毒扁豆碱的合成前体化合物的制备研究

本文以5-甲氧基色胺为起始原料,经胺基保护、分子内环化、甲基化及酰胺还原四步反应制备毒扁豆碱(Physostigmine)合成前体。该合成路线具有合成试剂价廉易得、合成操作简便、对环境友好等优点,工业化生产可行性高。作为毒扁豆碱(Physostigmine)的合成前体,本中间体也同样可作为苯胺基甲酸酯毒扁豆酚碱(Phenserine)以及各类毒扁豆碱衍生物的合成前体,因此具有很好的应用价值和发展潜力。

通过分子内酰胺α-芳基化环化合成3-季碳氧化吲哚反应研究进展

综述了通过分子内酰胺α-芳基化环化合成3-季碳氧化吲哚的方法,根据其机理主要讲金属催化的氧化还原历程,再根据原料和催化剂等不同分别进行介绍。

Coordination behavior of N-benzoylamino acids: Synthesis and structure of mixed-ligand complexes of palladium(Ⅱ) with N-benzoylamino acid dianion and diamine

Four new mixed-ligand complexes of pailadiumt(Ⅱ) with L1(N-benzoyl-α-amino acid dianion) and L2[ethyldiamine (en),2,2’-bipyridine (Bpy) and 1,10-phenanthroline (Phen)] were synthesized.Ail the complexes have been characterized by elemental analyses,molar conductance,infrared and 1H NMR spectra and therme-gravimetric analyses.Crystal structures of [Pd(Bpy)(Bzval-N,O)] and [Pd(en) (Bzphe-N,O)] H2O have been do termmed by X-ray diffraction analysis.The results indicate that in all the complexes hgand L1 coordinates to palladium (Ⅱ) through deprotonated amide nitrogen and carboxylic oxygen,and there are some intramolecular nonrovalent in teractions in the complexes.

Synthetic studies towards daphniyunnine B: Construction of AC bicyclic skeleton with two vicinal all carbon quaternary stereocenters

The AC bicyclic skeleton of daphniyunnine B with the required 3 stereocenters(C4,C5 and C8)was accomplished in a concise route which featured two Claisen-type rearrangement reactions to construct the required vicinal all carbon quaternary stereocenters(C5 and C8)and an intramolecular iodocyclization reaction to assemble the cis-confused bicyclic lactam.

A novel and concise synthetic access to chiral 2-substituted-4-piperidone

A novel and concise synthetic access to enantiopure chiral 2-aryl/alkyl substituted 4-piperidone has been demonstrated.This new route features two key steps:the highly diastereoselective conjugate addition of homochiral lithium amides to trans-β-substituted-α,β-unsaturated methyl esters guaranteed the enantiopurity at 2 position(de>19:1)and the intramolecular attacking of carbanions to methyl esters led to the formation of the piperidone ring.A wide range of substrates,including chiral2-aryl and 2-alkyl-4-piperidones,were successfully synthesized with modest to high yield.Moreover,some non-chiral3-substituted-4-piperidones were also synthesized with enhanced ring-formation yield,implicating the versatility of this method in construction of various piperidine rings.

Chemoselective synthesis and cytotoxic activity of a series of novel benzo[1,4]oxazin-3-one derivatives

That tetraacetonitrile copper perchlorate catalyzes intramolecular amidation of arenes was found to be a new strategy for construction of nitrogen-containing heterocycles and resulted in the formation of a series of novel benzo[1,4]oxazin-3-one derivatives from N-（1,3-diphenyl-1H-1,2,4-triazol-5-yl）-2-phenoxyacetamides.This approach of heterocyclic construction proceeds in a chemoselective manner in which only benzo[1,4]oxazin-3-one derivatives were obtained by C—N bonds formation with cheap and simple copper salt catalyst under mild conditions in moderate to good yields.The biological assay of some of benzo[1,4]oxazin-3-one derivatives showed that they had moderate antiproliferative activity toward MDA-MB231 and HeLa cancer cell lines.