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中文摘要：
本项目选择6类具有抗癌活性的天然产物（Haouamines A/ B，毛萼乙素，Ineleganolide ，文多灵碱，Strychnofoline和Spirotryprostatin B）、具有抗癌/促进骨生长活性的拟天然产物（3-羟基吡咯烷/4-羟基内酰胺）、以及抗Alzheimer（Cerebrosides sphingolipid、Agelasphine-9b和KRN-7000），抗炎活性环肽Thalassospiramides A 和B，和新颖结构、具有挑战性的天然产物Sarain A和百部生物碱stemocurtisine，oxystemokerrilactone，oxystemokerrin，oxystemokerrin N-oxyde，拟结合灵活多用的不对称合成方法学探索，开展其结构多样性合成，包括全合成、类似物合成研究，和构建若干拟天然产物库，并进行抗癌等生物活性研究。
英文摘要：
synthetic methodology；C-C bond formation；diversity-oriented synthesis；total synthesis；natural products
结论摘要：
本项目从发展灵活多用合成方法学入手开展天然产物的多样性合成研究。一、发展了若干多样性导向的合成方法:（1）基于酰胺活化、具有普适性和步骤经济性的C-C键形成方法学，包括叔酰胺直接还原双烷基化和单烷基化方法、仲酰胺直接还原烷基化、仲酰胺直接转化为酮、以仲酰胺为酰化剂的付克酰化反应；(2) 酚氧化偶联形成新颖螺环内酰胺的方法；(3) 酰胺？位芳基化串联烷基化反应用于含芳基季碳的合成方法；(4) 5-取代特特拉姆酯合成砌块及相应的高立体选择性C-C键形成方法；(5) SmI2介导的新合成方法学; (6)。基于分子内亲核酰化反应构建多取代哌啶-4-酮砌块的合成方法学。 二、应用该项目发展的多样性合成方法，完成了抗癌活性生物碱chaetominine、强效免疫抑制剂FR901483 、百部生物碱(-)-sessilifoliamide J 和stenine等20余个天然产物及其类似物和立体异构体的不对称全合成。三、发展了快捷构筑复杂天然产物sarain A核心三环骨架、毛萼乙素等二萜的ABCD四环、文多灵碱类化合物分子骨架和haliclonin A三环核心结构的方法。该项目所发展方法和全合成体现了四个特点，一是灵活多用性，可用于天然产物的多样性合成；二是合成策略高效简洁，融合了仿生合成、一瓶多步、串联反应等策略；三是在全合成中追求不对称合成和高立体选择性合成；四是多个天然产物为首次全合成，证实或更正了天然产物的结构并提出合理的生源合成途径。所发展的部分方法得到了国内外同行的关注、点评，被《Nature？ Chemistry》、ChemPubSoc Europe's Chemistry Views magazine、“Noteworthy Chemistry” 、Synfacts、国际有机化学学术网站Organic Chemistry Portal作为研究亮点评介。发展的方法和手性合成砌块被国际同行采用5次。在国内外重要学术刊物上发表论文98篇（Angew. Chem. Engl. Ed．、Chem. Eur. J 、Chem. Commun. 、Org. Lett.、J. Org. Chem. 、Adv. Synth. Catal.、Green Chem. 、Chem. Asian J.等）。申请发明专利18项,已授权6项。
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期刊论文
Versatile One-Pot Reductive Alkylation of Lactams/Amides via Amide Activation: Application to the Co
Inhibitory effects of hinokitiol on tyrosinase activity and melanin biosynthesis and its antimicrobi
Asymmetric syntheses of (8R,8aS)- and (8R,8aR)-8-hydroxy-5-indolizidinones: Two promising oxygenated
Versatile and Direct Transformation of Secondary Amides into Ketones via Organocerium Reagents-Based
A Flexible Asymmetric Approach to Methyl 5-Alkyltetramates and Its Application in the Synthesis of C
SmI2-Mediated Radical Cross-Couplings of alpha-Hydroxylated Aza-hemiacetals and N,S-Acetals with alp
Enantioselective Synthesis of Glutarimide Alkaloids Cordiarimides A, B, Crotonimides A, B, and Juloc
Studies towards the Total Asymmetric Synthesis of the Pentacyclic Indole Alkaloid Arboflorine: Asymm
A Flexible Approach to Azasugars: Asymmetric Total Syntheses of (+)-Castanospermine, (+)-7-Deoxy-6-e
A Concise, Protection-Free and Divergent Approach for the Enantioselective Syntheses of Two Pheromon
A flexible approach for the asymmetric syntheses of hyacinthacines A(2), A(3) and structural confirm
Direct, One-pot Sequential Reductive Alkylation of Lactams/Amides with Grignard and Organolithium Re
Studies towards an Enantioselective Total Synthesis of Sarain A: A Concise Asymmetric Construction o
Concise synthesis of two advanced intermediates for the asymmetric synthesis of polyhydroxylated ind
N-Benzyloxymalimide for an easy access to 5-alkyl-3-pyrrolin-2-ones: asymmetric synthesis of the mix
Highly diastereoselective addition of alkynylmagnesium chlorides to N-tert-butanesulfinyl aldimines:
SmI2-Mediated Intermolecular Coupling of Lactam N-?-Radicals with Activated Alkenes: Asymmetric Synt
Practical, environment-benign and atom economic KOAc-catalysed deprotection of aryl TIPS ethers unde
A concise and fully selective synthesis of the ant venom alkaloid (3S,5R,8S,9S)-3-butyl-5-propyl-8-h
Asymmetric Syntheses and Wnt Signal Inhibitory Activity of Melleumin A and Four Analogues of Melleum
A versatile approach to cis-5-substituted 4-hydroxy-2-pyrrolidinones: asymmetric synthesis of angiog
Total Synthesis of Emericellamide A: A Secondary Metabolite of Marine Cyclic Depsipeptide with Antim
BF(3)center dot Et(2)O catalyzed diastereoselective nucleophilic reactions of 3-silyloxypiperidine N
Samarium diiodide-mediated reductive couplings of chiral nitrones with aldehydes/ketones and acyl ch
Direct B-Alkyl Suzuki-Miyaura Cross-Coupling of Trialkylboranes with Aryl Bromides in the Presence o
A new method for the construction of the hydroxylated tropane skeleton: enantioselective synthesis o
Copper-Catalyzed Arylation of o-Bromoanilides: Highly Flexible Synthesis of Hexahydropyrroloindole A
A Short and Flexible Synthetic Approach to the Naturally Occurring Racemic Neoclausenamide and Its A
Enantioselective Syntheses of Rigidiusculamides A and B: Revision of the Relative Stereochemistry of
Direct Transformation of Secondary Amides into Secondary Amines: Triflic Anhydride Activated Reducti
A flexible approach to construct three contiguous chiral centers of sphingolipids, and asymmetric sy
Towards Reaction Control: cis-Diastereoselective Reductive Dehydroxylation of 5-Alkyl-4-benzyloxy-5-
A concise and divergent approach to radicamine B and hyacinthacine A(3) based on a step-economic tra
An unexpected high erythro-selection in the Grignard reaction with an N,O-acetal: a concise asymmetr
One-pot reductive coupling of N-acylcarbamates with activated alkenes: Application to the asymmetric
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