A novel complexity-to-diversity strategy for the diversity-oriented synthesis of structurally diverse and complex macrocycles from quinine.

Bioorganic & Medicinal Chemistry(2017)

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摘要
Recent years have witnessed a global decline in the productivity and advancement of the pharmaceutical industry. A major contributing factor to this is the downturn in drug discovery successes. This can be attributed to the lack of structural (particularly scaffold) diversity and structural complexity exhibited by current small molecule screening collections.
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ADMET,CtD,DCC,DCE,DIPEA,DMAP,DMF,DMSO,DOS,EDC,FDA,HATU,HTS,NCE,PMI,PPI,PTSA,TEA,THF
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