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 |
| ISSN号 | 0027-8424 |
| 关键词 | synthesis medicinal chemistry bioisosteres |
| DOI | 10.1073/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 |
| 出版者 | NATL ACAD SCIENCES |
| WOS记录号 | WOS:000685035200004 |
| 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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