Didemnaketal A类似物的合成研究──C1-C7中间体的合成

寻找抗艾滋病活性的抚导化合物是当前药物化学研究领域中的热点之一.     

Efficient Synthesis of the C1-C7 Fragment of Didemnaketal A

The stereoselective synthesis of the CI-C7 fragment (3R,4S,6R)-3,4-di[(tert-butyldimethylsilyl)oxy]-7-hydroxy-6-methylheptan-2-one, which is the crucial intermediate for synthesis ofthe HIV-1 protease inhibitive didemnaketals, was developed via 12 steps from the natural ( )-pulegone.     

Didemnaketal B的C17-C28片段的不对称合成

以易得的天然手性源(R)-(+)-长叶薄荷酮和(S)-(-)-香茅醛为起始原料，经过21步反应，成功地实现了Didemnaketal B C17-C28片段的不对称合成。关键反应分别为利用分子内的手性诱导来引入其余的两个手性中心和不平常的Julia偶联实现了C(22)-C(23)中三取代的E式双键的构筑。     

生物碱Actinophyllic Acid三环中间体的不对称合成

以(S)-3-(2,2-二甲基-5-(3-甲基-1H-吲哚-2-基)-1,3-二氧杂环己烷-5-基)吡咯烷-2-酮为原料,经吡咯烷酮还原开环、串联的氢化脱保护/分子内还原胺化反应等关键步骤,合成了吲哚生物碱actinophyllic acid的A/B/C环手性中间体(S)-3-(2-(2-氯乙酰氨基)-2′,2′-二甲基-1,2,3,4,5,7-六氢螺[氮杂环辛烷并[4,3-b]吲哚-6,5′-[1,3]二氧杂环己烷]-5-基)-3-丙酮酸甲酯（9）; 9可在氧化条件下转化为A/B/G环中间体(S)-7-(2-(2-氯乙酰氨基)乙基)-2′,2′-二甲基-8-氧代-7,8-二氢-5-H-螺[环庚烯并[b]吲哚-6,5′-[1,3]二氧杂环己烷]-9-甲酸酯（10）。该合成路线涉及9个新化合物,其结构经¹H NMR,¹³C NMR, 2D NMR和LC-MS(ESI)表征。     

1β—Methyl Carbapenem中间体的合成

综述了１β－Ｍｅｔｈｙｌ Ｃａｒｂａｐｅｎｅｍ中间体的合成方法，重点强调了如何构筑１位β构型的甲基。参考文献３７篇。     

聚苯醚合成机理的研究进展

聚苯醚是当今世界五大通用型工程塑料之一,广泛应用于各行各业。聚苯醚从首次合成出来距今已有半个多世纪,但是关于聚苯醚的合成机理至今仍然没有完全阐明。本文主要介绍了合成聚苯醚氧化偶合反应的三种可能机理:苯氧自由基协同配合物偶合机理、单电子转移偶合机理和一步双电子转移偶合机理。其中,一步双电子转移偶合机理是目前学术界所普遍接受的,并进一步阐述了聚苯醚合成过程中醌缩酮中间体再分配和醌缩酮中间体重排两种合成聚苯醚的链增长机理。     

Brazilin类似物的合成

以3-(3,4-二甲氧苯基)丙酸为原料, 经分子内傅-克反应、双羟基化、Lombardo 反应, 高价碘的氧化及类Pinacol重排等共10步反应, 完成了brazilin类似物的合成.     

手性螺环配体的合成及其在不对称催化反应中的应用研究进展

手性螺环配体的合成及其在不对称催化反应中的应用是不对称合成和催化研究中重要的研究领域之一, 一些手性螺环配体被合成出来并成功地应用于不对称催化反应中. 综述了近十年来手性螺环配体的合成及在不对称催化反应中的应用研究进展.     

Efficient Synthesis of the Cl- C7 Fragment of Didemnaketal A

The stereoselective synthesis of the C1-C7 fragment (3R,4S,6R)-3,4-di[(tert-butyl-dimethylsilyl)oxy]-7-hydroxy-6-methylheptan-2-one, which is the crucial intermediate for synthesis of the HIV-1 protease inhibitive didemnaketals, was developed via 12 steps from the natural (+)-pulegone.     

Efficient Synthesis of the C1-C8 Fragment of Reveromycins

A stereocontrolled synthesis of the C1-C8 fragment of reveromycins is presented herein. Key to our strategy was the implementation of Evans' aldol reaction that delivered the desired stereochemistry at the C4 and C5 stereocenters.     

Synthetic Studies Toward Bryostatin 1: Preparation of a C(1)-C(16) Fragment by Pyran Annulation

An expeditious assembly of a C₁-C₁₆ subunit of bryostatin 1 is described. A pyran annulation reaction was utilized to form the B-ring by reaction of a hydroxy-allylsilane with a fully elaborated A-ring subunit. This annulation process proceeded with complete diastereoselectivity and in excellent isolated yield despite the presence of potentially sensitive functionality in the A-ring segment.     

Synthesis of the C1-C20 and C15-C27 segments of aplyronine A

The synthesis of C1-C20 and C15-C27 segments of Aplyronine A is described. Oxidative cleavage of cyclic vinyl sulfones has been used to prepare key fragments of Aplyronine A. Key precursors are united by Horner-Wadsworth-Emmons and Julia-Kociensky olefination for the respective elaboration of the C1-C20 and C15-C27 segments.     

Synthetic Studies Toward Providencin: Efficient Construction of a Furanyl-Cyclobutanone Fragment

Described is the construction of a furanyl-cylcobutanone fragment suited for incorporation into a synthesis of the naturally occurring anti-cancer agent Providencin.