- Expanding the Protecting Group Scope for the Carbonyl Olefin Metathesis Approach to 2,5-Dihydropyrroles
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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
- Catti, Lorenzo,Huck, Fabian,Reber, Gian Lino,Tiefenbacher, Konrad
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p. 419 - 428
(2022/01/03)
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- NEUROKININ B ANTAGONIST FOR USE IN INHIBITING FOLLICLE DEVELOPMENT
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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,
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Paragraph 0052; 0053
(2016/09/26)
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- 2-Methylquinoline promoted oxidative ring-opening of N-sulfonyl aziridines with DMSO: facile synthesis of α-amino aryl ketones
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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.
- Zhang, Xianhui,Li, Shuai-Shuai,Wang, Liang,Xu, Lubin,Xiao, Jian,Liu, Zhen-Jiang
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p. 8073 - 8077
(2016/11/19)
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- Rhodium-Catalyzed Synthesis of 2,5-Epoxybenzo[f][1,4]oxazepines by Tandem Reaction of 1-Sulfonyl-1,2,3-triazoles and Salicylaldehydes
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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.
- Shi, Yinping,Yu, Xing,Li, Chuan-Ying
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p. 6429 - 6433
(2015/10/19)
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- A NK3 RECEPTOR ANTAGONIST COMPOUND (NK3RA) FOR USE IN A METHOD FOR THE TREATMENT OF POLYCYSTIC OVARY SYNDROME (PCOS)
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A method for treating polycystic ovarian syndrome and related conditions with a compound (I): or a pharmaceutically acceptable salt thereof.
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Page/Page column 25; 26
(2014/11/11)
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- Base-catalyzed N -N bond cleavage of hydrazones: Synthesis of α-amino ketones
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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.
- Tang, Hai-Tao,Zhou, Yun-Bing,Zhu, Yu,Sun, Hong-Chao,Lin, Min,Zhan, Zhuang-Ping
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supporting information
p. 1278 - 1281
(2014/05/06)
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- Synthesis of α-amino ketones from terminal alkynes via rhodium-catalyzed denitrogenative hydration of N -sulfonyl-1,2,3-triazoles
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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.
- Miura, Tomoya,Biyajima, Tsuneaki,Fujii, Tetsuji,Murakami, Masahiro
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p. 194 - 196
(2012/03/07)
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- Alkylsulphonamide Quinolines
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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
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Page/Page column 8
(2009/01/20)
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- Novel three-component synthesis and antiproliferative properties of diversely functionalized pyrrolines
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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
- Magedov, Igor V.,Luchetti, Giovanni,Evdokimov, Nikolai M.,Manpadi, Madhuri,Steelant, Wim F.A.,Van slambrouck, Severine,Tongwa, Paul,Antipin, Mikhail Yu.,Kornienko, Alexander
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p. 1392 - 1396
(2008/12/23)
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- ALKYLSULPHONAMIDE QUINOLINES
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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
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Page/Page column 16
(2008/06/13)
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- AMIDE SUBSTITUTED QUINOLINES
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Compounds of Formula I [Chemical formula should be inserted here. Please see paper copy] wherein R1, A, R2, n, R3, m, R4, R5 and q are as described in the specification, pharmaceutically-acceptable sa
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Page/Page column 25
(2008/06/13)
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- M-STAGE KINESIN INHIBITOR
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A mitotic kinesin Eg5 inhibitor which comprises a thiadiazoline derivative represented by the general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient: [wherein R1 represents a hydrogen atom and the like, R2 represents a hydrogen atom, -C(=W)R6 (wherein W represents an oxygen atom or a sulfur atom, and R6 represents substituted or unsubstituted lower alkyl and the like) and the like, R3 represents -C(=Z)R19 (wherein Z represents an oxygen atom or a sulfur atom, and R19 represents substituted or unsubstituted lower alkyl and the like) and the like, R4 represents substituted or unsubstituted lower alkyl and the like, and R5 represents substituted or unsubstituted aryl and the like] and the like are provided.
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Page/Page column 80
(2010/11/08)
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- THIADIAZOLINE DERIVATIVE
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(wherein R1 and R4 are the same or different and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted lower alkynyl, substituted or unsubstituted lower alkenyl, or the like; R5 represents a substituted or unsubstituted heterocyclic group, substituted or unsubstituted aryl, or the like; R2 represents -C(-W)R6 or the like; R3 represents a hydrogen atom, -C(=WA)R6A, or the like) Antitumor agents which comprises a thiadiazoline derivative represented by the aforementioned general formula (I) or a pharmacologically acceptable salt thereof as an active ingredient are provided.
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