56062-81-8Relevant academic research and scientific papers
Expanding the Protecting Group Scope for the Carbonyl Olefin Metathesis Approach to 2,5-Dihydropyrroles
Catti, Lorenzo,Huck, Fabian,Reber, Gian Lino,Tiefenbacher, Konrad
, p. 419 - 428 (2022/01/03)
Chiral pyrrolidine derivatives are important building blocks for natural product synthesis. Carbonyl olefin metathesis has recently emerged as a powerful tool for the construction of such building blocks from chiral amino acid derivatives. Here, we demons
2-Methylquinoline promoted oxidative ring-opening of N-sulfonyl aziridines with DMSO: facile synthesis of α-amino aryl ketones
Zhang, Xianhui,Li, Shuai-Shuai,Wang, Liang,Xu, Lubin,Xiao, Jian,Liu, Zhen-Jiang
, p. 8073 - 8077 (2016/11/19)
2-Methylquinoline promoted room-temperature oxidative ring-opening of N-sulfonyl aziridines with DMSO has been developed, providing a mild and convenient method for the synthesis of a variety of different N-sulfonyl protected α-amino aryl ketones. The employment of 2-methylquinoline was crucial for the success of this mild transformation and good to excellent yields could be achieved.
NEUROKININ B ANTAGONIST FOR USE IN INHIBITING FOLLICLE DEVELOPMENT
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Paragraph 0052; 0053, (2016/09/26)
This invention relates to use of compounds in female health applications,for example as a contraceptive. In particular the invention relates to the use of compounds targeting tachykinin receptors, in particular neurokinin B receptors (NK3R). For example,
Rhodium-Catalyzed Synthesis of 2,5-Epoxybenzo[f][1,4]oxazepines by Tandem Reaction of 1-Sulfonyl-1,2,3-triazoles and Salicylaldehydes
Shi, Yinping,Yu, Xing,Li, Chuan-Ying
, p. 6429 - 6433 (2015/10/19)
Readily available 1-sulfonyl-1,2,3-triazoles were converted into α-imino carbenes in the presence of catalytic amounts of rhodium(II) salts. The carbenes underwent a tandem reaction with salicylaldehydes to provide a series of functionalized 2,5-epoxybenzo[f][1,4]oxazepines in high yields. A novel protocol for the synthesis of 2,5-epoxybenzo[f][1,4]oxazepines is developed. The complicated ring system can be constructed from readily available N-sulfonyl-1,2,3-triazoles and salicylaldehyde derivatives in a one-pot procedure. Many valuable functional groups are well tolerated in this transformation. [Rh2(piv)4] = dirhodium(II) tetrapivalate.
Base-catalyzed N -N bond cleavage of hydrazones: Synthesis of α-amino ketones
Tang, Hai-Tao,Zhou, Yun-Bing,Zhu, Yu,Sun, Hong-Chao,Lin, Min,Zhan, Zhuang-Ping
supporting information, p. 1278 - 1281 (2014/05/06)
An efficient Cs2CO3-promoted synthesis of α-amino ketones using hydrazines, aldehydes, and α-haloketones as starting materials through a cascade condensation/nucleophilic substitution/N -N bond cleavage route is developed. The carbonyl group plays a key role in this novel N -N bond cleavage process. Breaking good: A novel method of base-catalyzed N -N bond cleavage of hydrazones has been discovered. A variety of α-amino ketones was synthesized using hydrazines, α-haloketones, and benzaldehyde as starting materials through a cascade condensation/ nucleophilic substitution/N -N bond cleavage sequence.
A NK3 RECEPTOR ANTAGONIST COMPOUND (NK3RA) FOR USE IN A METHOD FOR THE TREATMENT OF POLYCYSTIC OVARY SYNDROME (PCOS)
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Page/Page column 25; 26, (2014/11/11)
A method for treating polycystic ovarian syndrome and related conditions with a compound (I): or a pharmaceutically acceptable salt thereof.
Synthesis of α-amino ketones from terminal alkynes via rhodium-catalyzed denitrogenative hydration of N -sulfonyl-1,2,3-triazoles
Miura, Tomoya,Biyajima, Tsuneaki,Fujii, Tetsuji,Murakami, Masahiro
, p. 194 - 196 (2012/03/07)
N-Sulfonyl-1,2,3-triazoles react with water in the presence of a rhodium catalyst to produce α-amino ketones in high yield. An intermediary α-imino rhodium(II) carbenoid undergoes insertion into the O-H bond of water. This transformation formally achieves 1,2-aminohydroxylation of terminal alkynes in a regioselective fashion when combined with the copper(I)-catalyzed 1,3-dipolar cycloaddition with N-sulfonyl azides.
Alkylsulphonamide Quinolines
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Page/Page column 8, (2009/01/20)
Compounds of Formula I wherein R1, A, R2, R3, R4, R5, R8, n, m, q and r are as described in the specification, pharmaceutically-acceptable salts, methods of making, pharmaceutical compositi
Novel three-component synthesis and antiproliferative properties of diversely functionalized pyrrolines
Magedov, Igor V.,Luchetti, Giovanni,Evdokimov, Nikolai M.,Manpadi, Madhuri,Steelant, Wim F.A.,Van slambrouck, Severine,Tongwa, Paul,Antipin, Mikhail Yu.,Kornienko, Alexander
, p. 1392 - 1396 (2008/12/23)
Diversely substituted 2-pyrrolines have been prepared by a novel multicomponent process involving a reaction of various N-(aryl- and alkylsulfonamido)-acetophenones with aldehydes and malononitrile. While the reaction is highly regioselective, it is not s
ALKYLSULPHONAMIDE QUINOLINES
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Page/Page column 16, (2008/06/13)
Compounds of Formula (1), pharmaceutically-acceptable salts, methods of making them, pharmaceutical compositions containing them and methods for their use. The compounds are neurokinin- 3 (NK-3) receptor antagonists and are used in the treatment of diseas
