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1,2-Difunctionalized bicyclo[1.1.1]pentanes: Long-sought-after mimetics for ortho/ meta-substituted arenes

文献类型：期刊论文

作者Zhao, Jin-Xin1,2; Chang, Yu-Xuan1; He, Chi1; Burke, Benjamin J.3; Collins, Michael R.3; Del Bel, Matthew3; Elleraas, Jeff3; Gallego, Gary M.3; Montgomery, T. Patrick3; Mousseau, James J.4
刊名PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA
出版日期2021-07-13
卷号118期号:28页码:5
关键词synthesis medicinal chemistry bioisosteres
ISSN号0027-8424
DOI10.1073/pnas.2108881118|1of5
通讯作者Collins, Michael R.(michael.collins@pfizer.com) ; Baran, Phil S.(pbaran@scripps.edu)
英文摘要The development of a versatile platform for the synthesis of 1,2difunctionalized 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 orthoor meta-character of these bioisosteres.
WOS关键词REDOX-ACTIVE ESTERS
资助项目Pfizer ; NIH[GM-118176]
WOS研究方向Science & Technology - Other Topics
语种英语
WOS记录号WOS:000685035200004
出版者NATL ACAD SCIENCES
源URL[http://119.78.100.183/handle/2S10ELR8/297638]  
专题新药研究国家重点实验室
通讯作者Collins, Michael R.; Baran, Phil S.
作者单位1.Scripps Res Inst, Dept Chem, La Jolla, CA 92037 USA
2.Chinese Acad Sci, Shanghai Inst Mat Med, State Key Lab Drug Res, Shanghai 201203, Peoples R China
3.Pfizer Worldwide Res Dev & Med, Oncol Med Chem, San Diego, CA 92121 USA
4.Pfizer Worldwide Res Dev & Med, Discovery Sci, Med Design, Groton, CT 06340 USA
推荐引用方式
GB/T 7714		 Zhao, Jin-Xin,Chang, Yu-Xuan,He, Chi,et al. 1,2-Difunctionalized bicyclo[1.1.1]pentanes: Long-sought-after mimetics for ortho/ meta-substituted arenes[J]. PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF THE UNITED STATES OF AMERICA,2021,118(28):5.
APA Zhao, Jin-Xin.,Chang, Yu-Xuan.,He, Chi.,Burke, Benjamin J..,Collins, Michael R..,...&Baran, Phil 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),5.
MLA Zhao, Jin-Xin,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):5.

入库方式： OAI收割

来源：上海药物研究所

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