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酰化

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The key steps involved Friedel-Crafts reaction of o-cresol and the Wittig reaction for construction the skeleton of amine moiety,at the same time, using the synthesis of E,(7S)-7-methoxytetradec-4-enoic acid in chapter 2,and Johnson-Clainsen rearrangement as a key step for construction the fatty acid part,the corresponding acid was prepared in 23%and 50%overall yield,respectively.

随后将手性不饱和脂肪酸和氨片段进行酰胺化反应构筑了malyngamide M的基本骨架,再将Z-烯氯转化为E-烯氯完成了目标分子的全合成,高立体选择性地构筑了末端烯氯结构,为制备其它含有类似烯氯结构的malyngamides探索出行之有效的合成路线。

The synthesis of the pentacyclic skeleton of Et-743 and the construction of the five chiral centers thereof.1. The core pentacyclic skeleton of phthalascidin was constructed with L-dopa as the starting material via thirteen steps. First, two basic synthons, the C-1 functionalized tetrahydroisoquinoline compounds 8 and N-protected Z-dopa derivative 9, were prepared from L-dopa. They were coupled via amide bond to form the dipeptide compounds 10, which were the first key intermediates. Then the primary hydroxyl groups were transformed into the corresponding amino aldehydes 11 via Swern oxidation. Followed by the intramolecular Pictet-Spengler cyclization, the pentacyclic compounds 12 were synthesized.

五环骨架的构建及五个正确手性中心的确立:1.1我们以L-多巴为起始原料,经过多步官能团保护和转化合成了基本结构单元8然后和苯丙氨酸衍生物9,通过缩合反应生成酰胺中间体10,经Swern氧化得到醛化合物11,然后再次利用分子内改良的Pictet-Spengler反应一步构建c,d两环,得到五环骨架化合物12,最后,实现了21-位羰基向氰基的转化,得到了C-1位官能化的化合物14,化合物14不但具有和Et-743一致的五环骨架,而且分子中五个手性中心立体构型也与其完全相同:其中,3,位和13,位的手性中心由原料L-多巴带入,而1,位,11,位和21,位手性中心则通过不对称诱导而确立。

The same is carried out in the microwave, ethanol, dichloroethane, sodium carbonate, tetrabutylammonium iodide ammonium dissolved in dimethylformamide, then access to carbon dioxide.

同样是在微波炉中进行,把乙醇,氯乙烷,碳酸钠,四丁基碘化铵溶解在二甲基甲酰胺中,再通入二氧化碳。

With brain stereotaxis technique PP2A was inhibited in the nucleus basalis of Meynert and the cytoskeletal protein tau, neurofilament were found hyperphosphorylated and aggregating. The neurite became short and thickening, acetyltransferase aggregated in the body of neuron and the acetylcholine level in the nucleus basalis of Meynert was significantly decreased followed with spatial memory defict of rats.

利用立体定位技术抑制大鼠基底核PP2A活性,使基底核神经元微管相关蛋白tau及神经细丝出现过度磷酸化和聚积,轴突变短增粗,胆碱乙酰转移酶在胞体聚集,而使基底核乙酰胆碱含量降低,大鼠出现空间记忆障碍。

The N-alkylation of N-monosubstituted sulfonamide s with alkyl halides promoted by KF using ionic liquids as reaction media was reported in this paper.

报道了KF作用下离子液体介质中N-单取代磺酰胺和卤代烃的N-烷基化反应,考察了4种不同结构的离子液体BF4、BF4和PF6对反应的影响。

Phosphine generally require long exposure periods, whereas methyl bromide and sulfuryl fluoride provide a rapid fumigation that can be completed in less than 4 days, often within 24 hours.

磷化氢一般需要较长的密闭时间,而溴甲烷和硫酰氟则适合快速熏蒸,可在不到4天之内完成熏蒸工作,一般在24小时内完成。

Monochloroethylene carbonate is prepared by chlorination of ethylene carbonate with sulfuryl chioride ,a solution of monochloroethylene carbonate in ethylene carbonate is reacted with triethylamine to give vinylene carbonate.A parameter design method was applied to select the optimum synthesis conditions.63.3% and 78% yields superior to the conventional for monochloroethylene carbonate and vinylene carbonate were obtained respectively,and the process was also simplified .

以碳酸乙烯酯为原料,用磺酰氯作为氯化剂生成一氯代碳酸乙烯酯,三乙胺为脱卤化剂在碳酸乙烯酯溶剂中合成碳酸亚乙烯酯,对一氯代碳酸乙烯酯和碳酸亚乙烯酯制备的工艺参数进行优化,收率分别达到63.3%和78%,均超过了传统方法,且简化了工艺,缩短了反应时间,易于工业化生产。

Methods 42 Wistar male rats of hepatic fibrosis were induced by TAA and divided into 7 groups randomly (n=6). The rats of 1 model group were sacrificed every 2 weeks.

60只雄性 Wistar大鼠应用硫代乙酰胺饮用水喂养,制备肝纤维化模型。42只大鼠模型制备成功后,随机分为 7 组,每组6只。

The influentical factors on the synthesis of L-serine methyl ester hydrochloride with thionyl chloride were studied and optimized.

对亚硫酰氯法制备L-丝氨酸甲酯盐酸盐的影响因素进行试验及优化,较佳工艺条件下酯化收率可达85.0%以上,产品含量≥98.0%。

O-(1-Arylseleno-3-azido)isopropyl-O-2-(N3-tegafur)alkyl thiophosphate (3a~3f) were obtained via nu-cleophilic ring-opening of sodium azide to 2a~2f in dry DMF at room temperature, and their antitumor activities were tested.

以无水N,N-二甲基甲酰胺作溶剂,室温下,叠氮化钠中对2a~2f进行亲核开环,得到O-(1-芳硒基-3-叠氮基)异丙基-O-2-(N3-替加氟)乙基硫代磷酯。

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The labia have now been sutured together almost completely.The drains and the Foley catheter come out at the top.

此刻阴唇已经几乎完全的缝在一起了,排除多余淤血体液的管子和Foley导管从顶端冒出来。

To get the business done, I suggest we split the difference in price.

为了做成这笔生意,我建议我们在价格上大家各让一半。

After an hour and no pup, look for continued contractions and arching of the back with no pup as a sign of trouble.

一个小时后,并没有任何的PUP ,寻找继续收缩和拱的背面没有任何的PUP作为一个注册的麻烦。