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酰胺化

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In this paper, acrylamide-crylic acid hydrosol was synthesized by copolymerizating of acrylamide and crylic acid monomers in aqueous solution.

本文采用共聚法合成了丙烯酰胺-丙烯酸水溶胶,利用羟基化碳纳米管增加其强度和稳定性,制备成了具有温度和pH双重敏感特性的凝胶薄膜。

It was detected by DSC that the temperature of imide and crosslinking reaction are differentiated by the catalysis of acetyl acetone copper and rare earth.

DSC研究表明乙酰丙酮铜催化剂和稀土催化剂可以分开低聚物的亚胺化和交联反应温度。

The auxiliary can be recovered in high yield (81%) only by filtering and recrystallization. Besides, some other aldehydes have been chosen to test the enantioselectivity of N,N\'-dibenzyl tartamide, in comparison with two other allylaborates reagents developed previously by Roush and Brown, respectively. The results show that %e.e. of homoallylic alcohol is superior to that of the former, and approaches the Brown reagent.

产物经S_N2反应得瑞格列萘中间体-甲基烯丙基-2-氯苯基-叠氮甲烷(17);同时,将筛选出的新型手性配体N-苄基酒石酸二酰胺用于其他几种醛(正丁醛,异戊醛和环己醛)的不对称烯丙基化反应,并与广泛应用的Roush配体(22)和Brown配体(27)相比较,发现其立体选择性优于Roush配体,并接近Brown配体,但明显具有可回收利用的优势。

This invention is directed to the-tartaric acid salt of 2-amino-N-{1-(2,4-difluoro-benzyloxymethyl)-2-oxo-2-3-oxo-3a-pyridin-2-ylmethyl-2-(2,2,2-trifluoroethyl-2,3,3a, 4,6,7-hexahydro-pyrazolo(4,3-c) pyridin-5-yl-ethyl}-2-methyl-propionamide which is a growth hormone secretagogue and as such is useful for increasing the level of endogenous growth hormone.

本发明涉及2-氨基-N-{1--(2,4-二氟-卞氧甲基)-2-氧代-2-3-氧代-3a-(R-吡啶-2-基甲基-2-(2,2,2-三氟-乙基)-2,3,3a,4,6,7-六氢化-吡唑子基(4,3-c)吡啶-5-基-乙基}-2-甲基-丙酰胺的--酒石酸盐,它是一种生长激素促分泌素,并且可用于提高内源性生长激素水平。

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。

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。

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。

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。

Started from D-tyrosine, we obtained the tetramic acid 96 using Jouin reaction. The assembly of the second fragment 109 was stared from 1,4-butandiol,using asymmetric alkylation reaction developed by Oppolzer as a key step. Coupling of the tetramic acid 96 with 109 provided the key intermediate 110 according to Yoshii\'s procedure. After remove protective group and Sharpless epoxidation, we obtained the key intermediate 113. Its macrocyclization to form the final product is in progress.

本论文的第二章主要对Macrocidin A开展了合成工作,我们从D构型的酪氨酸出发,经过官能团转换;利用Jouin反应生成Tetramic acid 96,另外一个片断从1,4-丁二醇开始经过多步反应生成碘化物104,利用Oppolzer发展的手性樟脑磺酰胺为辅基参与的不对称烷基化反应,引入手性甲基,生成关键中间体109,接着通过Yoshii发展的方法连接96和109生成110,经过Sharpless不对称环氧化反应建立环氧化合物,然后脱去保护基得到关环前体113,分子内的Mitsunobu反应进行关大环反应正在进行之中。

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啊!不用提了。提到肉,真是糟透了。

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