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Then Doripenem came into the market in the July ,2005. We studied the synthesis of Doripemen.Firstly, we synthesized the chemical 2 from the starting material------o-hydroxylphenylacylamine through Reformastky reaction, alkylation, Diekmann reaction, enolization, esterification and etc. Secondly, we synthesized the chemical 3 from L — hydroxylproline through the protection of carboxyl, amidogen and hydroxyl group, reduction by NaBr, SN_2 substitution and Mitsumobu reaction.

我们以水杨酰胺为起始原料,经Reformatsky反应、烷基化、Diekmann环合、烯醇化、酯化等反应合成双环母核2;再从L-羟基脯氨酸出发,经酯化保护羧基、保护氨基、保护羟基、硼氢化还原酯得醇、Sn2取代和Mitsumobu反应等合成巯基侧链3;最后由化合物3经脱保护、水解得硫醇,和化合物2在二异丙基乙基胺的作用下缩合,最后Pd/C催化脱保护,历经16步反应最终得到产物多尼培南。

Photoreactions of 8 with 15-19, on the other hand, furnished the corresponding [2+2] cyclobutane products and the annulation products together.

二氯马来酰亚胺(8)与15—19的光化反应中则分别得到相应[2+2]的环丁烷产物和增环产物,在与19的反应中,还得到由环丁烷产物脱氯化氢后得到的环丁烯开环的二烯产物。

Starting from 3-benzoyl-5-formyl-indolizine, 3-benzoyl-5-(2'2'-diacetylethenyl)-indolizines and analogs were obtained by the 〓mediated aldol condensation or Wittig reaction. These compounds,promoted by low-valent titanium, gave highly functionlizedcycl[3,2,2]azine derivatives. The coupling reaction proceeded betweenthe carbonyl group and the carbon-carbon double bond, a rare example inMcMurry reaction.

我们以3-苯甲酰基-5-甲酰基中氮茚为原料,通过三碘化钐促进的aldol反应和Wittig反应制备了3-羰基-5-羰基乙烯基中氮茚,随后经低价钛还原偶联,没有生成正常的分子内羰基-羰基偶联产物,而是得到反常的羰基与α,β-不饱羰基的双键偶联产物,较高收率地得到了含多官能团的CycI[3,2,2]azine衍生物。

Results show that, by using thionyl chloride and N,N-dimethyl formamide as chlorinating reagent and dichloromethane as solvent and taking -15℃ as reaction temperature, Z-iomer crystals with pale white color and stable to temperature can be obtained with an overall yield of 70%.

以2-(2-氨基噻唑-4-基)-2-甲氧亚氨基乙酸为原料,经盐酸化、氯代等反应合成了Z-2-(2-氨基噻唑-4-基)-2-甲氧亚氨基乙酰氯盐酸盐;氯代时以用亚硫酰氯和N,N-二甲基甲酰胺的混合物代替五氯化磷作氯化剂,并考察了温度和溶剂对氯代产物中Z-异构体和E-异构体收率的影响。

When bromine was used to bromization reaction with 4-acetyl-guaiacol,the product bromide incompletely or super bromide partial,and the selectivity was poor.

使用单质溴与4-乙酰基愈创木酚进行溴化反应时,产物溴化不完全,或者局部过量的溴化,且选择性较差。

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。

In this paper the study on optimizing the esterification of cellulose and some character of CAB(the degree of substitution of cellulose, solubility, the thermal properties and molecular weight) was discussed. The mechanism of the esterification of cellulose in butyric acid/ acetic acid/ butyric anhydride which comprises the creation of the acetic butyric anhydride, acetyl cation and butyryl cation was investigated by the study of the effect of the content of the organic acid and anhydride on the degree of acetyl and butyryl substitution of cellulose.

最后本文根据纤维素在丁酸/乙酸/丁酸酐中的酯化反应中有机酸以及酸酐的添加量对最后产物纤维素醋酸丁酸酯中乙酯或者丁酯取代度的影响,提出纤维素在丁酸/乙酸/丁酸酐中的酯化反应经历一个混和酸酐以及乙酰碳正离子、丁酰碳正离子的生成过程。

Treatment of dials with N-tert-butanesulfinamide, all biaryl dials were successfully converted into the corresponding bis-imines which were then treated with samarium diiodide to afford diamine products. The absolute configurations of all the intramolecular coupling products were determined by X-ray crystallography.

轴手性二醛与N-叔丁基亚磺酰胺缩合得到相应的亚胺,其为一对非对映异构体。N-叔丁基亚磺酰亚胺在二碘化钐条件下得到的偶联产物,经X-衍射也确定了其立体构型。

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 famciclovir was synthesized from purine by a series of steps by Acylation, Decarboxylation, Reduction ,and so on; Derivatives of these intermediates is described from the 6-chloro- 9H- purin-2-amine as raw materials in different conditions when the iodine and bromide were synthesized with the addition of two intermediate 6-bromo-9H-purin-2-amine and 6-iodo-9H-purin-2-amine; There is elaborated from the main part of a acetophenone, urineaminohydrochloride, phenylhydrazine, ethyl acetoacetate as raw material through a series of reactions to synthetic 3-phenyl-4-formylphenyl pyrazole and 5-chloro-3-methyl-1-phenyl-1H-pyrazole-4-aldehyde two pyrazole aldehyde, and then with 2-amino-6-chlorine-9-(2-methicillin-oxo-co-methyl-4-yl) purine reaction of the two new pyrazole purine Schiff bases.

本论文主是采用以鸟嘌呤为原料,经过一系列的酰基化,脱羧,还原等反应作用下最终得到了产物2-氨基-9-(4-乙酰氧基-3-乙酰氧基甲基丁基)嘌呤;其中的中间体衍生物主要是阐述从以2-氨基-6-氯鸟嘌呤为原料通过在不同的条件下进行溴代与碘代分别合成了另外两种中间体2-氨基-6-溴鸟嘌呤及2-氨基-6-碘鸟嘌呤;还有一部分主要是阐述从以苯乙酮,盐酸氨基脲,苯肼,乙酰乙酸乙酯为原料通过一系列的反应先合成3-苯基-4-醛基吡唑及5-氯-3-甲基-1-苯基-1H-吡唑-4-甲醛这两个吡唑醛,然后再与2-氨基-6-氯-9-(2-甲氧羰基丁酸甲酯-4-基)嘌呤反应得到了两个新型的吡唑嘌呤席夫碱

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If you are unfortunate enough to the lovelorn, please tell me, I will help you out, really, please contact me!

如果你不幸失恋了,请告诉我,我会帮助你摆脱困境,真的,请联系我啦!

China's plan to cut energy intensity by 20 percent and pollutant discharges by 10 percent between 2006 and 2010 is a case in point.

中国计划在2006年到2010间降低20%的能源强度和减少10%的主要污染物排放,就是一个这样的例子。

Well, Jerry would rattle off all the details of that movie.

那么,杰瑞会急促背诵那部电影所有细节。