- Approach to 5-substituted 6,7,8,9-tetrahydro-5H-pyrido[3,2-c]azepines
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An approach to 5-substituted 6,7,8,9-tetrahydro-5H-pyrido[3,2-c]azepines via the cyclization of 1-(2-(3-azidopropyl)pyridin-3-yl)alkanones under Staudinger–aza-Wittig reaction conditions is described. The overall reaction sequence includes eight steps and allows for the preparation of gram quantities of the title products. In some cases, the formation of 5,7,8,9-tetrahydrooxepino[4,3-b]pyridine derivatives was observed.
- Subota, Andrii I.,Artamonov, Oleksiy S.,Gorlova, Alina,Volochnyuk, Dmitriy M.,Grygorenko, Oleksandr O.
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p. 1989 - 1991
(2017/04/27)
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- A simple method for the synthesis of 3-arylthieno[2,3-b]pyridines via iodine-mediated cyclization of 3-(1-arylalkenyl)-2-[(1-phenylethyl)sulfanyl] pyridines
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3-Arylthieno[2,3-b]pyridines are synthesized in a short four-step sequence from readily available 2-bromopyridines. The final and key step of the reported method involves an iodine-mediated 5-endo cyclization of 3-(1-arylalkenyl)-2- [(1-phenylethyl)sulfan
- Kobayashi, Kazuhiro,Nakamura, Daizo,Shiroyama, Yasuhiko,Fukamachi, Shuhei,Konishi, Hisatoshi
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experimental part
p. 2179 - 2183
(2009/12/31)
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- Synthesis of 1-aryl-1H-pyrrolo[2,3-b]pyridines (1-aryl-7-azaindoles) by a thermal dehydration-cyclization-dehydrogenation sequence of 2-arylamino-3-(1- hydroxyalkyl)pyridines
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1-Aryl-1H-pyrrolo[2,3-b]pyridines (1-aryl-7-azaindoles) have been prepared in reasonable yields from the corresponding 2-arylamino-3-(1-hydroxyalkyl) pyridines, on heating at ca. 250 °C, through a successive dehydration/cyclization/dehydrogenation sequenc
- Kobayashi, Kazuhiro,Fujita, Seiki,Fukamachi, Shuhei,Konishi, Hisatoshi
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experimental part
p. 2735 - 2744
(2011/04/17)
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- Synthesis of 3-substituted indazoles and benzoisoxazoles via Pd-catalyzed cyclization reactions: application to the synthesis of nigellicine
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Syntheses of 3-substituted indazoles and benzoisoxazoles were efficiently accomplished with the aid of Pd-catalyzed intramolecular carbon-nitrogen and carbon-oxygen bond formations. The catalyst system described herein allows the cyclization to proceed under very mild conditions and thus could be applied to a wide range of substrates with acid- or base-sensitive functional groups. A total synthesis for the indazole ring-containing natural product nigellicine is also described.
- Inamoto, Kiyofumi,Katsuno, Mika,Yoshino, Takashi,Arai, Yukari,Hiroya, Kou,Sakamoto, Takao
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p. 2695 - 2711
(2007/10/03)
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- TRIAZOLE DERIVATIVES AS TACHYKININ RECEPTOR ANTAGONISTS
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This application relates to a compound of Formula (I) or a pharmaceutically acceptable salt thereof, pharmaceutical compositions thereof, and its use as an inhibitor of the NK-1 subtype of tachykinin receptors, as well as a process for its preparation and intermediates therefor. (I) wherein: D is a C1-C3 alkane-diyl; R1 is phenyl, which is optionally substituted with one to three substitutents indpendently selected from the group consisting of halo, C1-C4 alkyl, C1-C4 alkoxy, cyano, difluoromethyl, trifluoromethyl, and trifluoromethoxy; R4 is a radical selected from the group consisting of: (IA), (IB), (IC), (ID), (IE), (IF), (IG), (IH)
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Page/Page column 43
(2010/02/07)
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