姜黄素类似物的合成及其清除自由基的研究

姜黄素(见图1)为中药姜黄的主要成分,是一种黄色色素。研究报道姜黄素具有抗氧化、抗炎、抗病毒、抗癌等生物活性[1-4]。本文通过芳香醛和环己酮催化缩合反应合成了一系列姜黄素类似物(见图2),研究了它们抗自由基的活性。图1姜黄素的化学结构F ig.1 Chem ical structure of cur     

A Convenient and Rapid Preparation of Novel Quinoxaline Derivatives

A simple and rapid method for the preparation of a series of novel quinoxaline derivatives in the presence of Ag⁺ is reported.     

Efficient synthesis of optically active α-substituted glutamate analogs possessing α-hydroxymethyl and α-alkoxymethyl groups

Highly enantioselective synthesis of (2R)-α-(hydroxymethyl)glutamate (1), a selective agonist of mGluR2 and 3, was achieved in short steps using an asymmetric version of the Strecker synthesis. This was converted into its α-methoxymethyl- and α-benzyloxymethyl derivatives 2 and 3, possible ligands as tools to investigate glutamate receptors, via protection of the sterically hindered amino group by means of phase transfer catalyst.     

A new approach to the synthesis of racemic analogs of 1,5-dimethyl-branched insect pheromones from 4-methyltetrahydropyran

A new procedure was developed for the synthesis of racemic analogs of 1,5-dimethyl-branched insect pheromones based on monoalkylation of ethyl acetoacetate with 1-acetoxy-5-bromo-3-methylpentane produced upon decyclization of 4-methyltetrahydropyran.     

New conversion of Friendl(a)nder reaction of 3-amino-lH-benzo[f]chromene-2-carbonitriles with cyclohexanone

Two different skeletons of heterocyclic compounds, quinoline and quinazolinone analogs could be obtained by a novel one-potsynthesis from substituted 3-amino-lH-benzo[f]chromene-2-carbonitrile derivatives and cyclohexanone in DMF in the catalyst ofanhydrous zinc chloride under reflux. A plausible mechanism was proposed.     

Molecular structures of some D-homo-6-oxa-8α analogs of steroidal estrogens

By X-ray crystallographic analysis and NMR spectroscopy it was demonstrated that the conformations of several D-homo-6-oxa-8α analogs of steroidal estrogens are similar in the crystal and in solution. The distances between the hydrogen atoms in these molecules, calculated by the ab initio and MM⁺ methods, correspond to the experimental data. __________ Translated from Khimiya Geterotsiklicheskikh Soedinenii, No. 2, pp. 202–207, February, 2008.     

Designing and Synthesis of Novel Amidated Fentanyl Analogs

Some new amidated fentanyl (=N‐[1‐(2‐phenylethyl)piperidin‐4‐yl]‐N‐phenylpropanamide) analogs with a 4‐(N‐phenylamido)piperidine scaffold and additional amide bonds have been designed and synthesized through Ugi four‐component reaction (Ugi‐4CR). Good‐to‐high yields, diversity‐oriented synthesis, and possible applications in drug discovery are advantages of this approach.     

Zinc perchlorate catalyzed one-pot amination-annulation of α-cyanomethyl-β-ketoesters in water. Regioselective synthesis of 2-aminopyrrole-4-carboxylates

In this paper, we report the efficient and regioselective synthesis of 2-aminopyrrole-4-carboxylates as derivatives of conformationally restricted analogues of γ-amino butyrates (GABA) via a zinc perchlorate catalyzed amination-annulation of α-cyanomethyl-β-ketoesters under mild reaction conditions in water.     

Synthesis of new fluorescently labeled glycosylphosphatidylinositol (GPI) anchors

The borondipyrromethene (BODIPY) labeled new glycosylphosphatidylinositol (GPI) molecules were synthesized as cellular probes to study the chemical basis of microdomain organization of GPI-anchored proteins and cholesterol in plasma membrane. The synthesis enabled by a new stereo-selective glycosylation of myo-d-inositol acceptor led to the preparation of optically pure glucosaminyl-(1-6)-α-phosphatidyl-myo-d-inositol and its unnatural stereoisomer.     

1,n-Diamines. Part 3: Microwave-assisted synthesis of N-acyl-N′-arylhexahydropyrimidines and hexahydro-1,3-diazepines

In this Letter we present a method for the synthesis of N-acyl-N′-arylhexahydropyrimidines 1, by ring closure of N-acyl-N′-aryl-1,3-propanediamines 3 with formaldehyde. Cyclodehydrations were performed in aqueous medium under microwave irradiation, and led to high yields of the desired compounds in remarkably short reaction times. The method also allowed for the synthesis of hitherto unreported N-acyl-N′-arylhexahydro-1,3-diazepines 2. The acyclic tetramethylenic precursors 4 were synthesized by selective functionalization of N-arylputrescines.