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METHODS: Based on the antitumor activity and structural feature of 8-chloroadenosine and retinoic acid, modifications were made at positions 5′ and 8,substituted cinnamoyl and benzoyl groups were bound at 8 position through amido and ester bonds, sulfonation and nitrosation at 5′-OH and its direct chlorination were conducted.

对腺苷的8位和8-Cl-腺苷的糖环羟基进行了结构改造,以酰胺键和酯键在腺苷的8位连接了具共轭基团的肉桂酰基和苯甲酰基,得到腺苷的维甲类似物;对8-Cl-腺苷的5′-羟基进行了甲磺酰化,硝基化以及氯代反应,得到了它的衍生物。

Quinazolin-4(3H)-ones(1) were conveniently synthesized from anthranilic acids and amidines,which could be chloridized with POCl_3 to obtain 4-chloroquinazolines (2).The reaction of 2 and 1H-pyrazol-3-amine would give two types of products.In the presence of acid or base,the C-N bond would be formed between the 4-position carbon of 2 and the NH_2 of 1H-pyrazol-3-amine.While the C-N bond between the 4-position carbon of 2 and the NH of 1H-pyrazol-3-amine would be formed when Pd catalyst was utilized.

以邻氨基苯甲酸类化合物和脒为原料,可方便地获得喹唑啉-4(3H)-酮类产物(1),1经POCl_3氯化可到4-氯代喹唑啉化合物(2)。2与3-氨基-1H-吡唑化合物反应可得到两种类型的产物,在酸、碱条件下2的4位碳和3-氨基-1H-吡唑化合物的NH_2发生C-N成键反应;在Pd催化条件下,2的4位碳则和3-氨基-1H-吡唑化合物的环内NH发生C-N成键反应。

The bay area has no substituent and has electron-withdrawing groups,such as bromine atom,cyano-group and 4-formyl phenoxy group compounds have strong absorption in 525 nm,when excitated them,they have strong yellow and salmon pink luminescence bettwen 538 and 566 nm.When introduce electron-donating substituents,such as phenoxy group,morpholinyl,piperidinyl and n-butylamino group,the absorption bathochromic shift while the electron-donating ability is improved,bettwen 536 and 692 nm have strong absorption,reach to the near-infrared region. When excitated them,only the phenoxy group compound has strong salmon pink luminescence in 572 nm,the others have no fluorescence.

其中,港湾位无取代的以及含吸电基团(—Br、—CN、对甲酰基苯氧基)化合物在525 nm左右处均有很强的吸收ε>10~4M~(-1cm~(-1),当光激发时,港湾位无取代、溴代和氰基取代物发出538~547 nm的强烈黄色荧光,对甲酰基苯氧基取代物则发出566 nm的强烈橙红色荧光;含供电基团(苯氧基、吗啉基、哌啶基、正丁氨基)化合物随着供电子能力的增强,吸收发生红移,在536~692 nm处均有很强的吸收ε>10~4M~(-1cm~(-1),达到了近红外区,当光激发时,只有苯氧基取代物发出572 nm的强烈橙红色荧光,而含氮供电基取代物均发生了荧光淬灭。

Direct competitions of intramolecular C - H insertions into benzylic C - H and 4-nitroor 4-methoxy substituted benzylic C - H of methyl 2-diazo-3-oxo-6-(4-substituted phenyl)-4-(2-phenylethyl)hexanoate 44a and 44b catalyzed by Rh-mediated carbenoid were alsoinvestigated, and the relative reactivities obtained by compound 44a or 44b were comparableto those obtained by indirect method.

此外,还研究了Rh催化分解下,对位硝基取代或甲氧基取代的4-(2-苯基乙基)-6-(4-取代苯基)-2-重氮基-3-氧代己酸甲酯44a、44b苯甲位C-H插入反应的相对速率,与化合物47a和47f得到的结果比较,数据平行。

The spectral data suggest that intramolecular carbonyl oxygen to tin coordination in 1 is existent and is not allowedin order to accommodate two and three bidentate dithiocarbamate ligands in 3 and 4 respectively.

波谱数据表明化合物1和2存在着分子内羰基氧原子对锡原子的配位,而在化合物3和4中这一配位则被两个或三个双齿二硫代氨基甲酸配体所替代。

Urine VMA level is a useful marker to detect extra-adrenal pheochromocytoma and CT scan is the most reliable in localizing the lesions.131-MIBG scintigraphy is of great value for the localiza-tion and quantitative for extrarenal pheochromocytoma with high sensitivity and accuracy.It may be also used as a therapeutic method.

VMA及血、尿儿茶酚胺是定性诊断异位嗜铬细胞瘤的主要依据,CT诊断定位准确、131碘-间位碘代苄胍(131I-MIBG)定位准确、敏感性高,且可作为治疗措施。

In the presence of catalytic rhodium acetate, ethyl 2-diazo-3-oxo-per fluoroalkanoates, reacted readily with nitriles to give a series of 5-fluoroalkyl substituted 1, 3oxazoles with high regio-selectivity through a metal carbenoid intermediate. The reactions of carbenoids with noncyclic vinyl ethers or cyclic vinyl ethers afforded dihydrofuroates in good to excellent yields. Interestingly, only vinyl C-H insertion compound was obtained concerning of the reaction of carbenoids with 2, 5dimethylfuran due to the steric hindrance of methyl group

醋酸铑分解2-重氮-3-氧代-全氟羧酸乙酯形成的金属卡宾作为1,3-偶极体,可以与一系列芳基或烷基取代的腈反应,高度区域选择性地生成一系列4-乙氧羰基-5-氟烷基取代的噁唑化合物;也可以与富电子的链状和环状的烯基醚反应,以优良的产率得到一系列氟烷基取代的二氢呋喃类化合物;而与2,5-二甲基呋喃的反应,由于甲基的位阻作用,只得到金属卡宾对呋喃3-位烯基碳氢键插入产物。

Deming took over as chief executive in late1994,succeeding two nonfamily chief executives and becoming the first third-generation family member to run the company.

戴明继两位非家族老总之后,于1994年年底接任首席执行官,从而成为第一位管理该公司的第三代家族成员。

A 43-year-old jobless woman, who never dreamed of becoming a lawmaker, was elected to Japan's House of Representatives, local media reported. A Democratic Party of Japan upper house lawmaker presciently asked Kayoko Isogai, who has held mostly non-regular jobs since finishing university, to run as a candidate at the bottom of a local ballot and she got the nod from voters.

日本媒体日前披露,不久前当选国会议员的矶谷香代子是个普通的钟点工,大学毕业以后一直没有固定工作,更毫无当选的思想准备。43岁的她此前被一位民主党参议员推荐参加竞选,排在名古屋东海地区候选人中的最末位。

Anteac had addressed herself sharply to the heavyset officer commanding the Fish Speaker escort, a glowering woman with low brows and the muscles of a manual laborer.

安缇克曾严厉地向一位指挥鱼之代言者护卫的体格魁梧的官员抗议,她是位眉毛低垂、有着体力劳动者的肌肉、瞪着双眼的女人。

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