酰胺型茄呢醇衍生物的合成与生理活性

酰胺型茄呢醇衍生物的合成与生理活性;N-茄呢基酰胺;N-酰基-N′-茄呢基哌嗪;合成;生理活性     

茄呢基氮芥衍生物的合成及生理活性

茄呢基氮芥衍生物的合成及生理活性;氮芥;茄呢醇;合成;生理活性     

二元酸茄呢醇乙酰葡萄糖二酯的合成及其生物活性

二元酸茄呢醇单酯;体外活性;二元酸茄呢醇乙酰葡萄糖二酯的合成及其生物活性     

N-茄呢基-N,N'-二(3,4-二甲氧基苄基)乙二胺的合成

茄呢基溴;;抗肿瘤药;N-茄呢基-N;N'-二(3;4-二甲氧基苄基)乙二胺的合成     

茄呢基胺类化合物的合成研究(Ⅰ)——N,N-二(酰氧基乙基)茄呢基胺的合成

茄呢基胺类化合物的合成研究(Ⅰ)——N;N-二(酰氧基乙基)茄呢基胺的合成     

茄呢基胺-氮芥衍生物的合成

首次设计并制备了二种以茄呢基胺和茄呢基哌嗪为载体的新型氮芥衍生物.即以二 (2 氯乙基 )胺盐酸盐为原料与邻苯二甲酸酐反应,合成出含有抗肿瘤活性基团的化合物 2 { [二 ( 2 氯乙基 )氨基 ]羰基 }苯甲酸,然后在二环己基碳二亚胺存在下,分别与茄呢基胺和茄呢基哌嗪进行酰化反应,得到两种含茄呢基胺类基团的氮芥衍生物,其结构经元素分析,IR,1HNMR和MS确证.     

N-酰基-N′-茄呢基哌嗪衍生物的合成及生物活性

以茄呢醇为起始原料和茄呢基哌嗪为关键中间体合成了 4个N 酰基 N′ 茄呢基哌嗪 ( 4a～ 4d) ,以及 2个含葡萄糖单元的N ( 2 全乙酰葡萄糖基苯甲酰基 ) N′ 茄呢基哌嗪 ( 5 )和N ( 2 葡萄糖基苯甲酰基 ) N′ 茄呢基哌嗪 ( 6) ,共 6个新茄呢基哌嗪衍生物 .其结构经元素分析 ,IR ,1HNMR和MS确证 .测试了化合物 4c ,5 ,6对三种人癌细胞 (Bel 740 2 ,KB ,HCT 8)的体外生理活性 ,初步结果表明化合物 6比 4c和 5对三种所测细胞有更好的抑制效果     

N-酰基-N''''-茄呢基哌嗪衍生物的合成及生物活性

以茄呢醇为起始原料和茄呢基哌嗪为单元的N-(2-全乙酰葡萄糖基苯甲酰基)-N'-茄呢基哌嗪(5)和N-(2-葡萄糖基苯甲酰基)-N'-茄呢基哌嗪(6),共6个新茄呢基哌嗪衍生物.其结构经元素分析,IR,1H NMR和MS确证.测试了化合物4c,5,6对三种人癌细胞(Bel-7402,KB,HCT-8)的体外生理活性,初步结果表明化合物6比4c和5对三种所测细胞有更好的抑制效果.     

N-茄呢基谷氨酰胺类化合物的合成

在N,N 二环己基碳二酰亚胺存在下,N 苯甲酰 Nα 茄呢基 L 谷氨酰胺酸和N 羟基琥珀酰亚胺反应制成活化酯,然后分别与胺或者氨基酸甲酯盐酸盐反应制得3种新N 茄呢基谷氨酰胺类化合物.这些化合物的结构经IR、1HNMR、MS和元素分析确证.     

N-茄呢基胺类糖酯化合物的合成及生理活性

在氢氧化钠和四丁基溴化铵存在下,将化合物2-N-茄呢基胺基苯甲酸(3)和N-茄呢基己二酰胺酸(6)分别与O-乙酰基溴代葡萄糖、O-乙酰基溴代半乳糖、O-乙酰基溴代乳糖和O-乙酰基溴代麦芽糖反应制得对应的糖酯4a～4d和7a～7d,由元素分析,IR,1H NMR和MS确证了8个新化合物的结构,并对其中6个化合物(4a,4d和7a～7d)在三种癌细胞模型上进行了一些初步体外生理活性的测试.     

二氧化碳和丙烯直接合成甲基丙烯酸的NiPMo/TiO2催化剂的研究

用溶胶-凝胶法以磷钼酸(MPA)的镍盐溶液水解钛酸四丁酯制备了NiPMo/TiO2催化剂.使用ICP、 XRD、 TG-DTA、 IR、 TPD-MS和微反应技术研究了催化剂的化学组成、热稳定性、化学吸附性质和催化反应性能.杂多钼酸盐与TiO2通过O2-在TiO2表面发生了键合.在623 K下,杂多阴离子仍保持原有的Keggin结构.CO2在Lewis酸位Ni(Ⅱ)和Lewis碱位Ni-O-Mo的桥氧协同作用下生成CO2卧式吸附态Ni(Ⅱ)←O-(CO)←(O--Ni).丙烯有多种吸附态在催化剂上吸附.在563 K、 1 MPa和空速1500 h-1的反应条件下,丙烯的摩尔转化率为3.2%,产物MAA选择性为95%.     

Toward new camptothecins. Part 6: Synthesis of crucial ketones and their use in Friedländer reaction

In the context of the preparation of camptothecin and luotonin A analogs, the synthesis of some key keto-precursors and their use in Friedländer condensation are described. This paper also focuses on the stability of these keto intermediates and emphasizes the major differences between indolizinones and pyrroloquinazolinones series. Noteworthy is also the report of some original structures isolated as by-products of some experiments.     

CoFe2O4自形成磁性液体场致结构化对磁化的影响

The Langevin paramagnetic theory can’t describe the relation between magnetization of ferrofluids and applied magnetic field. The structuralization of ferrofluids, which is considered the main influence factor of the magnetization, is regarded. The part of magnetization works is deposited when the structure is forming. This action influences the magnetization of ferrofluids directly or indirectly. On the base of the “compressing” model, the Langevin function that usually describes the magnetization of ferrofluid is modified, and a well-fitted curve is obtained. An equation of the relation between the equivalent volume fraction after being “compressed” and the intensity of magnetic field is discovered, which approximately describes the process of magnetization. The relation between the approximate initial susceptibility and the volume fraction can be obtained from modified formula.     

Highly regioselective Buchwald–Hartwig amination at C-2 of 2,4-dichloropyridine enabling a novel approach to 2,4-bisanilinopyridine (BAPyd) libraries

The highly regioselective Buchwald–Hartwig amination at C-2 of the cheap and readily accessible reagent, 2,4-dichloropyridine with a range of anilines and heterocyclic amines is described. This new methodology is robust and provides a facile access to 4-chloro-N-phenylpyridin-2-amines on 0.25 mol scale. These intermediates undergo a further Buchwald–Hartwig amination at higher temperature to enable rapid exploration of the chemical space at C-4 and to provide a library of 2,4-bisaminopyridines.     

KMnO4-mediated oxidative CN bond cleavage of tertiary amines: Synthesis of amides and sulfonamides

KMnO₄-mediated oxidative CN bond cleavage of tertiary amines producing secondary amine was introduced, which was trapped by electrophiles (acyl chloride and sulfonyl chloride) to form amides and sulfonamides. The reaction could take place at mild condition, tolerating a wide range of function groups and affording products in moderate to excellent yields.     

Chemistry of heterocyclic compounds at the A. E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences, over 50 years (Review)

The review contains a concise historical account and information on the most significant researches undertaken by the staff at the A. E. Favorsky Irkutsk Institute of Chemistry, Siberian Branch of the Russian Academy of Sciences on the Chemistry of Heterocyclic Compounds. Dedicated to Academician of the Russian Academy of Sciences B. A. Trofimov on his 70th jubilee. Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 10, pp. 1443–1502, October, 2008.     

Sulfur-directed metal-free and regiospecific methyl C(sp3)–H imidation of thioanisoles

Regiospecific and direct imidation of the methyl C(sp³)–H bond of thioanisoles is realized under mild and metal-free conditions with N-fluorobis(benzenesulfonyl)imide as an oxidant and nitrogen source. Proposed mechanism suggests that thionium ion intermediates and a Pummerer-type reaction are involved. The imidation has advantages such as high step-economy, excellent functionality tolerance, and regiospecificity, giving structurally diverse imidation products.     

Selective syntheses of 2H-1,3-oxazines and 1H-pyrrol-3(2H)-ones via temperature-dependent Rh(II)-carbenoid-mediated 2H-azirine-ring expansion

The Rh(II)-catalyzed reaction of 2-carbonyl-substituted 2H-azirines with ethyl 2-cyano-2-diazoacetate or 2-diazo-3,3,3-trifluoropropionate provides an easy access to 2H-1,3-oxazines and 1H-pyrrol-3(2H)-ones. These compounds can be selectively prepared from the same starting material using temperature as the only varied parameter. The 2-azabuta-1,3-diene intermediate, a common precursor for both heterocyclic products, isomerizes into 2H-1,3-oxazine under kinetic control, while 1H-pyrrol-3(2H)-one is the sole product of the reaction at elevated temperatures. According to DFT-calculations a one-atom oxazine ring contraction involving ring-opening to a 2-azabuta-1,3-diene intermediate, followed by a 1,5- and 1,2-prototropic shift leads to the consecutive formation of imidoylketene and azomethine ylide, which then further undergo cyclization to the pyrrole derivative.     

Synthesis of 1-benzyloxypyrazin-2(1H)-one derivatives

Different approaches for the synthesis of 1-benzyloxypyrazin-2(1H)-one derivatives from simple amino acids have been investigated. A library of 33 precursors for the preparation of N-hydroxy pyrazinones was obtained in moderate to good yields.