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DOI	10.1073/pnas.2108881118
	1,2-Difunctionalized bicyclo[1.1.1]pentanes: Long–sought-after mimetics for ortho/ meta-substituted arenes
	Zhao J.-X.; Chang Y.-X.; He C.; Burke B.J.; Collins M.R.; Del Bel M.; Elleraas J.; Gallego G.M.; Montgomery T.P.; Mousseau J.J.; Nair S.K.; Perry M.A.; Spangler J.E.; Vantourout J.C.; Baran P.S.
发表日期	2021
ISSN	0027-8424
卷号	118 期号:28
英文摘要	The development of a versatile platform for the synthesis of 1,2-difunctionalized bicyclo[1.1.1]pentanes to potentially mimic ortho/ meta-substituted arenes is described. The syntheses of useful building blocks bearing alcohol, amine, and carboxylic acid functional handles have been achieved from a simple common intermediate. Several ortho- and meta-substituted benzene analogs, as well as simple molecular matched pairs, have also been prepared using this platform. The results of in-depth ADME (absorption, distribution, metabolism, and excretion) investigations of these systems are presented, as well as computational studies which validate the ortho- or meta-character of these bioisosteres. © 2021 National Academy of Sciences. All rights reserved.
英文关键词	Bioisosteres; Medicinal chemistry; Synthesis
语种	英语
来源期刊	Proceedings of the National Academy of Sciences of the United States of America
文献类型	期刊论文
条目标识符	http://gcip.llas.ac.cn/handle/2XKMVOVA/238481
作者单位	Department of Chemistry, Scripps Research Institute, San diego, CA 92037, United States; State Key Laboratory of Drug Research, Shanghai Institute of Materia Medica, Chinese Academy of Sciences, Shanghai, 201203, China; Oncology Medicinal Chemistry, Pfizer Worldwide Research,, Development and Medical, San Diego, CA 92121, United States; Discovery Sciences, Medicine Design, Pfizer Worldwide Research, Development and Medical, Groton, CT 06340, United States
推荐引用方式 GB/T 7714	Zhao J.-X.,Chang Y.-X.,He C.,等. 1,2-Difunctionalized bicyclo[1.1.1]pentanes: Long–sought-after mimetics for ortho/ meta-substituted arenes[J],2021,118(28).
APA	Zhao J.-X..,Chang Y.-X..,He C..,Burke B.J..,Collins M.R..,...&Baran P.S..(2021).1,2-Difunctionalized bicyclo[1.1.1]pentanes: Long–sought-after mimetics for ortho/ meta-substituted arenes.Proceedings of the National Academy of Sciences of the United States of America,118(28).
MLA	Zhao J.-X.,et al."1,2-Difunctionalized bicyclo[1.1.1]pentanes: Long–sought-after mimetics for ortho/ meta-substituted arenes".Proceedings of the National Academy of Sciences of the United States of America 118.28(2021).