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近五十多年来,科学家们普遍认为是生物体内的自由基的不可逆的氧化导致了生物体生理机能的衰老[1 3]。帕金森症[4]在人群中多发生于老年人。它主要的病理异常是黑质变性,会导致中枢神经纹状体致密区中的多巴胺耗竭。由Hueb ner[5]等人对N 炔丙基 N 取代茚满类化合物所进行的药理作用与其结构关系的研究,发现具有N 炔丙基的胺类或氨基酸类化合物,对于生物体中单胺氧化酶有较高的抑制作用;而抑制单胺氧化酶,可有效地提高人体大脑中多巴胺的水平[4,6,7]。本文以简便的方法合成了十种尚未见文献报道的N 炔丙基胺的化合物Ⅰ Ⅹ(表… 相似文献
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利用N-甲基吲哚对类固醇药物的前驱体16-脱氢孕烯醇酮乙酸酯(16-DPA)的D环C16位进行修饰,采用ZrCl4-乙酸乙酯廉价催化体系,合成了16个3β-乙酰氧基-16α-3’-吲哚孕烯醇酮化合物和6个3β-羟基-16α-3’-吲哚孕烯醇酮衍生物.该方法具有收率高、立体选择性好和底物适应性强等优点.通过噻唑蓝(MTT)比色法测试了22个化合物对三阴性乳腺癌细胞(MDA-MB-231)的抗肿瘤活性.初步测试结果表明, 3β-乙酰氧基-16α-3’-吲哚孕烯醇酮化合物6h和6i对MDA-MB-231癌细胞有较好的抑制活性,其半数抑制浓度(IC50)分别为18.07和23.22μmol/L;而化合物7a~7f均对MDA-MB-231癌细胞有较好的抑制活性,其中化合物7e的抗肿瘤活性最好,其IC50为12.50μmol/L.目标化合物为药物筛选提供了一定的参考. 相似文献
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Yuan Zou Fu-Lin Zhu Zheng-Chao Duan Ya-Hui Wang De-Yang Zhang Zhong Cao Zhuo Zheng Xiang-Ping Hu 《Tetrahedron letters》2014
A copper-catalyzed asymmetric propargylic amination with a chiral ketimine P,N,N-ligand that proceeds via decarboxylation of propargyl carbamates has been developed. The reaction can be performed under the mild condition for a broad range of substrates, providing the corresponding propargylic amines in high yields and with up to 97% ee. This reaction represents a new and facile access to optically active propargylic amines. 相似文献
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《Tetrahedron letters》2019,60(50):151305
A copper-catalyzed asymmetric etherification of propargylic acetates with oximes as O-nucleophiles has been developed. The employment of a chiral tridentate P,N,N-ligand proved to be crucial for the success of the reaction. The reaction features a broad scope on either reaction partners and led to a variety of etherification products in good yields and enantioselectivities. 相似文献
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A highly efficient one-pot procedure for the synthesis of indolines and their homologues based on a domino Cu-catalyzed amidation/nucleophilic substitution reaction has been developed. Substituted 2-iodophenethyl mesylates and related compounds afforded the corresponding products in excellent yields. No erosion of optical purity was observed when transforming enantiomerically pure mesylates under the reaction conditions. 相似文献
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Takayoshi HaraKohsuke Mori Tomoo MizugakiKohki Ebitani Kiyotomi Kaneda 《Tetrahedron letters》2003,44(33):6207-6210
A hydroxyapatite-bound palladium catalyst was found to be effective for the dehydrogenation of various types of indolines to give the corresponding indoles. Moreover, the catalyst was readily recovered from the reaction mixture, and could be reused without any loss of its catalytic activity. 相似文献
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This Letter describes an efficient method—one that takes advantage of hydrogen bond-guided self-assembly and ruthenium-catalysed propargylic substitution—for the preparation of rotaxanes. The substitution reactions of a pseudorotaxane with a diverse range of heteroatom- and carbon-atom-centred nucleophiles were catalysed by the [(Cp∗)RuCl(SMe)]2 complex to furnish rotaxanes in good yields. 相似文献
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The copper-mediated trifluoromethylselenolation of propargylic chlorides and allylic bromides is described. This approach provides a wide range of propargylic and allylic trifluoromethyl selenoethers in moderate to good yields. These results open the way to synthesis strategies for various trifluoromethylselenolated compounds. 相似文献
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An enantioselective carboxylative cyclization of propargylic alcohols and CO2 was realized under mild conditions,based on a kinetic resolution strategy,which enabled the synthesis of chiral cyclic carbonates and propargylic alcohols with promising yield and enantioselectivity simultaneously. 相似文献
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Mark. C. Wilkinson 《Tetrahedron letters》2005,46(28):4773-4775
The development of an asymmetric route to an aminomethyl morpholine intermediate via palladium-catalysed allylic substitution is described. 相似文献