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The results of clinical assessment showed that levosimendan was safe and effective which could improve the prognosis of the patients and kept normal blood kinetics. By improving the reported synthetic route, levosimendan was synthesized from acetanilide via eight steps of reaction.

本论文探索了左西孟旦的合成路线,对文献报道的合成工艺进行了合理有效的改进,以乙酰苯胺为原料,最终经Friedel-Crafts反应,羰基α-位溴代,丙二酸二乙酯缩合,水解,脱羧,环合,拆分及重氮化加成等八步反应合成了左西孟旦。

The results indicate that the optimized sulfonylation reaction time is 4 h, the materiel rate of chlorosulfonic acid and 2-chloroimidazo[1,2-α]pyridine is 1.2 : 1, with ethylamine the yield increasing from 15.4% to above 70%; the optimized ammonolysis reaction time is 3 h and the reaction temperature is 27℃, with the acetonitrile yield increasing from 60.1% to above 79.6%.

实验结果表明,磺酰化反应的最佳反应时间为4 h,氯磺酸与2-氯咪唑并[1,-α]吡啶的用量比为1.2:1,加入三乙胺可将收率由15.4%提高到70%以上;氨解反应的最佳反应时间为3 h,反应温度为27 ℃,加入乙腈可将收率由60.1%提高到79.6%;方案经改进后,总反应时间缩短3 h,收率提高了5.5%。

The activity of the co-catalysts consisting of H form zeolites ( HY, H-β and HZSM-5) and SnO in the reaction of anisole with acetyl chloride mainly depended upon the SiO2/Al2O3 molar ratio of the zeolite used.

由H型沸石(HY和H-ZSM-5沸石)和SnO组成的复合催化剂在苯甲醚与乙酰氯的酰化反应中的催化活性主要取决于所用沸石的硅铝比。

In the acylation reaction between anisole with acetyl chloride, The catalyst of ZnCl〓/HY-98 prepared by MWI had the best catalytic activity and the selectivity of p-methoxy acetopheone. The catalytic active centers were ZnCl〓 dispersed in zeolite and the Bronsted acid sites in HY-98 zeolite itself.

在苯甲醚与乙酰氯的酰化反应中,微波固相法制备的ZnCl〓/Y催化剂有相对较好的催化活性和选择性,起催化作用的主要是分散在分子筛表面的ZnCl〓和分子筛本身的B酸。

Methods The propylbridged biferrocenyl substituted pyridazinone was synthesized by the reaction of propylbridged biferrocene with ethyl succinyl chloride, and then condensed with hydrazine hydrate.

双二茂铁丙烷先与丁二酸单乙酯酰氯发生酰化反应,生成的1,4酮酸酯再与水合肼缩合得到含有双二茂铁丙烷的哒嗪酮衍生物。

Highly selective acylation at C-5 of indole was realized and a new method was established in the synthesis of TIMs.

采用三氟乙酰基作为吲哚C-3的保护基团,在路易酸催化下使吲哚的酰化反应高选择性地发生在5-位。

In a system consisting of 20% PEG 400 and 12% magnesium sulfate, the partition coefficient of PGA was less than 0.01, PGA almost completely partitioned into the magnesium sulfate-rich bottom phase. Meanwhile, the partition coefficient of cephalexin was 6.7, the partition coefficients of phenylglycine methyl ester and 7-ADCA were 1.5 and 1.2, respectively.

通过考察头孢氨苄、苯甘氨酸甲酯和7-氨基脱乙酰氧基头孢烷酸(7-ADCA)在ATPS中的分配行为建立了一个含20%PEG 400和12%硫酸镁的ATPS,在此体系中头孢氨苄的分配系数为6.7,苯甘氨酸甲酯的分配系数为1.5,7-ADCA的分配系数为1.2,且青霉素酰化酶的分配系数小於0.01。

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。

These changes were prevented by genistein (a protein tyrosine kinase inhibitor) and antioxidant N-acetyl-L-cysteine, but promoted by sodium orthovanadate (a protein phosphatase inhibitor), which were administered to the SD rats 20 min before ischemia.

进一步的研究表明,缺血前20 min腹腔注射给药,然后缺血30 min,发现蛋白酪氨酸激酶抑制剂染料木黄酮和抗氧化剂N-乙酰半胱氨酸能显著地抑制核内STAT3的磷酸化水平及DNA结合活性的增加(磷酸化水平从2.3和2.5倍分别降为1.2和1.4倍, DNA结合活性则从2.8和3.7倍分别降为1.1和1.5倍),而蛋白酪氨酸磷酸酶抑制剂矾酸钠则能明显地促进他们的增高(磷酸化水平从2.0倍增到3.4倍, DNA结合活性从3.1倍增为5.1倍)。

Furthermore, proton singlets of Fmoc group were treated as internal standard because of their station in both starting material and product.

用HR/MAS NMR分析技术不仅跟踪优化了固相羟基氨基酸的糖基化反应条件,而且选择固载在树脂上的糖基化Nα-Fmoc保护羟基氨基酸〓H NMR中最低场,且分辨好的Fmoc保护基信号做为内标,糖上乙酰基的积分面积为标准直接定量了键合在Tenta Gel S NH〓树脂上氨基酸甙化的产率。

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