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- W2485399056 abstract "Synthetic macrocycles are an attractive area in drug discovery. However, their use has been hindered by a lack of versatile platforms for the generation of structurally (and thus shape) diverse macrocycle libraries. Herein, we describe a new concept in library synthesis, termed multidimensional diversity-oriented synthesis, and its application towards macrocycles. This enabled the step-efficient generation of a library of 45 novel, structurally diverse, and highly-functionalized macrocycles based around a broad range of scaffolds and incorporating a wide variety of biologically relevant structural motifs. The synthesis strategy exploited the diverse reactivity of aza-ylides and imines, and featured eight different macrocyclization methods, two of which were novel. Computational analyses reveal a broad coverage of molecular shape space by the library and provides insight into how the various diversity-generating steps of the synthesis strategy impact on molecular shape." @default.
- W2485399056 created "2016-08-23" @default.
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- W2485399056 date "2016-08-03" @default.
- W2485399056 modified "2023-09-29" @default.
- W2485399056 title "A Multidimensional Diversity-Oriented Synthesis Strategy for Structurally Diverse and Complex Macrocycles" @default.
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- W2485399056 doi "https://doi.org/10.1002/anie.201605460" @default.
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