对映选择合成
兴奋剂
化学
产量(工程)
BETA(编程语言)
三氟甲基
衍生工具(金融)
四级碳
立体化学
组合化学
受体
有机化学
催化作用
生物化学
计算机科学
材料科学
经济
冶金
程序设计语言
金融经济学
烷基
作者
Matthew L. Maddess,Jeremy P. Scott,Anthony Alorati,Carl A. Baxter,Nadine Bremeyer,Sarah E. Brewer,Kevin R. Campos,Ed Cleator,A. Dieguez-Vazquez,Andrew Gibb,Andrew Gibson,Melissa E. Howard,Stephen P. Keen,Artis Klapars,Jaemoon Lee,Jing Li,Joseph E. Lynch,Peter R. Mullens,Debra J. Wallace,Robert D. Wilson
摘要
The development and execution of a practical asymmetric synthesis of the estrogen receptor beta selective agonist (8R,10aS)-6-(trifluoromethyl)-8,9,10,11-tetrahydro-8,10a-methanocyclohepta[1,2]indeno[4,5-d][1,2,3]triazol-7(3H)-one is described. The optimized route features a key chiral auxiliary-mediated dialkylation approach to set the all-carbon quaternary center with exceptional stereocontrol. Overall, the chemistry has been used to prepare >30 kg of drug candidate in 21% overall yield through 13 longest linear steps and with >99% ee.
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