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从51株细菌和酵母中筛选到能够将苯甲酰丙酮(1)不对称催化还原为3-羟基-1-苯丁酮(2)的8株菌株,其中Yarrowia lipolytica CGMCC 2.150 2(A)和Trichosporon cutaneum CGMCC 2.250 0(B)具有高度的对映选择性[A还原1为(R)-(-)-2,B还原1为(S)-( )-2].A的最佳反应条件为:c(1)=30.9 mmol·L-1.c(A)=200 nag·mL-1,在1%乙醇中,pH6.5的条件下,于38℃反应20 h,(R)-(-)-2收率大于99.0%,e.e.98.7%;B的最佳反应条件为:c(1)=3.1 mmol·L-1.c(B)=200 mg·mL-1,在1%乙醇中,pH 8.0的条件下,于38℃反应36 h,(S)-( )-2收率96.2%,e.e.96.4%. 相似文献
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合成了 2 羟基 4 磺酰氨基苯重氮氨基偶氮苯 (HSDAA) ,并研究了在TritonX 1 0 0表面活性剂存在下HSDAA与镉的显色反应。在pH 8 5~ 1 0 5的Na2 B4 O7 NaOH缓冲溶液中 ,该试剂与镉生成 2∶1型深红色配合物。配合物的最大吸收峰位于 5 2 5nm处 ,表观摩尔吸光系数达 1 84× 1 0 5L·mol- 1·cm- 1。ρ(Cd2 + )在 0~ 480 μg/L范围内符合比耳定律。用拟定方法测定样品中的微量镉 ,结果满意。 相似文献
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取代酰肼化合物是制备偶氮化合物的原料,是一种非常重要的有机化合物,具有广泛的应用价值。它可以和金属形成稳定络合物,对聚烯烃等高分子材料的“铜害”有良好的防护,因而在电线、电缆、钢丝、轮胎等与铜及其它重金属相接触的高分子工业制品中得到广泛应用,被称为金属减活剂[2 相似文献
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Corey氧化剂及其在选择性氧化中的应用 总被引:5,自引:0,他引:5
Corey氧化剂(PCC)是一种为世界公认的有效选择性氧化剂之一,应用非常广泛。本文就1982年以来PCC的发展状况和趋势作一较详细的介绍和评述。包括:一、对醇类的氧化;二,对甾族化合物的氧化;三、对话泼亚甲基的氧化;四、对含活泼碳碳双键化合物的氧化;五、对硅、硼金属有机化合物的氧化;六、载体在PCC选择性氧化中的应用;七、超声泼在PCC选择性氧化中的应用。 相似文献
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利用商品化的高价碘试剂亚碘酰二内酯(Iodosodilactone)作为最终氧化剂, 配合催化量的氮氧自由基2,2,6,6-四甲基哌啶-1-氧自由基(TEMPO)和当量的4-二甲氨基吡啶(DMAP)所组成的反应体系可以将含有不同官能团的伯醇快速高效地氧化为相应的醛且不会发生过度氧化; 将反应体系中的催化剂换为空间位阻较小的氮氧自由基1-甲基-2-金刚烷氮氧自由基(1-Me-AZADO)则可以将仲醇高效地氧化为相应的酮. 值得指出的是, 反应结束后Iodosodilactone的还原态2-碘-间苯二甲酸和DMAP可以通过简单的过滤及酸碱中和处理进行回收, Iodosodilactone的再生可通过用次氯酸钠/盐酸体系氧化2-碘-间苯二甲酸来高效实现. 相似文献
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依据生物活性叠加原理,将邻羟苯基、吡唑啉酮、苯腙基团进行合理组合,构建并合成了2-取代苯腙基-3-(2-羟基苯甲酰腙基)-丁酸乙酯(3a~3f)和1-(2-羟基苯甲酰基)-3-甲基-4-取代苯腙基-吡唑啉酮(4a~4f)两类、共计12种化合物,其中8种化合物未见报道,12种化合物的抑菌活性均未见报道.以芳胺为原料,经重氮化、与乙酰乙酸乙酯反应,与水杨酰肼缩合制得3a~3f,3a~3f经分子内关环制得4a~4f,化合物的结构经IR,1HNMR,元素分析等证实.生物活性测试表明,质量浓度为0.01%时,化合物3b,3c对大肠杆菌的抑菌率高达100%,具有很强的抑菌活性;化合物3a~3f对白色念珠菌、金黄色葡萄球菌的抑菌率均达70%以上,具有较强的抑菌活性;化合物4a~4f对白色念珠菌、大肠杆菌的抑菌率均接近或达到100%,具有很强的抑菌活性,对金黄色葡萄球菌的抑菌率均达78%以上,具有较强抑菌活性;与3a~3f相比,形成吡唑啉酮环后的化合物4a~4f的抗菌活性更高. 相似文献
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A novel and facile synthesis of 4-arylquinolin-2(1H)-ones without metal catalysis has been developed. This reaction involved cyclization/elimination steps and was performed under metal-free conditions using inexpensive reagents such as NaI, selectfluor and KOH. 相似文献
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Synthesis, Crystal Structure and Antibacterial Activity of 1-((2-Chloroquinolin-3-yl)-methyl)-pyridin-2(1H)-one 总被引:1,自引:0,他引:1
S. Mohana Roopan Venkatesha R. Hathwar F. Nawaz Khan Atul Kumar Kushwaha 《结构化学》2010,29(11):1612-1617
On the basis of the interesting structures and biological activities exhibited by several heterocyclic systems possessing the pyridone nucleus such as mappcine and camptothecin, we have planed to design the synthesis, crystal studies and antibacterial activity of the new 1-((2- chloroquinolin-3yl)-methyl)-pyridine-2(1H)-one building block. An X-ray analysis has provided valuable insight into the effect of steric factors on the three-dimensional shape of this compound which serves as a useful advanced intermediate in the synthesis of these biologically active molecules. A multistep synthesis of camptothecin (5) has been designed by retrosynthetic analysis as part of an ongoing program on lead anticancer drug. 相似文献
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Zhen Li Min Yi Hua Zhang Yi Sheng Lai Si Xun Peng 《中国化学快报》2008,19(8):915-917
A one-pot synthesis of 2-(1-acyloxypcntyl) benzoic acids by trapping the carboxylatc/alkoxide dianion with acylating reagents following Grignard addition with n-BuMgBr to 2-formylbcnzoic acid was described. Compared with routine synthetic method, this novel procedure has the advantage of convenient operation and higher yields. 相似文献
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Rajendra K. Kharul Pinkal N. Prajapati Amol A. Thorave Hardik A. Shah Arghya Dhar Darshan A. Joshi 《合成通讯》2013,43(22):3265-3279
A convenient and effective synthesis of novel 1,5-disubstituted 2,1-benzisothiazol-3(1H)-one derivatives is described. The approach involves nitration of inexpensive isatoic anhydride followed by its conversion to 5-nitro-2,1-benzisothiazol-3(1H)-ones in excellent yield and alkylation at the 1-position. The 5-amino group was further derivatized. 相似文献
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The Synthesis of 3-(2'-Hydroxybutyl) isobenzofuran-1 (3H)-one 总被引:1,自引:0,他引:1
l(3H】.Isobenzoturans(Dhthalldes】werereDortedtoexhibitawiderangeofbiologicalactivities.Forexample,3-n-butylphthallde(NB)exhibitsantlasthmatlc’,antlconvuls-ant“actlvltles.PenEandZhouhavestudiedonthemetabolismofNBPInrats‘.Theyfoundthat... 相似文献
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A heteropolyacid efficiently catalyzed the cyclocondensation reaction of 2-aminobenzamide and salicylamide with aldehydes and ketones to afford good yields of benzoxazine and quinazoline ring systems in an aqueous medium. The method gives clean reactions, has simple workup procedure, and uses environment friendly conditions. 相似文献
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A new protocol for the dehydrogenation of dihydropyridazin-3(2H)-one has been carried out by catalytic amount of iodine in dimethyl sulphoxide in good yield with easy workup. 相似文献
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A facile, SbCl3-catalyzed, one-pot, tandem Friedel–Crafts/lactonization reaction of phenols and mandelic acids has been developed under solvent-free conditions to afford 3-aryl benzofuran-2(3H)-ones in good to high yields (52–90%). Additionally, the utility of 3-aryl benzofuran-2(3H)-ones is demonstrated by using them as precursors in the synthesis of a new class of spirocyclic benzofuran-2-ones using classical synthetic methodologies. 相似文献