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In the first step of thedouble annulation route, 2-amino-3-carbamoyl-5,6-dihydro-4-pyridones 2 werecreated in high to excellent yields by a formal [5C + 1N] annulation reaction ofketene--acetals 1 with ammonia.

第一步,二硫缩烯酮1和氨源通过[5C + 1N]加成反应产率极高的得到了2-氨基-3-氨基甲酰基-5,6-二氢-4-吡啶酮2。

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。

In order to testify our whether correction to Rossi's exchange term andthe potential of electron and nucleus is reasonable, we calculate 〓 moleculeelastic differential scattering cross section by electron impact on 100eV, ourresult is obviously better than Rossi's. Then we calculate elastic differentialscattering cross section at 150eV. In order to check the program thatcalculates molecule excitation cross section by electron impact, we calculatehydrogen excitation cross section from ground state to 〓 state at 20eVand 30eV, oxygen excitation cross section from ground state to 〓 state at15eV and 20eV. These calculations are in agreement with other theoreticresults, and experiment measure. Finally, we calculate sulfur moleculeexcitation〓 cross section by electron impact at5eV,7eV,9eV, 11eV, 13eV,15eV, and draw curve of excitation total crosssection corresponding to incident electron energy.

为了核对我们修改的计算激发态的程序是否正确,计算了电子与氢分子碰撞从基态激发到〓态入射能量分别为20eV和30eV时的微分截面以及电子与氧分子碰撞从基态激发到〓态入射能量分别为15eV和20eV时的微分截面,与别人的理论计算结果、实验的测量值基本一致,最后计算了电子与硫分子在5eV、7eV、9eV、11eV、13eV、15eV时的碰撞激发〓截面,作出了电子的入射能量与激发总截面的关系曲线,找出了总截面最大时对应的电子入射能量大约是11电子伏。

Methods Naloxone was synthesized starting from oxidation of thebaine, followed by hydrogenation, acylation, cyanidation, O-demethylation, hydrolyzation and N-allylation. The alternative method of O-demethylation, methane sulfonic acid/DL-methionine and hydrobromic acid were investigated.

在以蒂巴因为原料,经氧化、氢化、酰化、氰化、去氧甲基、水解、N-烯丙基化得到纳洛酮的合成路线中,分别采用甲磺酸/DL-甲硫氨酸和氢溴酸代替三溴化硼进行去氧甲基化和后续水解反应。

CH3OH could attack the phosphor atom in 1,3,2-dioxaphopholane of compiound (1) to give O-methyl O-hydroxyethyl-O-phthalimidoethyl thiophosphate in 85% yield; in the presence of potassium hydroxide aryl selenol could attack the carbon atom in 1,3,2-diox-aphopholane of the cyclic phospholipid conjugate of N^1-(2-furanidyl)-N^3--5-fluorouracil to give the corresponding product of ring-opening in high yields.

在室温下,以异丙醇作溶剂,苯硒酚与化合物2不反应。在氢氧化钾存在下,以异丙醇/水作溶剂(体积比20:1,在室温下,硒酚可以有效地进攻中化合物2中1,3,2-二氧磷杂环戊烷中的碳原子生成相应的开环产物。按照这一反应条件,顺利实现了硒酚对N^1-(2-呋喃基)-N^3-羟烷基-5-氟脲嘧啶硫代环甘油磷脂缀合物的亲核开环,生成甘油骨架的端碳原子上带有芳硒基新颖的磷脂核苷缀合物。

Double chain naphthyurea/thiourea piperazine derivatives could act as a fluorescent chemosensor not for aromatic dicarboxylate but for linear dicarboxylate especially for pimelate anion.

双链萘脲基或硫脲基哌嗪化合物与直链二羧酸盐络合具有较高的稳定常数和1∶1的化学计量比,两者通过六个氢键形成双点结合的络合物。

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。

The alternative method of O-demethylation,methane sulfonic acid/DL-methionine and hydrobromic acid were investigated.

方法在以蒂巴因为原料,经氧化、氢化、酰化、氰化、去氧甲基、水解、N-烯丙基化得到纳洛酮的合成路线中,分别采用甲磺酸/DL-甲硫氨酸和氢溴酸代替三溴化硼进行去氧甲基化和后续水解反应。

Less preferred metal chelating groups are hydroxides amines which may be aliphatic aryl or heteroaryl; or mercaptans which may be aliphatic aryl or heteroaryl.

次选项金属螯合组的氢氧化物胺可能是脂肪族,芳基或杂;或硫醇可能是脂肪族,芳基或杂。

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I didn't watch TV last night, because it .

昨晚我没有看电视,因为电视机坏了。

Since this year, in a lot of villages of Beijing, TV of elevator liquid crystal was removed.

今年以来,在北京的很多小区里,电梯液晶电视被撤了下来。

I'm running my simile to an extreme.

我比喻得过头了。