitrochloro benzene)1:1, and reacted under 155~160℃ for 18 h; reduction reaction is carried out in methanol with Raney nickel, which is used as catalyst; the raw product is added an antioxidant, and distilled simply under reduced pressure to obtain 4-fluoroaniline with excellence quality, purity is over 99.5%, total yield is 89.3%.

实验结果表明，氟化反应的最佳条件为：二甲基甲酰胺为溶剂、复合季铵盐为催化剂，n：n=1：1.2，m（催化剂：m=4%，m：m=1：1，于155~160℃下反应18h；还原反应在甲醇中进行，以阮内镍为催化剂；粗产品加入抗氧剂，减压条件下简单蒸馏得高品位的对氟苯胺。

The split between the two groups can hardly be papered over.

这两个团体间的分歧难以掩饰。

This approach not only encourages a greater number of responses, but minimizes the likelihood of stale groupthink.

这种做法不仅鼓励了更多的反应，而且减少跟风的可能性。