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首页> 外文期刊>Nature reviews. Endocrinology >Obesity: Success of a new programme for tackling obesity in men.
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Obesity: Success of a new programme for tackling obesity in men.

机译:肥胖:成功解决男性肥胖的新计划。

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Despite the longstanding importance of polyketide natural products in human medicine, nearly all commercial polyketide-based drugs are prepared through fermentation or semi-synthesis. The paucity of manufacturing routes involving de novo chemical synthesis reflects the inability of current methods to concisely address the preparation of these complex structures. Direct alcohol C-H bond functionalization via"C-C bond forming transfer hydrogenation" provides a powerful, new means of constructing type I polyketides that bypasses stoichiometric use of chiral auxiliaries, premetallated C-nucleophiles, and discrete alcohol-to-aldehyde redox reactions. Using this emergent technology, total syntheses of 6-deoxyerythronolide B, bryostatin 7, trienomycins A and F, cyanolide A, roxaticin, and formal syntheses of rifamycin S and scytophycin C, were accomplished. These syntheses represent the most concise routes reported to any member of the respective natural product families.
机译:尽管聚酮化合物天然产物在人类医学中具有长期重要性,但是几乎所有基于聚酮化合物的商业药物都是通过发酵或半合成制备的。涉及从头化学合成的生产路线的匮乏反映了当前方法无法简洁地解决这些复杂结构的制备问题。通过“ C-C键形成转移氢化”的直接醇C-H键官能化提供了构建I型聚酮化合物的有力的新方法,其绕开了手性助剂,预金属化的C-亲核试剂和离散的醇-醛氧化还原反应的化学计量使用。使用这种新兴技术,可以完成6-脱氧赤藓醇内酯B,抑菌素7,曲安霉素A和F,氰化物A,罗克他汀的合成,以及利福霉素S和细胞霉素C的正式合成。这些合成方法代表了报告给各个天然产物家族的任何成员的最简洁的途径。

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