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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。

The partial substitution of α-olefine sulfonate instead of alkylbenzene sulfonate and the production technology of α-olefine sulfonate were also described.

介绍近几年来大型磺化反应器和磺化装置的国产化及原有磺化装置的技术改造,α-烯基磺酸盐部分取代烷基苯磺酸盐及AOS生产技术,并概述了脂肪酸甲酯磺酸盐的产品开发、磺化产品的活性物干燥,以及其他磺化产品的开发等。

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。

One synthetic strategy started fromγ-butyrolactone 38, from which a cyclohexadiene intermediate 30 was prepared in an overall yield of 44% in a 7-step procedure after y-butyrolactone underwent a-bromination, dehydrobromination, Diels-Alder reaction, aminolysis, benzylation, bromination and dehydrobromination, with the key step being the Diels-Alder reaction under harsh condition.

其中一个路线从γ-丁内酯38开始,连续经过α-溴化、脱溴化氢、Diels-Alder反应、胺解、苄基化、溴化和脱溴化氢共7步反应,制备了一个环己二烯衍生物30,总产率44%,关键步骤是高温高压下Diels-Alder反应。

We studied DBU-mediated Ireland-Claisen rearrangement. Using DBU as the base for enolization of allylic esters of unsaturated acids 9-16, we found a novel DBU-mediated tandem Ireland-Claisen rearrangement /isomerization reactions and established a consecutive Ireland-Claisen rearrangement /Cope rearrangement.

利用DBU作为烯醇化碱,对含有活泼质子的烯酸烯丙酯类化合物9-16的Ireland-Claisen重排进行了系统的研究,创建了一条新颖的DBU-促进的Ireland-Claisen重排/异构化串联反应及Ireland-Claisen重排/Cope重排的串联反应路线。

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。

The latices were stable ,thixotropic and monodisperse .The particle sizes range from 192 to 94 nm depending on the acrylamide fractions. The Hofmann reactions of these latices were carried out to introduce primary amines on the particle surface.

由于一直以来,丙烯酰胺-苯乙烯的共聚物胶乳只能用于制备两性胶乳,为了得到较高的胺化度,我们对不同单体配比的丙烯酰胺-苯乙烯共聚物胶乳进行Hofmann反应,探讨了丙烯酰胺在单体中所占的比例对Hofmann反应的影响。

Generally, these compounds are derived from accessible α–oxoketen dithioacetals and the common methods of preparation involve regioselective sodium borohydride 1,2-reduce of α–oxoketen dithioacetals, 1,2-nucleophilic addition of organomatals such as organomagnesium, organolithium, Reformatsky regent to α–oxoketen dithioacetals, Baylis-Hillman reaction between polarized ketene dithioacetals and aldehydes.

主要方法包括:使用硼氢化钠1,2-选择性还原α-羰基二硫缩烯酮;利用有机金属化合物(如有机镁试剂,有机锂试剂,Reformatsky试剂等)对α-羰基二硫缩烯酮进行1,2-亲核加成;通过α-羰基二硫缩烯酮与芳醛进行Baylis-Hillman反应等获得。

The C_(60)-fused tetrahydrofuran derivatives are excellent synthons for further functionalization.While treated with different equiv,of BF_3·OEt_2 at various temperature,several novel functionized fullerene derivatives have been successfully synthesized.2.1,4-Fullerenols C_(60)ArOH were synthesized via the reaction of[60]fullerene with 4-substituted phenylhydrazine hydrochlorides and sodium nitrite under moisture and aerobic conditions.

这种四氢呋喃环合富勒烯衍生物作为一个合成中间体又可发生进一步的衍生化反应,其与不同当量BF_3·OEt_2在不同温度条件下可以得到二氢呋喃环合富勒烯衍生物、三元环合富勒烯衍生物等。2。

Allyl-functional novolac with allylation degree of 173 % was synthesized , followed by copolymerizing with 4 , 42bismaleimide biphenyl methane at a mass ratio of 1∶1 to obtain BMI2modified allyl-functional novolac (BMAN173) resin.

制备了烯丙基化程度可达 173 %的烯丙基酚醛树脂(AN173),并与双马来酰亚胺以 1 ∶1 的质量比进行共聚,制备了双马改性的烯丙基酚醛树脂(BMAN173)。

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Lao Qiu is the Chairman of China Qiuyang Translation Group and the head master of the Confucius School. He has committed himself to the research and promotion of the classics of China.

老秋先生为中国秋阳翻译集团的董事长和孔子商学院的院长,致力于国学的研究和推广。