5763-55-3Relevant academic research and scientific papers
Photoinduced remote regioselective radical alkynylation of unactivated C-H bonds
Hu, Qu-Ping,Liu, Yong-Ze,Liu, Yu-Tao,Pan, Fei
supporting information, p. 2295 - 2298 (2022/02/25)
A method for the remote regioselective alkynylation of unactivated C(sp3)-H bonds in diverse aliphatic amides by photogenerated amidyl radicals has been developed. The site-selectivity is dominated via a 1,5-hydrogen atom transfer (HAT) process of the amide. Mild reaction conditions and high regioselectivity are demonstrated in this methodology.
Remote Regioselective Radical C-H Functionalization of Unactivated C-H Bonds in Amides: The Synthesis of gem-Difluoroalkenes
Hu, Qu-Ping,Cheng, Jing,Wang, Ying,Shi, Jie,Wang, Bi-Qin,Hu, Ping,Zhao, Ke-Qing,Pan, Fei
supporting information, p. 4457 - 4462 (2021/05/26)
The site-selective functionalization of unactivated aliphatic amines is an attractive and challenging synthetic approach. We herein report a general strategy for the remote site-selective functionalization of unactivated C(sp3)-H bonds in amides by photogenerated amidyl radicals to form gem-difluoroalkenes with trifluoromethyl-substituted alkenes. The site selectivity is controlled by a 1,5-hydrogen atom transfer (HAT) process of the amide. This photocatalyzed transformation shows both chemo- and site-selectivity, facilitating the formation of a secondary, tertiary, or quaternary carbon center.
Remote Directed Isocyanation of Unactivated C(sp3)-H Bonds: Forging Seven-Membered Cyclic Ureas Enabled by Copper Catalysis
Zhang, Hongwei,Tian, Peiyuan,Ma, Lishuang,Zhou, Yulu,Jiang, Cuiyu,Lin, Xufeng,Xiao, Xiao
supporting information, p. 997 - 1002 (2020/02/15)
Reported herein is an unprecedented copper-catalyzed site-selective ?-C(sp3)-H bonds activation of aliphatic sulfonamides for constructing the synthetically useful seven-membered N-heterocycles. A key to success is the use of in-situ-formed amide radicals, to activate the inert C(sp3)-H bond, and inexpensive TMSNCO, as a coupling reagent under mild conditions. To the best of our knowledge, this represents the first use of alkylamine derivatives as a five-membered synthon to prepare a seven-membered N-heterocycles.
Efficient preparation and application of monodisperse palladium loaded graphene oxide as a reusable and effective heterogeneous catalyst for suzuki cross-coupling reaction
Diler, Fatma,Burhan, Hakan,Genc, Hayriye,Kuyuldar, Esra,Zengin, Mustafa,Cellat, Kemal,Sen, Fatih
, (2019/11/29)
A homogeneously dispersed graphene oxide supported palladium nanomaterial (Pd?GO) has been successfully synthesized and used as a catalyst in cross-coupling reactions at room temperature. Various analytical techniques such as X-ray Diffraction (XRD), X-ray photoelectron spectroscopy (XPS), transmission electron microscopy (TEM), high-resolution transmission electron microscopy (HR-TEM) were used to characterize the monodisperse Pd?GO. Monodisperse Pd?GO nanomaterials were used for the cross-coupling reactions which brought together organic molecules with functional significance. This catalyst showed superior catalytic activity and stability for these coupling reactions. High product yields, short reaction times and mild reaction conditions, obtained by the using of developed catalysts. Importantly, the catalyst can be used at least five experiments successfully without losing its efficiency.
Copper-Catalyzed Amide Radical-Directed Cyanation of Unactivated Csp3-H Bonds
Zhang, Hongwei,Zhou, Yulu,Tian, Peiyuan,Jiang, Cuiyu
supporting information, (2019/03/19)
A method for site-selective intermolecular δ/?-Csp3-H cyanation of aliphatic sulfonamides is developed using TsCN as the cyanating reagent, catalyzed by a Cu(I)/phenanthroline complex. The mild, expeditious, and modular protocol allows efficient remote Csp3-H cyanation with good functional group tolerance and high regioselectivity. Mechanistic studies indicate that the reaction might proceed through a Cu(I)-mediated N-F bond cleavage to generate an amidyl radical, 1,5-HAT, and cyano group transfer of the resulting carbon radical with TsCN.
Efficient synthesis of unsymmetrical sulfamides from sulfamic acid salts by activation with triphenylphosphine ditriflate
Shehata, Mina F.,Short, Melanie A.,Sanders, Matthew A.,Roizen, Jennifer L.
supporting information, p. 3186 - 3194 (2019/03/13)
A general approach to prepare unsymmetrical sulfamides is described. This method relies on the activation of sulfamic acid salts with triphenylphosphine ditriflate, and subsequent trapping by a nucleophilic amine. This strategy improves access to N-octade
THF-CONTAINING SULFONAMIDE INHIBITORS OF ASPARTYL PROTEASE
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, (2008/06/13)
The present invention relates to a class of THF-containing sulfonamides which are aspartyl protease inhibitors. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention.
