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Total Synthesis of Hapalosin and Its Analogues:Construction of Three Small Hapalosin C-9 Analogues Libraries and Studies on Total Synthesis of Melleumins A and B

Abstract

环肽类化合物是一类结构复杂多样的天然产物。自然界中存在大量的环肽类化合物,表现出多种生物活性,如杀虫、抗菌、抗肿瘤、抗病毒、和免疫抑制等。环肽类化合物作为富有实用前景的先导化合物在药物发现中受到越来越多的关注,新的活性天然产物也不断被发现。同时,环肽类天然产物的全合成也成为不对称合成的新热点。Hapalosin(1a)是1994年从蓝藻中分离提取的一类新型结构的环肽化合物,因其对肿瘤细胞的多药耐药性细胞系有很强的抑制作用,一经发现就引起了广大合成化学家和药物化学家的关注。本论文的目标在于拓展手性合成砌块(R/S)苹果酰亚胺的多用性,将其应用于环肽类天然产物hapalosin和melleumin...Cylcopeptides with complex and diversified structures are widespread in nature. Many of them exhibit various biological activities, such as, antibiotics, antitumor, antivirus, immunosuppressive effect and pesticides. As promising lead compounds in drug discovery, cylcopeptides are receiving more and more attention. And the studies on the asymmetric total synthesis of these compounds have been a ne...学位:理学博士院系专业:化学化工学院_有机化学学号:B20022501

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