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Six novel dihydrobenzofuran and benzofuran neolignans compounds(1~6) were synthesized by knoevenagel reactiton,esterfication, biomimetic oxidative coupling ,DDQ dehydrogenation,reduction and hydrolysis with 4-hydroxybenzaldehyde and malonic acid as starting material.

以对羟基苯甲醛和丙二酸为原料,经Knoevenagel缩合反应,酯化、仿生氧化偶联、DDQ脱氢、还原和水解等反应步骤,合成了6种未见文献报道的苯并二氢呋喃新木脂素和苯并呋喃新木脂素类化合物(1~6)。

A better understanding of the role of PPAR in insulin action system will be critical in developing more efficacious and safe agent s that act on PPAR and benefit patients with type 2 diabetes. The main content is followed: Synthesis and analysis of 1,3-dicarbonyl compounds. Make use of easily available cheap reagent such as 2-naphthol, 6-hydroxyquinoline, 1,2-dibromoethane, 4- hydroxybenzaldehyde, dimethyl malonate, 2-{4- [(2-napthoxy)ethoxyl] benzyl} malonates and 2-{4 [(1,2,3,4-tetrahydro-6 -quinolinoxy)ethoxyl] benzyl } malonates were synthesized through 6-8 steps in virtue of Williamson, Knoevenagel reaction, Pd/C catalyzed hydrogenation with mild conditions and high yield. The total yield of 40-50%.

本论文的主要内容和研究结果如下: 1,3-二羰基类化合物的合成及分析,采用2-萘酚、6-羟基喹啉、1 ,2二溴乙烷、对羟基苯甲醛、丙二酸二甲酯等常见易得试剂,利用Williamson反应、Knoevenagel反应、钯碳加氢等条件温和且收率高的方法,分别合成了2-{4- [(2-萘氧)乙氧基]苄基}丙二酸衍生物和2-{4 [(1,2,3,4-四氢-6-喹啉氧基)乙氧基]苄基}丙二酸衍生物两个系列8个化合物,经6-8步反应,总收率为40-50%,具有一定绿色化学特性。

Isolation, purification and characteristics of D-hydantoinase were carried out. The experiment results showed that the optimal pH and temperature of pure D-hydantoinase were pH 8. 5 and 35℃, respectively. D-hydantoinase activity could be increased significantly by Mn〓 and Fe〓. Substrate specificity of D-hydantoinase on various hydantoin derivatives showed the optimal substrate of D-hydantoinase was 5-phenylhydantoin, but hydantoin, 5-methylthioehylhydantoin, 5-hydroxyphenylhydantoin, 5-methylhydantoin, 5-benzylhydantoin could also be hydrolyzed by D-hydantoinase.

本文还进行了海因酶的分离纯化及性质研究,发现酶的最适反应温度为35℃,最适pH为8.5,金属离子Mn〓和Fe〓能显著提高D-海因酶活力。D-海因酶的特异性实验表明,D-海因酶的最适底物为D,L-苯海因,其次为海因,D,L-对羟基苯海因和D,L-甲硫乙基海因,对D,L-甲基海因和D,L-苯甲基海因也有一定的作用。

Novel organic silane of 3,3′-dihydroxyldiphenoxydimethyl alkoxy silane and 3,3′,3-trihydroxyldiphenoxydimethylalkoxy silane triglycidyl ether for epoxy resin modification were synthesized.

研究了含酚羟基有机烷氧基硅烷及3,3′,3-三羟基苯氧基硅烷三缩水甘油醚两种新型有机硅改性剂对双酚F环氧树脂力学性能及热性能的影响。

A compound 2-(3-hydroxyphenyl)[60] fullerene pyrrolidine was synthesized by the 1,3-dipolar cycloaddition reaction of the fullerene(C60) and azomethine ylide (prepared from glycine and 3-hydroxybenzaldehyde). The product was characterized by UV-Vis,1H-NMR ,FT-IR and MS. The reaction conditions affecting the yields of product were investigated and the optimum reaction conditions with product yield 75%(based on consumed C60) were:molar ratio of C60∶3-hydroxybenzaldehyde:glycine 1∶3∶6,reaction temperature 95℃,reaction time 18h.

利用甘氨酸和3-羟基苯甲醛与C60发生1, 3-偶极环加成反应,合成分离得到了2-(3-羟基苯基)[60]富勒烯吡咯烷,用UV-Vis、1H-NMR、FT-IR、MS等测试手段表征了产物的结构,并通过单因素方法,探讨了反应条件对产物产率的影响,得到最佳工艺条件:反应物摩尔比1∶3∶6,温度95 ℃,反应时间18 h,产物的产率可达75%(以消耗的C60计)。

Crumb rubber asphalt concrete leachates contain the organic mixture and metallic contaminants,such as, benzothiazole ,2-hydroxybenthiazoles and 2-(4-morpholino) benthiazole, mercury, aluminum .

橡胶粉沥青混泥土沥出液是一种含有苯噻唑、2 羟基苯噻唑和 2 (4 )吗啉代苯噻唑等有机物化合物和汞、铝等金属杂质的混合物。

To synthesize the octreotide, Phe-Leu-Glu-Glu-Leu and C_(15)H_(31)-CO-Lys-Thr -Thr-Lys-Ser peptides, the strategies are as followings: Fmoc- group as protective group for α-NH_2; TBTU, DIEA and HOBt as coupling reagent; and ethanedithiol -phenol - thioanisole - H_2O - TFA ( 2.5:5:5:5:82.5 , V/V ) as cleaving solution.

采用Fmoc固相合成法,以苯并三哗四甲基脲四氟硼酸盐、二异丙基乙胺和1-羟基苯骈三氮唑为缩合剂;苯酚—乙二硫醇—苯甲硫醚—水—三氟乙酸(5:5:2.5:5:82.5,V/V)为切割试剂,合成了奥曲肽、Phe-Leu-Glu-Glu-Leu及C_(15)H_(31)-CO-Lys-Thr-Thr-Lys-Ser三种小分子多肽,并对奥曲肽的合成规模进行了放大。

Carboxybenzyloxy)phenylacetic acidwas synthesized from 4-Hydroxyphenyl acetic acidand phthalide in the presence of the catalyst sodium methoxide.

采用对羟基苯乙酸和苯酞为原料,在甲醇钠的催化下,以n∶n∶n=1.0∶1.1∶2.2,于130℃反应7h制备4-(2-羧基苄氧基)苯乙酸。

Results Eleven compounds were obtained and identified as sarcodonin A, scabronine B, 3β-hydroxy-5α, 8a-epidioxyergosta-6, 22-dien,(22E, 24R)-ergosta-7, 22-diene-3β, 5α, 6β-triol,(22E, 24R)-ergosta-7, 22-diene-3β-ol, benzoic acid, 4-hydroxylben-zaldehyde, 4-monopropanoylbenzenediol, ethy1-β-D-glucopyranoside, thioacetic anhydride,(2S, 2'R, 3S, 4R)-2-(2-hydroxyoctadecanoylamino) docosane-1, 3, 4-triol.

结果共分离鉴定了11个化合物,分别是:sarcodonin A、scabronine B、3β羟-5α,5α-过氧麦角甾-6,22-二烯-3β-醇、(22E,24R)-麦角甾-7,22-二烯-3β,5α,6β三醇、(22E,24R)-麦角甾-7,22-二烯-3β-醇、苯甲酸、对羟基苯甲醛、对羟基苯甲酸乙酯、乙基-β-D-吡喃葡萄糖苷、硫代乙酸酐、(25,2'R,3S,4R)-2-(2-羟基-十八碳酰胺)二十二碳烷-l,3,4-三醇。

Methods 4-Hydroxy- benzonitrile was treated with sodium hydrogen sulfide and anhydrous magnesium chloride in dimethyl formamide to give thioamide, which was then directly cyclized with ethyl 2-chloroacetoacetate without separation to give ethyl 2-(4-hydroxyphenyl)-4-methylthiazole-5-carboxylate(2) in one-pot; then 2 was formylated with Duff reaction adopting hexamethylenetetramine in trifluoroacetic acid to give ethyl 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylate(3); finally, the target compound was obtained by the treatment of 3 with hydroxylamine hydrochloride and sodium formate in formic acid.

采用&一勺烩&方法,以4-羟基苯甲腈为起始原料,首先与硫氢化钠和无水氯化镁在N,N-二甲基甲酰胺中反应,所得中间体不经分离,直接加入2-氯乙酰乙酸乙酯进行环合反应,得到2-(4-羟基)苯基-4-甲基-5-噻唑甲酸乙酯(2);然后通过六亚甲基四胺/三氟乙酸进行Duff反应,得到2-(3-甲酰基-4-羟基)苯基-4-甲基-5-噻唑甲酸乙酯(3);再经盐酸羟胺/甲酸/甲酸钠体系脱水得到目标化合物。

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