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15 result(s) for "全合成"
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氨柔比星治疗小细胞肺癌研究进展
盐酸氨柔比星是日本住友制药株式会社开发全合成的蒽环霉素类抗恶性肿瘤药物,于2002年在日本注册并上市,被批准用于非小细胞肺癌及小细胞肺癌(small cell lung cancer,SCLC)的治疗,本文就氨柔比星治疗小细胞肺癌的研究进展做一综述。
C-H bond activation in the total syntheses of natural products
The transition metal-mediated C-H bond activation has emerged as a powerful and ideal method for the total syntheses of natural products and pharmaceuticals, and has had a significant impact on synthetic planning and strategy in complex natural products. In this review, we describe selected recent examples of the transition metal-mediated C-H bond activation strategies for the rapid syntheses of natural products.
Asymmetric construction of all-carbon quaternary stereocenters in the total synthesis of natural products
Structure units containing all-carbon quaternary stereogenic center are found in many bioactive natural products. However, enantioselective construction of this type of structure units has been a formidable challenge for synthetic community due to the steric hindrance enforced by all-carbon quatemary stereocenters. In this review, we present the achievements made by Chinese scientists in the area of asymmetric synthesis of all-carbon quaternary stereocenters in natural products during the past two years.
Advances of radical and photo reactions in natural products synthesis
This review will focus on the recent advances of radical and photo reactions and their applications in the natural products total synthesis. A brief introduction to the development and mechanism of the newly developed radical and photo reactions will be presented. The organization of the each section is based on the type of reactions used. Examples of synthetic applications are discussed to demonstrate the potential of related methodologies and inspire future explorations.
The first enantioselective total synthesis of(+)-preussin B and an improved synthesis of(+)-preussin by step-economical methods
The first enantioselective total synthesis of(+)-preussin B and an improved synthesis of the antifungal alkaloid(+)-preussin are described. Our approach relied on the four step-economical synthetic methods developed in our laboratory:(1) the cis-diastereoselective reductive dehydroxylation of hemiaminals;(2) the direct amide/lactam reductive alkylation;(3) the one-pot N,O-bisdebenzylation-N-methylation; and(4) the one-step synthesis of malimide from malic acid. Both total syntheses are quite concise, which have been achieved in six steps, and gave overall yields of 25.7% and 27.6%, respectively.
Stereoselective construction of skipped polyol enabled by oxonia-Cope rearrangement and iodolactonization: enantioselective synthesis of (+)-yashabushitriol
Skipped polyol is a common motif in numerous biologically significant polyketides and has been the focus of the development of novel synthetic methods and strategies. In this work, we devised a highly diastereoselective approach to access skipped triol (anti, syn-isomer) from a chiral α-allenic alcohol which was derived from kinetic resolution in our previous studies. An iodolactonization and subsequent radical deiodonation efficiently introduced the hydroxyl group at C3 in a highly diastereoselective manner and exemplified in enantioselective total synthesis of (+)-yashabushitriol.
Total synthesis of proposed structures ofjiangrines C and D
On the basis of the proposed structures ofjiangrines C and D, a synthetic strategy was initiated from D-glyceraldehyde acetonide, a readily available chiral material. Through a linear seven-step synthesis, the target molecules were accomplished. However, all characteristic data of the synthetic 3 and 4 were found to be different from those of natural jiangrines C and D. Accordingly, the molecular structures ofjiangrines should be revised and a possible molecular skeleton for them was proposed.
Michael addition-based cyclization strategy in the total synthesis of Lycopodium alkaloids
Lycopodium alkaloids, a unique family of biologically important natural products isolated and characterized from various species ofLycopodium (sensu lato), have attracted extensive attention from chemists and pharmacists in the past three decades. Michael addition-based cyclization has been successfully employed as an elegant and efficient ring-construction protocol of constructing key cyclohexanone intermediates in the total synthesis of Lycopodium alkaloids. This mini-review chooses and summarizes several representative total syntheses of various Lycopodium alkaloids in which intramolecular Michael addition severed as the key methodology.
Recent advances in terpenoid syntheses from China
Total syntheses of terpenoids play an essential role in the development of synthetic organic chemistry and medicinal science. Chinese synthetic community has made more and more profound contribution to this field and has gradually grown into a major force in the world over the past years. In this review, we shall celebrate the achievement by surveying the recent terpenoid syntheses from China since 2010.
Total synthesis of (-)-isoaltholactone
A short and efficient stereoselective synthesis of a styryllactone (-)-isoaltholactone has been achieved in seven steps and 33% overall yield, starting from the readily available carbohydrate D-mannose. The key steps of our synthesis involve intramolecu-lar tetrahydrofuran cyclization and one-pot acetonide deprotection-lactonization.