外消旋木榄醇甲的简捷合成

报道了天然产物木榄醇甲的一种高效合成方法. 目标分子结构中的饱和碳链部分以廉价的化工原料4-羰基戊酸(国内俗称“左旋糖酸”或“果糖酸”)为起始原料合成. 经Wittig反应与间甲氧基苯甲醛相连接后, 对所形成的碳-碳双键进行环氧化并在苄位进行选择性脱氧形成关环前体. 关键的桥环部分结构的建立利用了由缩酮为烷化剂的分子内Friedel-Crafts反应.     

一种含硝基的Plakoric酸类似物的合成

Synthesis of a nitro analogue of plakoric acid is presented. The peroxy bond was incorporated into the substrate structure through a boron trifluoride etherate catalyzed methoxy-hydroperoxy group partial exchange reaction in diethyl ether with urea-hydrogen peroxide complex （UHP, a commercially available solid reagent） as the source of the hydrogen peroxide. Under the given conditions, only one of the two methoxyl groups underwent the MeO—— OOH exchange and the resulting hydroperoxy hemiketal proceeded directly to the end product through an intramolecular Michael addition of the hydroperoxyl group to the nitro group activated carbon-carbon double bond.     

A Formal Synthesis of (+)-Cassiol Exploiting Meyers'''' Bicyclic Lactam Methodology

ＩｎｔｒｏｄｕｃｔｉｏｎＩｎ 1988,ｆｒｏｍａｎａｑｕｅｏｕｓｅｘｔｒａｃｔｉｏｎｏｆＣｈｉｎｅｓｅｃｉｎ ｎａｍｏｎ ,ｗｈｉｃｈｈａｓｌｏｎｇｂｅｅｎｕｓｅｄｉｎｔｈｅｔｒａｄｉｔｉｏｎａｌＣｈｉ ｎｅｓｅｍｅｄｉｃｉｎｅａｓａｄｉａｐｈｏｒｅｔｉｃ ,ａｎｔｉｐｙｒｅｔｉｃ ,ｏｒａｎａｌｇｅｓｉｃａｇｅｎｔ,Ｆｕｋａｙａａｎｄｃｏ ｗｏｒｋｅｒｓｉｓｏｌａｔｅｄｃａｓｓｉｏｓｉｄｅ (1)ａｎｄｆｏｕｎｄｔｈａｔｔｈｉｓｃｏｍｐｏｕｎｄｐｏｓｓｅｓｓｅｄｒｅｍａｒｋａｂｌｅａｎｔｉｕｌ ｃｅｒｏｇｅｎｉ…     

有机过氧化物中过氧键的建立(引入)方法

有机过氧化物目前已发展成非常重要的一类抗疟药物. 形成/引入过氧键是合成有机过氧化物的关键步骤和难点所在. 对合成有机过氧化物时常见的建立或引入过氧键的方法、各方法的适用范围及优劣所在作了简要的综述.     

无C环青蒿素类似物的合成研究

以天然的(-)-香芹酮为原料,设计、合成了四种环状烯醇醚,它们是标题化合物的关键中间体,然而这些化合物出乎意料地与单线态氧不发生反应,仅为光氧化反应提供了有参考价值的经验积累,以(-)-薄荷醇为原料用同样方法则可合成得到化合物4的骨架化合物的混合物。     

Alkylation of Sulfur Ligand in Cysteinate－Iron Chelates by a 1,2,4,5－Tetraoxane

Reaction of a 1,2, 4, 5-tetraoxane with cysteinate-iron in the presence of excess methyl cysteinate led to formation of sulfuralkylated methyl cysteinate in 33 % yield, illustrating a possible mechanism for tetraoxanes‘ antimalarial action.     

有机合成的新世纪――－有机合成近年进展鉴赏

本文简要介绍了2005年至今有机合成领域的进展,第一部份有机合成方法学的一些新进展中突出介绍了金属参与的有机合成反应、自由基介导的合成反应、"一个反应瓶"内的多步反应以及不对称反应四个方面;第二部份复杂天然产物全合成则以10个分子的为例介绍这方面的进展。     

一种四氧螺环过氧化物的合成

本文报道了一种新型的含双过氧键的螺环化合物的合成。该合成以双氧水为过氧键来源，经酮羰基的缩酮交换反应在底物中引入两个过氧氢基。然后通过汞离子诱发的对双键的加成反应分别将两个过氧氢基的羟基端固定在碳骨架上，形成双过氧螺环结构。螺环两端都含酯基，可供进一步结构修饰、合成衍生物用。     

Synthesis of a 1,2,7,8-Tetraoxa-spiro[5.5]undecane

Synthesis of a new spiro organic peroxide is described. The peroxy bonds were incorporated into the substrate framework via an acid-catalyzed ketal exchange reaction using hydrogen peroxide as the source of peroxy linkage. The hydroperoxyl groups were then bonded at the OH ends via Hg（II）-induced electrophilic additions to the C-C double bonds, giving a novel sprio structure with one peroxy bond in each of the two six-membered rings. The ester functionalities in the side chains also make it possible to conduct further structural modifications.     

若干简单Plakoric acid类似物的合成及体外抗疟活性

Several simple analogues of peroxyplakoric acid were synthesized by using Kobayashi＇s method to construct the key 1,2-dioxane core and tested in vitro for antimalarial activity. The scope and limitation of the method was also briefly examined.