53088-68-9Relevant articles and documents
2-azabicyclo [3.2.0] compound as well as synthesis method and application
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Paragraph 0107-0110; 0118; 0129-0131; 0134, (2021/07/17)
The invention discloses a 2-azabicyclo [3.2.0] compound as well as a synthesis method and an application. The 2-azabicyclo [3.2.0] compound comprises a compound with a structure as shown in a formula I and pharmaceutically acceptable salts thereof, wherein R is a substituted or unsubstituted benzene ring, a C1-8 aliphatic group or trifluoromethyl, R1 and R2 are respectively a substituted or unsubstituted benzene ring, a hydrogen atom or a C1-8 aliphatic group, R3 is a substituted or unsubstituted benzene ring, a hydrogen atom, a C1-8 aliphatic group or a heterocyclic substituent, R4 is a heterocyclic substituent or a substituted or unsubstituted benzene ring, R5 is a C1-8 fatty group, a benzyl group or -COOR6, and R6 is a C1-4 fatty group or a benzyl group. The invention belongs to the technical field of pharmaceutical chemicals, and after the prepared 2-azabicyclo [3.2.0] compound acts on an animal body, anti-sedation and anti-hypnosis effects can be achieved by adjusting the intracerebral level of histamine.
Pd-Catalyzed Decarboxylative Olefination: Stereoselective Synthesis of Polysubstituted Butadienes and Macrocyclic P-glycoprotein Inhibitors
Chen, Xiangyang,Hao, Jiping,Houk, K. N.,Li, Yingzi,Lou, Liguang,Quan, Haitian,Song, Bichao,Wang, Lu,Xia, Yuanzhi,Xie, Peipei,Xu, Zhongliang,Yang, Weibo
supporting information, p. 9982 - 9992 (2020/06/27)
The efficient and stereoselective synthesis of polysubstituted butadienes, especially the multifunctional butadienes, represents a great challenge in organic synthesis. Herein, we wish to report a distinctive Pd(0) carbene-initiated decarboxylative olefination approach that enables the direct coupling of diazo esters with vinylethylene carbonates (VECs), vinyl oxazolidinones, or vinyl benzoxazinones to afford alcohol-, amine-, or aniline-containing 1,3-dienes in moderate to high yields and with excellent stereoselectivity. This protocol features operational simplicity, mild reaction conditions, a broad substrate scope, and gram-scalability. Notably, a structurally unique allylic Pd(II) intermediate was isolated and characterized. DFT calculation and control experiments demonstrated that a rare Pd(0) carbene intermediate could be involved in this reaction. Moreover, the polysubstituted butadienes as novel building blocks were unprecedentedly assembled into macrocycles, which efficiently inhibited the P-glycoprotein and dramatically reversed multidrug resistance in cancer cells by 190-fold.
Enantioselective Construction of Quaternary All-Carbon Centers via Copper-Catalyzed Arylation of Tertiary Carbon-Centered Radicals
Wu, Lianqian,Wang, Fei,Chen, Pinhong,Liu, Guosheng
supporting information, p. 1887 - 1892 (2019/02/05)
An enantioselective copper-catalyzed arylation of tertiary carbon-centered radicals, leading to quaternary all-carbon stereocenters, has been developed herein. The tertiary carbon-centered radicals, including both benzylic and nonbenzylic radicals, were produced by the addition of trifluoromethyl radical to α-substituted acrylamides, and subsequently captured by chiral aryl copper(II) species to give C-Ar bonds with excellent enantioselectivity. Importantly, an acylamidyl (CONHAr) group adjacent to the tertiary carbon radical is essential for the asymmetric radical coupling. The reaction itself features broad substrate scope, excellent functional group compatibility and mild conditions.
