- Total syntheses of smenothiazoles A and B
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Concise total syntheses of smenothiazoles A (1) and B (2), two distinguished vinyl chloride containing natural products isolated from the marine sponge S. aurea, have been developed. Silastannation, Stille reaction and a carefully controlled desilylchlorination were employed as key steps to construct unique polyketide acid fragments, and the optimized reaction conditions avoided migration of 2,5-diene to a 2,4-conjugated system. This report unambiguously confirmed the structures of both natural products.
- Ma, Xiao,Chen, Yajie,Chen, Sigui,Xu, Zhengshuang,Ye, Tao
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p. 7196 - 7203
(2017/09/07)
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- Synthesis of dysideaproline e using organocatalysis
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(S)-4,4-Dichloro-3-methylbutanoic acid was prepared in 51% overall yield from commercially available starting materials using an organocatalytic transfer hydrogenation to 4,4-dichloro-3-methylbut-2-enal in the key step. The (S)-dichloro acid was used as an intermediate in the first total synthesis of dysideaproline E and a diastereomer confirming the structure of the natural product.
- Owusu-Ansah, Ernest,Durow, Amanda C.,Harding, John R.,Jordan, Angela C.,O'Connell, Susan J.,Willis, Christine L.
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experimental part
p. 265 - 272
(2011/02/24)
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- Pyrrolidine amides of pyrazolodihydropyrimidines as potent and selective KV1.5 blockers
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Design and synthesis of pyrazolodihydropyrimidines as KV1.5 blockers led to the discovery of 7d as a potent and selective antagonist. This compound showed atrial selective prolongation of effective refractory period in rabbits and was selected for clinical development.
- Lloyd, John,Finlay, Heather J.,Vacarro, Wayne,Hyunh, Tram,Kover, Alexander,Bhandaru, Rao,Yan, Lin,Atwal, Karnail,Conder, Mary Lee,Jenkins-West, Tonya,Shi, Hong,Huang, Christine,Li, Danshi,Sun, Huabin,Levesque, Paul
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scheme or table
p. 1436 - 1439
(2010/07/02)
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