933-04-0Relevant articles and documents
Photoinduced remote regioselective radical alkynylation of unactivated C-H bonds
Hu, Qu-Ping,Liu, Yong-Ze,Liu, Yu-Tao,Pan, Fei
, 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
, 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.
SMALL MOLECULE VE-PTP INHIBITORS
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, (2022/01/05)
The present disclosure relates to compounds capable of inhibiting vascular endothelial protein tyrosine phosphatase (VE-PTP). These compounds are also capable of activating Tie2 receptor-mediated signaling. The present disclosure also relates to pharmaceutically acceptable salts of said compounds, to pharmaceutical compositions comprising such compounds and/or pharmaceutically acceptable salts thereof, and to the use of such compounds, pharmaceutically acceptable salts thereof, and/or pharmaceutical compositions comprising the same in treating diseases and/or conditions mediated by VE-PTP signaling, such as those mediated by Angiopoietm/Tie2 signaling.
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
, 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 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
5-(PYRIDIN-3-YL)OXAZOLE ALLOSTERIC MODULATORS OF M4 MUSCARINIC ACETYLCHOLINE RECEPTOR
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Page/Page column 72, (2019/01/16)
Provided are 5-(pyridin-3-yl) oxazole compounds, the compositions comprising these compounds and the uses of these compositions in the potential prevention or treatment of such diseases in which M4 muscarinic acetylcholine receptors are involved.
Copper-Catalyzed Amide Radical-Directed Cyanation of Unactivated Csp3-H Bonds
Zhang, Hongwei,Zhou, Yulu,Tian, Peiyuan,Jiang, Cuiyu
, (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.
Corresponding amine nitrile and method of manufacturing thereof
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Paragraph 0138; 0139; 0140; 0149; 0150, (2018/05/07)
The invention relates to a manufacturing method of nitrile. Compared with the prior art, the manufacturing method has the characteristics of significantly reduced using amount of an ammonia source, low environmental pressure, low energy consumption, low production cost, high purity and yield of a nitrile product and the like, and nitrile with a more complex structure can be obtained. The invention also relates to a method for manufacturing corresponding amine from nitrile.
SUBSTITUTED PYRROLIDINE AND PIPERIDINE COMPOUNDS, DERIVATIVES THEREOF, AND METHODS FOR TREATING PAIN
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Page/Page column 78-79, (2009/10/22)
The present application relates to pyrrolidine, piperidine, and other nitrogen-containing heterocyclic derivatives and the use of these compounds for treating and preventing pam or inflammation. The analgesic compounds demonstrate efficacy in the treatment of neuropathic pain resulting from a variety of conditions such as diabetic neuropathy, HIV infections, and post-herpetic neuralgia.