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M. Madesclaire P. Coudert V. Gaumet V. P. Zaitsev Yu. V. Zaitseva 《Chemistry of Heterocyclic Compounds》2006,42(5):665-670
We have synthesized a series of (1R,2R,4S,5S,8S)-2,8-diaryl-4-(4-nitrophenyl)-1-aza-3,7-dioxabicyclo[3.3.0]octanes as a result
of reaction of (1S,2S)-2-amino-1-(4-nitrophenyl)-1,3-propanediol with aromatic aldehydes. The structure of the compounds obtained
was established on the basis of 1H NMR data.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 5, pp. 757–763, May, 2006. 相似文献
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Anica Markovac Ambalal R. Patel Maurice P. MontagneLa Arthur B. Ash 《Journal of heterocyclic chemistry》1977,14(1):147-148
The preparation of 4-(3-nitrophenyl)-2-pieoline (3) was accomplished in one step by the Zecher-Krohnke ring-closure reaction. Compound 3 is the starling material for 2-lormyl-4-(3-arninophenyl)pyridine thiosemicarbazone (4-APPT), a promising antineoplastie agent. 相似文献
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以L-抗坏血酸(1)为原料,经3步反应制得(S)-缩异丙氧叉甘油醛(4).该手性醛与苄胺缩合制得相应的手性亚胺(5).甘氨酸经保护后制成酰氯,在有机碱作用下首先生成不稳定的烯酮(8),继与手性亚胺5迅速进行[2+2]环加成反应,合成标题化合物N-苄基-3(S)-邻苯二甲酰亚胺基-4(S)-[4(S)-2,2-二甲基-1,3-二氧环戊-4-基]-2-氧吖丁啶.由于环加成的面向立体选择性容易控制,由此所得产物的光学纯度和化学收率均较高 相似文献
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Xing Zhou LI Xian Ping DAI Jun Hai XIAO Song LI* Beijing Institute of Pharmacology & Toxicology Beijing School of pharmaceutical Engineering Shenyang Pharmaceutical University Shengyang 《中国化学快报》2005,16(9):1137-1139
For discovering novel small molecule inhibitors of transforming growth factor-β1(TGF-β1)type-I receptor(ALK5),we designed1,3,5-triaryl-4-hydroxyl-4,5-dihydro-1H-pyrazole(1)as target compound,mimic the structure of SB-431542which is a2-pyridyl substituted triarylimiazole inhibitor of ALK51.Racemic compound1showed moderate ALK5inhibitory activity in luciferase reporter assays[inhibition(%control):0.1umol/L8.79%;1umol/L19.05%].To investigate the influence of the absolute configuration of… 相似文献
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(2S,3S)-[3-(2)H1]-4-Methyleneglutamic acid 1a and (2S,3R)-[2,3-(2)H2]-4-methyleneglutamic acid 1b have been synthesised for use in biosynthetic and metabolic studies. 相似文献
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《Tetrahedron: Asymmetry》2005,16(6):1135-1140
Stereoselective synthesis of pharmaceutically interesting chiral tetrahydrofurans starting from mannose diacetonide is reported. A 1,4-diol system derived from mannose diacetonide, through a Mitsunobu reaction was stereospecifically cyclized to give chiral tetrahydrofurans. Both the C-1 and C-4 centers of d-mannose are successfully exploited to install the requisite side chains. 相似文献
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M. Madesclaire P. Coudert V. Goumet V. P. Zaitsev J. V. Zaitseva 《Chemistry of Heterocyclic Compounds》2006,42(6):813-817
The configuration of the asymmetric atoms in the molecule of (1R,2R,4S,5S,8S)-2,8-bis(4-chlorophenyl)-4-(4-nitrophenyl)-1-aza-3,7-dioxabicyclo[3,3,0]octane
has been determined using X-ray analysis.
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Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 6, pp. 930-934, June, 2006. 相似文献
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(R)-2-{[4-(3-甲氧基丙氧基)-3-甲基吡啶-2-基]甲基亚硫酰基}- 1H-苯并咪唑的合成 总被引:1,自引:0,他引:1
以2,3-二甲基吡啶为起始原料, 经过11步反应, 不对称合成了质子泵抑制剂的关键中间体: (R)-2-{[4-(3-甲氧基丙氧基)-3-甲基吡啶-2-基]甲基亚硫酰基}-1H-苯并咪唑. 研究了用手性高效液相色谱拆分对映体、测定产品光学纯度的方法, 结果表明目标产品的ee值达到99%. 通过IR, UV, MS以及1H NMR分析对重要中间体和目标产品进行了结构鉴定. 相似文献
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The photoprocesses of nifedipine, a 4-(2-nitrophenyl)-1,4-dihydropyridine, and nimodipine and nitrendipine, two 3-nitrophenyl Hantzsch-type analogues, were studied by steady-state and time-resolved methods. The intramolecular photoreduction of nifedipine into its nitrosophenyl product takes place within a few ns. The quantum yield of conversion is Φred = 0.3 and does not depend significantly on the oxygen concentration and solvent properties. Formation of the fully reduced 4-(2-aminophenyl)-1,4-dihydropyridine as minor product is indicated by fluorescence spectroscopy. The photoreduction of nimodipine and nitrendipine is inefficient, Φred = 0.002 in acetonitrile, but markedly enhanced in the presence of donors such as triethylamine (TEA) and 2-propanol, e.g. for TEA Φred is up to 0.03. The triplet states of nimodipine and nitrendipine were characterized. They react intermolecularly with TEA and 2-propanol, forming radicals as intermediates and eventually several reduction products. 相似文献
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