奈必洛尔中间体的不对称合成

(S,R,R,R)-奈必洛尔是一种新型、强效的β1-肾上腺素能受体阻滞剂降压药物.采用氧化/Wittig烯化一锅煮反应和Sharpless不对称环氧化/环化一锅煮反应,经八步反应,不对称合成出(S,R,R,R)-奈必洛尔的两个关键中间体1-[6-氟-(2S)-3,4-二氢-2H-2-苯并吡喃]-(1R)-1,2-乙二醇和1-[6-氟-(2R)-3,4-二氢-2H-2-苯并吡喃]-(1S)-1,2-乙二醇.该合成路线工艺简单,单步反应产率高,八步反应总收率达19%.     

α－紫罗兰酮合成新工艺研究

对α－紫罗兰酮合成的环化剂和溶剂进行了筛选．对合成的工艺条件（环化剂与溶剂的用量、反应时间、反应温度）进行了优化，在优化工艺条件下，紫罗兰酮的得率可达８０％以上，α－紫罗兰酮的相对含量为８０％左右．     

Prins成环反应研究最新进展

Prins反应作为有机合成中一个经典的碳碳键构成方法，近来重新引起有机合成化学工作者的重视，尤其是分子内Prins成环反应具有非常大的合成价值，作者整理和总结了近几年来对该反应的文献报道，包括反应的催化体系、反应选择性、相关合成方法学、反应机理以及在复杂天然产物分子合成中的应用等多方面所取得的重要进展。     

Biosynthesis, immunity, regulation, mode of action and engineering of the model lantibiotic nisin

This review discusses the state-of-the-art in molecular research on the most prominent and widely applied lantibiotic, i.e., nisin. The developments in understanding its complex biosynthesis and mode of action are highlighted. Moreover, novel applications arising from engineering either nisin itself, or from the construction of totally novel dehydrated and/or lanthionine-containing peptides with desired bioactivities are described. Several challenges still exist in understanding the immunity system and the unique multiple reactions occurring on a single substrate molecule, carried out by the dehydratase NisB and the cyclization enzyme NisC. The recent elucidation of the 3-D structure of NisC forms the exciting beginning of further 3-D-structure determinations of the other biosynthetic enzymes, transporters and immunity proteins. Advances in achieving in vitro activities of lanthionine-forming enzymes will greatly enhance our understanding of the molecular characteristics of the biosynthesis process, opening up new avenues for developing unique and novel biocatalytic processes. Received 9 April 2007; received after revision 31 August 2007; accepted 28 September 2007     

一步法合成多取代2-氨基噻酚衍生物

在碳酸钾作用下, 采用乙酰乙酰胺类化合物与苯硫代异氰酸酯、 溴代乙酸乙酯在N,N-二甲基甲酰胺中反应, 合成了多取代2-氨基噻酚衍生物, 通过核磁共振、 红外光谱及元素分析方法对产物进行表征, 并对该反应机理进行初步探讨.     

A STUDY OF THE IMPOVEMENT OF TENACITY OF POLYACRYLONITRILE PREOXIDED FIBRE BY USING CUPROUS SALT

Polyacrylonitrile preoxided fibre PANOF is an intermediate in carbon fibre preparation. Thequality of PANOF is closely related to the property and structure of carbon fibre. In this paper, thermal mechanical analysis(TMA), thermogravimetric analysis(TGA), swell-ing differential scanning calorimetry(SDSC)and X-ray photoelectron spectroscopy(XPS)wereused to study the increase in tenacity of PANOF from the precursor treated with cuprous salt It has been discovered that the cuprous salt reacts strongly with the uncyclized CN of PANOF,resulting in an increase in the tenacity of PANOF by 30%. The results shwo that the cause of thistenacity improvement is the formation of coordinated complex. Cu~+is the central ion, and PANOFthe ligand. It is due to the coordinate bond that the network structure is formed from uncyclizedCN of PANOF. Therefore the tenacity of PANOF is remarkably increased.     

铜盐对聚丙烯腈预氧化纤维增强作用的研究

聚丙烯腈预氧化纤维(以下简称PANOF)是碳纤维生产过程中的中间产品,其性能的好坏与最终产品碳纤维的优劣密切相关。本文采用热机械分折(TMA)、热失重分折(TGA)、溶胀差示扫描量热分折(SDSC)、X光电子能谱分折(XPS)等实验方法研究了铜盐对PANOF的增强作用。发现Cu~+与PANOF中未环化的氰基有着强烈的相互作用。经铜盐处理后所制得的PANOF,其强度可增加30％。研究结果表明,PANOF得以增强的原因是由于发生了以Cu~+为中心离子,PANOF作为配位体的络合作用。络合配位键的生成使未环化的氰基得以交联,交联网络的形成使PANOF的强度明显提高。     

3—取代—2—酰亚胺—4—噻唑烷酮及其5—乙酸化合物的合成

通过N-烃基-N′-酰基硫脲和卤代乙酸(或卤代乙酸酯)反应,合成了一些新的3-取代-2-酰亚胺-4-噻唑烷酮类化合物,并对反应机理作了探讨.利用N-烃基-N′-酰基硫脲与顺丁烯二酸酐反应,得到3-取代-2-酰亚胺-4-噻唑烷酮-5-乙酸化合物.     

由芳香胺的Mannich碱合成吡唑和吡唑啉类化合物

采用芳香胺的Mannich碱亚硝化后再还原、环化的方法制备了3个吡唑类(Ⅳ_(a~c))和11个吡唑啉类(Ⅱ_(a~k))化合物,其中9个是未见报导的新化合物。所有化合物经红外、元素分析确证,对部分化合物的核磁、质谱作了报导。     

烯胺酰化／缩合-锅法构建5，6，7，8-四氢吡啶[4，3-d]嘧啶核心结构及其在5HT2A受体拮抗剂合成上的应用

报道了1条5HT2A受体拮抗剂的高选择性合成路线．烯胺酰化／缩合-锅法可用于有效构建5,6,7,8-四氢吡啶[4,3-明嘧啶核心结构,其中哌啶催化剂的使用对于这一新方法至关重要．