4-(4'-丙基环己基)环己醇的合成

钌/碳催化剂应用于4-(4'-丙基环己基)苯酚(3PCO)的加氢反应,合成了4-(4'-丙基环己基)环己醇.以环己烷为溶剂,在98℃/2MPa,3PCO的转化率为100.0%,催化剂可以重复使用两次.     

4-对丙烯基苯氨基喹唑啉衍生物的合成及抗肿瘤活性研究

以3-羟基苯甲腈为原料,经过6步反应(醚化、硝化、还原、甲脒的形成、环化和取代)合成了两个新型4-对丙烯基苯氨基喹唑啉衍生物4-[4-(E)-丙烯基苯氨基]-6-[2-吗啉基乙氧基]喹唑啉和4-[4-(E)-丙烯基苯氨基]-6-[3-吗啉基丙氧基]喹唑啉。化合物的结构经IR、HRMS、1H NMR和13C NMR确认。以人结肠癌细胞(SW480)、人肺癌细胞(A549)、人皮肤鳞状细胞癌细胞(A431)为模型,采用MTT法对所得化合物进行了体外抗肿瘤活性评价。结果表明,两个化合物均具有一定的抗肿瘤活性。特别是化合物4-[4-(E)-丙烯基苯氨基]-6-[3-吗啉基丙氧基]喹唑啉对所试肿瘤细胞均表现出良好的生长抑制活性(IC50:10.0~18.2μmol/L),与临床使用药物吉非替尼的活性(IC50:4.1~18.5μmol/L)相当。     

4-(2''''-呋喃甲基)氨基嘧啶衍生物的合成及生理活性

细胞分裂素可以促进植物的细胞分裂、延缓叶绿素的降解及其它老化过程。常见的细胞分裂素有玉米素(Zeatin)、激动素(Kinetin)、6-苄氨基嘌呤(6-BA)等，这些物质中均含有嘌呤环。鉴于嘌呤环和嘧啶环均为核酸的碱基成分、激动素中含有2’-呋喃甲基，本文利用活性结构拼接原理，将该类细胞分裂素的嘌呤环换成嘧啶环，合成了2种4-(2‘-呋喃甲基)氨基嘧啶衍生物，以试验其生理活性。目标化合物的合成路线如下。     

Synthesis and pharmacological activity of diterpenylnaphthoquinone derivatives

New diterpenylquinones, combining a diterpene diacid and a naphthoquinone, were prepared from junicedric acid and lapachol. The new derivatives were assessed as gastroprotective agents by the HCl-EtOH-induced gastric lesions model in mice as well as for basal cytotoxicity on the following human cell lines: Normal lung fibroblasts (MRC-5), gastric epithelial adenocarcinoma (AGS), and hepatocellular carcinoma (Hep G2). Several of the new compounds were significantly active as antiulcer agents and showed selective cytotoxicity against AGS cells.     

3,3,6,6-四甲基-9-对氯苯基-1,8-二氧代-2,3,4,5,6,7-六氢氧杂蒽的合成和晶体结构

标题化合物C2 3H2 5O3Cl是由对氯苯甲醛与 5,5 二甲基 1 ,3环己二酮在乙二醇中反应而得。结构通过单晶X 射线衍射法测定 ,其晶体属于单斜晶系 ,空间群P2 1 /n ,a =6.0 4 8(1 ) ,b =1 9.543(3) ,c =1 7.42 0 (3) ,β =97.2 9(1 )° ,V =2 0 4 2 .2 (6) 3,Mr=384.90 ,Dc=1 2 52 g/cm3,Z =4,μ(MoKα) =2 .0 6cm- 1 ,F(0 0 0 ) =81 6。晶体结构用直接法解出 ,经用全矩阵最小二乘法对原子参数进行修正 ,最终的偏离因子为R =0 .0 39,Rw=0 .0 4 7。X 射线衍射分析表明 :平面 1 (C(8) -C(9) -C(1 9) )与平面 2 (C(1 0 ) -C(1 1 ) -C(1 2 ) )之间的两面角为1 6.2 4° ;平面 1与平面 3(C(7) -C(8) -C(9) )之间的两面角为 1 77.37° ;平面 1与平面 4(C(1 )-C(5) -C(6) )之间的两面角为 98.2 1°;平面 2与平面 3之间的两面角为 1 61 .1 2° ;平面 2与平面 4之间的两面角为 81 .98°;平面 3与平面 4之间的两面角为 79.1 5°     

4'-(丹磺酰氨基)苯并冠醚和4'-[α-(丹磺酰氨基)乙基]苯并-15-冠-5的合成

从B12C4, B15C5和B18C6经过硝化、催化氢化和丹磺酰化合成了三种4'-(丹磺酰氨基)苯并冠醚, 从B15C5径乙酰化, Leuckart反应和丹磺酰化合成了另一个4'-[α-(丹磺酰氨)乙基]苯并-15-冠-5这些丹磺酰氨衍生物均为新荧光冠醚.     

Synthesis and anticonvulsant activity of some quinazolin-4-(3H)-one derivatives

A number of 3-substituted-2-(substituted-phenoxymethyl) quinazolin-4(3H)-one derivatives 4a,b, 5a-c, 6, 7a-f, 8a-e and 9a,b have been synthesized. Their structures have been elucidated on the basis of elemental analyses and spectroscopic studies (IR, 1H-NMR, MS). A preliminary evaluation of the anticonvulsant activity of the prepared compounds has indicated that compounds 4b, 7b-f, 8a and 9b exhibit significant anticonvulsant activity, while compounds 6, 8b and 8d show mild to moderate activity.     

Synthesis and pharmacological activity evaluation of curcumin derivatives

Curcumin 3,4-dihydropyrimidinones/thiones/imines have been synthesized using one-pot cyclocondensation of curcumin with substituted aromatic aldehydes and urea/thiourea/guanidine in the presence of chitosamine hydrochloride as a biodegradable and nontoxic catalyst under solvent-free microwave irradiation. The synthesized product was purified by crystallization from ethanol and the process does not involve any hazardous solvent. All the synthesized curcumin derivatives 4a-o were screened for antioxidant and anti-inflammatory activity. Biological activity data of the synthesized showed that most of the synthesized compounds exhibited greater antioxidant and anti-inflammatory activity than curcumin.     

Mass spectra and three-dimensional structure of 4-hydroxypiperidine derivatives

The mass spectra of stereoisomeric derivatives of 4-hydroxypiperidines obtained at various ionizing-electron energies with the application of isotopic substitution and high-resolution mass spectrometry are examined. The character of the fragmentation of the piperidine ring as a function of the position and spatial orientation of the substituent is discussed.     

Synthesis of (-)-arctigenin derivatives and their anticancer activity

The natural dibenzylbutyrolactone type lignanolide (-)-arctigenin, which was prepared from fructus arctii, showed obvious anticancer activity. The synthesis of four new (-)-arctigenin derivatives and their anticancer bioactivities were examined. The structures of the four new synthetic derivatives were elucidated.     

Synthesis and biological activity of novel 2-(3-trifluoromethylphenoxy)-4-trifluoromethylthiazole-5-carboxamide derivatives

Novel 2-(3-trifluoromethylphenoxy)-4-trifluoromethylthiazole-5-carboxamides were designed and synthesized utilizing ethyl 3-amino-4,4,4-trifluoro-2-butenoate as a starting material via six steps. Subsequently, their biological activities were evaluated in the greenhouse. Results indicated that several compounds have some insecticidal or fungicidal activity at 600 g ai/ha and 300 g ai/ha, respectively.     

3'-(叔丁基二甲基硅氧)-苯并噁嗪利福霉素的合成

<正>众所周知,结核病是一种常见的、多发的、古老而现代的慢性传染病,系世界三大传染病之一,严重危害人类的健康。利福霉素类抗生素,诸如利福平、利福喷丁及利福布汀等抗结核药物,在防痨抗痨中发挥着极为重要作用,但在结核病的治疗过程中却逐渐出现耐药性及交叉耐药性,特别是HIV与鸟分枝杆菌     

Synthesis and pharmacological activity of 2-(biphenyl-4-yl)imidazo[1,2-a]benzimidazoles

Russian Chemical Bulletin - An efficient method for the synthesis of novel 9H-imidazo[1,2-a]benzimidazole derivatives containing a biphenyl substituent at position 2 was developed. These compounds,...     

Synthesis and antiemetic activity of 1,2,3,9-tetrahydro-9-methyl-3-(4-substituted-piperazin-1-ylmethyl)-4H-carbazol-4-one derivatives

5-HT₃ receptor antagonists, such as Ondansetron, are used for anti-emesis after chemotherapy, radiotherapy and operations. Some Ondansetron analogs possessing piperazine ring as side chains were synthesized in our lab. Thus, one of the two carbonyl groups of starting material 1,3-cyclohexandione (1) was condensed with phenylhydrazine hydrochloride to form monophenylhydrazone (2). 1,2,3,9-Tetrahydro-4H-carbazol-4-one (3) was prepared from 2 via cyclization and rearranged in the presence of ZnCl₂. Through a methylation reaction, compound 3 was converted to 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one (4). 3-Dimethylaminomethyl substituted compound (5) was synthesized from 4 by a Mannich reaction in glacial acetic acid. Nine novel 1,2,3,9-tetrahydro-9-methyl-3-(4-substituted-piperazin-1-ylmethyl)-4H-carbazol-4-one derivatives (6a–6i) were synthesized through nucleophilic substitution reaction of 5 with piperazines. The structures of all the target compounds were determined by elemental analysis, IR, MS, ¹H NMR and ¹³C NMR spectra. The results of preliminary pharmacological test show that part of the novel compounds have antiemetic activity comparable to that of the control Ondansetron. __________ Translated from Chinese Journal of Organic Chemistry, 2008, 28(2) (in Chinese)     

3-甲基-4-乙氧基(二乙氨基)羰基-1H-吡唑衍生物的合成 及其生物活性

以乙酰乙酸乙酯的二硫缩醛为原料,分别合成了1-磺酰基-3-甲基-4-乙氧基(二乙氨基)羰基-5-甲硫(甲磺酰)基-1H-吡唑和1-甲酰基-3-甲基-4-乙氧基羰基-5-甲硫基1H-吡唑。元素分析、1^HNMR证实了它们的结构,部分化合物经过MS和IR的证实。初步的生测结果表明部分化合物对芦笋茎枯病和番茄早疫病具有较好的效果。     

Synthesis of 1,2,5-trimethyl-4-ethoxycarbonylmethyl-4-hydroxypiperidine and its homologs

1,2,5-Trimethyl-4-ethoxycarbonylmethyl-4-hydroxypiperidine was obtained by the Reformatsky reaction between 1,2,5-trimethyl-4-piperidone and ethyl bromoacetate. Homologs were obtained from the same piperidone and ethyl -bromo--alkylacetates. Some further reactions of these hydroxypiperidines were studied.     

Synthesis of 3-(α-naphthylmethyl)-4-hydroxycoumarin and its derivatives

3-(α-Naphthylmethyl)-4-hydroxycoumarin and a series of derivatives are prepared by condensing phenols with diethyl α -naphthylmethylmalonate under the influence of heat.