Catalytic Ullmann-Type N-Arylation to Access Medicinally Important SuFEx-able Pyrazolo[1,5- a]Quinoxalinones [0.03%]
用于药物研究的含SuFEx官能团吡唑并[1,5-a]奎 啉酮衍生物的Ullmann型N-芳基化反应
Bipin Khanal,Kanokwan Jaithum,Mark Aldren M Feliciano et al.
Bipin Khanal et al.
Pyrazole-fused quinoxalines provide an attractive structural motif for medicinal chemistry and have inspired the development of novel synthetic methods. This work details a concise methodology for the synthesis of a new class of pyrazolo[1,...
PRODUCTION OF 11C-LABELED AMIDES VIA "IN-LOOP" 11C-CARBONYLATION [0.03%]
利用“回路法”11C-羰基化合成11C标记的酰胺类化合物
Tanpreet Kaur,Xia Shao,Allen F Brooks et al.
Tanpreet Kaur et al.
The carbon-11 (11C) labeling of benzamides holds great promise in the development of PET radiotracers given the prevalence of benzamides in bioactive molecules. This work establishes an improved automated route to carbon-11 labeled primary ...
One-Pot Synthesis of 2-Substituted Indoles and 7-Azaindoles via Sequential Alkynylation and Cyclization of 2-Iodo- N-mesylarylamines and Alkynes in the Presence of Cu2O [0.03%]
Cu2O存在下2-Mesylarylamines和炔烃的串联偶联环化反应合成2-取代吲哚和7-氨基吲哚的一锅法研究
Ahmed R Ali,Longqin Hu
Ahmed R Ali
A one-pot process was developed to synthesize in moderate to high yield a series of 2-substituted indoles and 7-azaindoles starting from 2-iodo-N-mesylarylamines and terminal alkynes in the presence of Cu2O in DMF at 90-120 °C. Without iso...
Joshua R Turek-Herman,Mike Rosenberger,Todd K Hyster
Joshua R Turek-Herman
Quaternary carbons are useful motifs in chemical synthesis but can be challenging to prepare using many chemical methods. Here, we report a stereoselective synthesis of β-quaternary lactams using flavin-dependent 'ene'-reductases via a 5-e...
San Khong,Telugu Venkatesh,Ohyun Kwon
San Khong
This Minireview provides insight into the early history of nucleophilic phosphinocatalysis. The concepts of 1,4-addition of a tertiary phosphine to an α,β-enone and of equilibrium between the resulting phosphonium zwitterion and phosphoni...
Triazolyl Dibenzo[ a,c]phenazines Stabilize Telomeric G-quadruplex and Inhibit Telomerase [0.03%]
三唑二苯并〔a，c〕菲嗪类化合物稳定端粒G-四聚体和抑制端粒酶活性
Sarmistha Pal,Khushnood Fatma,Velayutham Ravichandiran et al.
Sarmistha Pal et al.
We herein report the synthesis and biophysical evaluation of triazolyl dibenzo[a,c]phenazine derivatives as a novel class of G-quadruplex ligands. The aromatic core facilitates π-π interaction and the flexible, protonatable side chains in...
Ajay L Chandgude,Alexander Dömling
Ajay L Chandgude
A TiCl4-mediated reaction for the direct amination of α-hydroxy amides has been developed. This simple, general, additive/base/ligand-free reaction is mediated by economical TiCl4. The reaction runs under mild conditions. This highly effic...
Fenfen Xiao,Wu Liu,Yunxia Wang et al.
Fenfen Xiao et al.
Photogenic: The synthesis of linderaspirone A has been accomplished in only three steps by a Darzens cyclopentenedione synthesis and dioxygen-assisted photochemical dimerization. Moreover, the thermal isomerization of linderaspirone A into ...
A Redox Auxiliary Strategy for Pyrrolidine Synthesis via Photocatalytic [3+2] Cycloaddition [0.03%]
基于光催化[3+2]环加成的吡咯烷合成的氧化还原辅助策略
Adrian G Amador,Evan M Sherbrook,Tehshik P Yoon
Adrian G Amador
Cycloaddition reactions can be used to efficiently assemble pyrrolidine rings that are significant in a variety of chemical and biological applications. We have developed a method for the formal cycloaddition of cyclopropyl ketones with hyd...
Nature Inspired Molecular Design: Stereoselective Synthesis of Bicyclic and Polycyclic Ethers for Potent HIV-1 Protease Inhibitors [0.03%]
受自然启发的分子设计：合成手性双环及多环醚类高效HIV-1蛋白酶抑制剂
Arun K Ghosh,Margherita Brindisi
Arun K Ghosh
We have developed a conceptually new generation of non-peptidic HIV-1 protease inhibitors incorporating novel structural templates inspired by nature. This has resulted in protease inhibitors with exceptional potency and excellent pharmacol...