GSTDTAP

浏览/检索结果: 共13条,第1-10条 帮助

已选(0)清除 条数/页:   排序方式:
Copper-mediated synthesis of drug-like bicyclopentanes 期刊论文
NATURE, 2020, 580 (7802) : 220-+
作者:  Canavelli, Pierre;  Islam, Saidul;  Powner, Matthew W.
收藏  |  浏览/下载:7/0  |  提交时间:2020/07/03

Multicomponent reactions are relied on in both academic and industrial synthetic organic chemistry owing to their step- and atom-economy advantages over traditional synthetic sequences(1). Recently, bicyclo[1.1.1]pentane (BCP) motifs have become valuable as pharmaceutical bioisosteres of benzene rings, and in particular 1,3-disubstituted BCP moieties have become widely adopted in medicinal chemistry as para-phenyl ring replacements(2). These structures are often generated from [1.1.1]propellane via opening of the internal C-C bond through the addition of either radicals or metal-based nucleophiles(3-13). The resulting propellane-addition adducts are then transformed to the requisite polysubstituted BCP compounds via a range of synthetic sequences that traditionally involve multiple chemical steps. Although this approach has been effective so far, a multicomponent reaction that enables single-step access to complex and diverse polysubstituted drug-like BCP products would be more time efficient compared to current stepwise approaches. Here we report a one-step three-component radical coupling of [1.1.1]propellane to afford diverse functionalized bicyclopentanes using various radical precursors and heteroatom nucleophiles via a metallaphotoredox catalysis protocol. This copper-mediated reaction operates on short timescales (five minutes to one hour) across multiple (more than ten) nucleophile classes and can accommodate a diverse array of radical precursors, including those that generate alkyl, alpha-acyl, trifluoromethyl and sulfonyl radicals. This method has been used to rapidly prepare BCP analogues of known pharmaceuticals, one of which is substantially more metabolically stable than its commercial progenitor.


A one-step, three-component radical coupling of [1.1.1]propellane by a photoredox reaction mediated by a copper catalyst produces drug-like bicyclopentanes.


  
Episodic Occurrence of Field-Aligned Energetic Ions on the Dayside 期刊论文
GEOPHYSICAL RESEARCH LETTERS, 2020, 47 (2)
作者:  Yue, Chao;  Bortnik, Jacob;  Zou, Shasha;  Nishimura, Yukitoshi;  Foster, John C.;  Coppeans, Thomas;  Ma, Qianli;  Zong, Qiugang;  Hull, A. J.;  Henderson, Mike;  Reeves, Geoffrey D.;  Spence, Harlan E.
收藏  |  浏览/下载:7/0  |  提交时间:2020/07/02
field-aligned PADs  ring current energetic ions  ionospheric disturbance  tail injections  
Segmentation of SED by Boundary Flows Associated With Westward Drifting Partial Ring current 期刊论文
GEOPHYSICAL RESEARCH LETTERS, 2019, 46 (14) : 7920-7928
作者:  Wang, Zihan;  Zou, Shasha;  Coppeans, Thomas;  Ren, Jiaen;  Ridley, Aaron;  Gombosi, Tamas
收藏  |  浏览/下载:7/0  |  提交时间:2019/11/27
polar cap patch  partial ring current  Birkeland current boundary flow  
Ion Heating by Electromagnetic Ion Cyclotron Waves and Magnetosonic Waves in the Earth's Inner Magnetosphere 期刊论文
GEOPHYSICAL RESEARCH LETTERS, 2019, 46 (12) : 6258-6267
作者:  Ma, Q.;  Li, W.;  Yue, C.;  Thorne, R. M.;  Bortnik, J.;  Kletzing, C. A.;  Kurth, W. S.;  Hospodarsky, G. B.;  Reeves, G. D.;  Spence, H. E.
收藏  |  浏览/下载:9/0  |  提交时间:2019/11/26
ion heating  electromagnetic ion cyclotron waves  ring current  resonant interaction in plasmasphere  Van Allen Probes observation  quasilinear modeling  
Quenching of Equatorial Magnetosonic Waves by Substorm Proton Injections 期刊论文
GEOPHYSICAL RESEARCH LETTERS, 2019, 46 (12) : 6156-6167
作者:  Dai, Guyue;  Su, Zhenpeng;  Liu, Nigang;  Wang, Bin;  Zheng, Huinan;  Wang, Yuming;  Wang, Shui
收藏  |  浏览/下载:6/0  |  提交时间:2019/11/26
radiation belt  ring current  wave-particle interaction  magnetosonic wave  Bernstein mode instability  substorm injection  
Magnetospheric Signatures of STEVE: Implications for the Magnetospheric Energy Source and Interhemispheric Conjugacy 期刊论文
GEOPHYSICAL RESEARCH LETTERS, 2019, 46 (11) : 5637-5644
作者:  Nishimura, Y.;  Gallardo-Lacourt, B.;  Zou, Y.;  Mishin, E.;  Knudsen, D. J.;  Donovan, E. F.;  Angelopoulos, V.;  Raybell, R.
收藏  |  浏览/下载:6/0  |  提交时间:2019/11/26
STEVE  SAPS  interhemispheric conjugate phenomena  storm and ring current  THEMIS  Van Allen Probes (RBSP)  
Ion Energies Dominating Energy Density in the Inner Magnetosphere: Spatial Distributions and Composition, Observed by Arase/MEP-i 期刊论文
GEOPHYSICAL RESEARCH LETTERS, 2018, 45 (22) : 12153-12162
作者:  Keika, K.;  Kasahara, S.;  Yokota, S.;  Hoshino, M.;  Seki, K.;  Nose, M.;  Amano, T.;  Miyoshi, Y.;  Shinohara, I.
收藏  |  浏览/下载:8/0  |  提交时间:2019/04/09
magnetic storms  ring current ions  energy density  transport and acceleration  substorms  Arase  
Substorm-Associated Ionospheric Flow Fluctuations During the 27 March 2017 Magnetic Storm: SuperDARN-Arase Conjunction 期刊论文
GEOPHYSICAL RESEARCH LETTERS, 2018, 45 (18) : 9441-9449
作者:  Hori, T.;  Nishitani, N.;  Shepherd, S. G.;  Ruohoniemi, J. M.;  Connors, M.;  Teramoto, M.;  Nakano, S.;  Seki, K.;  Takahashi, N.;  Kasahara, S.;  Yokota, S.;  Mitani, T.;  Takashima, T.;  Higashio, N.;  Matsuoka, A.;  Asamura, K.;  Kazama, Y.;  Wang, S. -Y.;  Tam, S. W. Y.;  Chang, T. -F.;  Wang, B. -J.;  Miyoshi, Y.;  Shinohara, I.
收藏  |  浏览/下载:14/0  |  提交时间:2019/04/09
SuperDARN  ULF wave  substorm injection  ERG  ring current electron  M-I coupling  
Magnetosonic Harmonic Falling and Rising Frequency Emissions Potentially Generated by Nonlinear Wave-Wave Interactions in the Van Allen Radiation Belts 期刊论文
GEOPHYSICAL RESEARCH LETTERS, 2018, 45 (16) : 7985-7995
作者:  Liu, Nigang;  Su, Zhenpeng;  Zheng, Huinan;  Wang, Yuming;  Wang, Shui
收藏  |  浏览/下载:5/0  |  提交时间:2019/04/09
magnetosonic wave  rising  falling frequency  Bernstein mode instability  wave propagation  radiation belt  ring current  
Magnetic Field Dipolarization and Its Associated Ion Flux Variations in the Dawnside Deep Inner Magnetosphere: Arase Observations 期刊论文
GEOPHYSICAL RESEARCH LETTERS, 2018, 45 (16) : 7942-7950
作者:  Nose, M.;  Matsuoka, A.;  Kasahara, S.;  Yokota, S.;  Teramoto, M.;  Keika, K.;  Yamamoto, K.;  Nomura, R.;  Fujimoto, A.;  Higashio, N.;  Koshiishi, H.;  Imajo, S.;  Oimatsu, S.;  Tanaka, Y. -M.;  Shinohara, M.;  Shinohara, I.;  Miyoshi, Y.
收藏  |  浏览/下载:18/0  |  提交时间:2019/04/09
dipolarization  inner magnetosphere  O+ outflow  acceleration  partial ring current