New synthetic approaches to CNS drugs. A straightforward, efficient synthesis of tetrahydroindol-4-ones and tetrahydroquinolin-5-ones via palladium-catalyzed oxidation of hydroxyenaminones
摘要:
We have developed a facile and efficient synthesis of new conformationally restricted butyrophenones in the indole and quinoline series via palladium-catalyzed oxidation of hydroxyenaminones, and subsequent cyclization followed by spontaneous arornatization. (C) 2002 Elsevier Science Ltd. All rights reserved.
New synthetic approaches to CNS drugs. A straightforward, efficient synthesis of tetrahydroindol-4-ones and tetrahydroquinolin-5-ones via palladium-catalyzed oxidation of hydroxyenaminones
摘要:
We have developed a facile and efficient synthesis of new conformationally restricted butyrophenones in the indole and quinoline series via palladium-catalyzed oxidation of hydroxyenaminones, and subsequent cyclization followed by spontaneous arornatization. (C) 2002 Elsevier Science Ltd. All rights reserved.
One-pot Synthesis, Crystal structure, and Bioactivity of<i>N</i>-Phenoxyacetyl-2,4,5-trisubstituted-1,3-oxazolidines
作者:Ying Fu、Wen-Geng Chen、Yu-Wen Hou、Bin Wang、Li-Xia Zhao、Fei Ye
DOI:10.1002/jhet.2706
日期:2017.3
N‐phenoxyacetyl‐1,3‐oxazolidine derivatives were synthesized by the cyclization and acylation with β‐amino alcohol, ketone, and phenoxyacetyl chloride as the starting materials. All compounds were characterized by IR, 1H NMR, 13C NMR, ESI‐MS, and elemental analysis. The configuration of 4a was determined by X‐ray crystallography. The preliminary biological tests showed that all products could protect
N-苯氧基乙酰基-1,3-恶唑烷衍生物是通过以β-氨基醇,酮和苯氧基乙酰氯为原料的环化和酰化反应合成的。所有化合物均通过IR,1 H NMR,13 C NMR,ESI-MS和元素分析进行了表征。4a的构型由X射线晶体学确定。初步的生物学测试表明,所有产品都可以在一定程度上保护大豆免受2,4-D丁酸酯的伤害。
Tordoir, Chemisches Zentralblatt, 1902, vol. 73, # I, p. 716
作者:Tordoir
DOI:——
日期:——
An efficient reduction protocol for the synthesis of β-hydroxycarbamates from β-nitro alcohols in one pot: a facile synthesis of (−)-β-conhydrine
作者:Partha Pratim Saikia、Gakul Baishya、Abhishek Goswami、Nabin C. Barua
DOI:10.1016/j.tetlet.2008.08.113
日期:2008.11
An efficient and practical one-pot protocol for the reduction of beta-nitro alcohols to their corresponding N-(tert-butoxycarbonyl) amino alcohols using Zn-NH4Cl in aqueous methanol is described. Other reducible groups such as ketones and isolated double bonds remained intact. This methodology allows a short synthesis of (-)-beta-conhydrine to be achieved. (C) 2008 Elsevier Ltd. All rights reserved.
Jaenecke, Chemische Berichte, 1899, vol. 32, p. 1096
作者:Jaenecke
DOI:——
日期:——
Microwave-Assisted Synthesis and Bioactivity of Novel 2,2,4,5-Tetrasubstituted 3-Dichloroacetyl-1,3-oxazolidines
作者:Fei Ye、Lei Yang、Ying Fu、Shuang Gao
DOI:10.3987/com-11-12326
日期:——
An efficient one-pot synthesis of 2,2,4,5-tetrasubstituted 3-dichloroacetyl-1,3-oxazolidines under microwave irradiation was developed. The intermediate oxazolidines were attained by the reaction of amino alcohol with aldehyde or ketone in refluxing benzene with microwave-assisted cycloaddition, and then the acylation followed with dichloroacetyl chloride and NaOH acting as the attaching acid agent. All the compounds were characterized by FR, H-1-NMR, C-13-NMR and elemental analysis. The preliminary biological test shows that these compounds could protect maize against injury caused by acetochlor to a certain extent.