共查询到19条相似文献,搜索用时 78 毫秒
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以5-苯基-1,3-环己二酮,醛,乙酰乙酸乙酯(或乙酰丙酮)和乙酸铵为原料,在无水乙醇中经一锅反应合成了14个新型的7-苯基-1,4,5,6,7,8-六氢喹啉酮衍生物,总收率85%~95%,其结构经1H NMR, 13C NMR, IR和HR-MS表征。采用X-ray单晶衍射研究了2-甲基-4,7-二苯基-5-氧代-1,4,5,6,7,8-六氢喹啉顺反异构体(5a和5a′)的晶体结构。结果表明:5a空间群为C2/c, a=9.458 35(19) ,b=19.789 0(4) ,c=11.040 9(2) , α=90°, β=105.614(2)°, γ=90°,V=1 990.28(7) 3, Z=4, μ=0.673 mm-1, F(000)=824; 5a′空间群为C2/c, a=9.770 2(5) , b=19.981 0(10) , c=10.430 1(4) , α=90°, β=98.361(5)°, γ=90°, V=2 014.51(17) 3, Z=4, μ=0.665 mm-1, F(000)=824。 相似文献
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1,2,3,4—四氢—2—苄基异喹啉酮—4衍生物的合成 总被引:1,自引:0,他引:1
1,2,3,4-四氢-2-取代异喹啉酮-4衍生物中有不少具有重要的药理活性。许多学者进行了这一方面的合成工作。作者根据Hanna等 相似文献
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运用药物分子片段原理及拼合原理,设计了四氢异喹啉阿司匹林衍生物。以取代苯甲酸、3,4-二甲氧基苯乙胺或胡椒乙胺为原料,通过酰胺化反应、Bischler-Napieralski反应和亲核取代反应等步骤,合成了12个全新的四氢异喹啉阿司匹林衍生物。以5-氟尿嘧啶为阳性对照药,采用SRB法对所合成化合物进行抗肿瘤活性初步筛选。结果显示:所合成化合物对A549、MCF-7、HepG2肿瘤细胞具有一定的抑制作用,且除化合物8k外,其余化合物对A549肿瘤细胞的抑制活性均比阳性对照5-氟尿嘧啶强。 相似文献
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2-Arylidene-3-oxo-2,3,4,5,6,7-hexahydrobenzo[b]furans 2 react with hydrazine hydrate to afford 5,6,7,8-tetrahydro-4-cinnolones. By methylation, these compounds gave the corresponding N-1 and N-2 methyl derivatives. The mesoionic compounds are obtained, accompanied by 3-arylacetyl-4,5,6,7-tetrahydroindazoles upon reaction of 2 with methylhydrazine. 相似文献
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2-Amino-4-[3-methyl-3-(5,6,7,8-tetrahydro-2-naphthyl)cyclobutyl]thiazole was synthesized by reaction of 1-methyl-1-(5,6,7,8-tetrahydro-2-naphthyl)-3-chloroacetylcyclobutane with thiourea in ethanol, and its subsequent transformations afforded new derivatives which were tested in vitro for antibacterial activity against some bacteria using the disk diffusion technique.__________From Zhurnal Organicheskoi Khimii, Vol. 40, No. 12, 2004, pp. 1861–1865.Original English Text Copyright © 2004 by Koparr, Cansz, Ahmedzade.The original article was submitted in English. 相似文献
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以3-溴-1,3,4,5-四氢-2H-1-苯并氮杂--2-酮为起始原料,与苄胺反应制得3-苄氨基-1,3,4,5-四氢-2H-1-苯并氮杂(堇)-2-酮(2);2经5% Pd/C催化加氢合成了3-氨基-1,3,4,5-四氢-2H-1-苯并氮杂——革)-2-酮(3),总收率90%.最佳氢化反应条件为:以无水乙醇为溶剂,5% Pd/C用量为总用量的10%,于100℃/2.5 MPa条件下反应10 h,3的收率95.5%,纯度99.7%.5% Pd/C可套用7次,收率稳定在95%左右. 相似文献
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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.
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Translated from Chinese Journal of Organic Chemistry, 2008, 28(2) (in Chinese) 相似文献