- Synthesis of new substituted 2-(trimethylstannyl)indoles
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Synthesis of the previously unreported 2-(trimethylstannyl)indole derivatives, 5-bromo-1-(tert-butoxycarbonyl)-2-(trimethylstannyl)-1H-indole, 6-bromo-1-(tert-butoxycarbonyl)-2-(trimethylstannyl)-1H-indole, 1-(tert-butoxycarbonyl)-2-(trimethylstannyl)-1H-indole-5-carbonitrile, 1-(tert-butoxycarbonyl)-2-(trimethylstannyl)-1H-indole-6-carbonitrile and 1-(tert-butoxycarbonyl)-2-(trimethylstannyl)-1H-pyrrolo[2,3-b] pyridine-6-carbonitrile, is described. Georg Thieme Verlag Stuttgart.
- Kumar, Arvind,Say, Martial,Boykin, David W.
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Read Online
- Synthetic method of 6-chloro-7-azaindole
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The invention discloses a synthetic method of 6-chloro-7-azaindole, belonging to the field of chemical synthesis. 7-azaindole is taken as a raw material, and the 6-chloro-7-azaindole is synthesized by three actions of N-oxidation, chlorination and hydrolysis. The process route is optimized, and the yield is improved by 70% or more, and is improved by 7% compared with the prior art. The improved synthetic route is simple to operate and feasible, the economic benefits are effectively improved, and large-scale industrial promotion is facilitated.
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Paragraph 0041; 0042; 0043; 0044; 0045
(2017/01/02)
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- NEW CRTH2 ANTAGONISTS
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The present invention relates to compounds of formula (I), to the process for preparing such compounds and to their use in the treatment of a pathological condition or disease susceptible to amelioration by CRTh2 antagonist activity.
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Page/Page column 137
(2013/03/26)
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- ANTICANCER AGENT
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An anticancer agent comprising a compound represented by the formula (I) [R1 represents hydrogen atom, hydroxyl group, a C1-6alkoxy group and the like; R2 and R3 represents hydrogen atom, a halogen atom, a C1-6alkyl group and the like; R4 represents hydrogen atom, a C1-6alkyl group, a C1-6alkylsulfonyl group and the like; R5 represents hydrogen atom or a substituent; .... represents a single bond or a double bond; R6 and R7 represents hydrogen atom, a C1-6alkyl group and the like; R8 represents hydrogen atom, a C1-6alkyl group and the like; A represents -O-, -S-, or - CH2-; D represents -C= or -N=; X represents methylene group, -O-, or -CO-; Q represents -N= or -C(R8)=; and Y represents a heterocyclic group or amino group], which shows a superior inhibitory activity against pim-1 kinase.
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Paragraph 0277
(2013/03/26)
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- Scaffold-hopping strategy: Synthesis and biological evaluation of 5,6-fused bicyclic heteroaromatics to identify orally bioavailable anticancer agents
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Utilizing scaffold-hopping drug-design strategy, we sought to identify a backup drug candidate for BPR0L075 (1), an indole-based anticancer agent. For this purpose, 5,6-fused bicyclic heteroaromatic scaffolds were designed and synthesized through shufflin
- Tung, Yen-Shih,Coumar, Mohane Selvaraj,Wu, Yu-Shan,Shiao, Hui-Yi,Chang, Jang-Yang,Liou, Jing-Ping,Shukla, Paritosh,Chang, Chun-Wei,Chang, Chi-Yen,Kuo, Ching-Chuan,Yeh, Teng-Kuang,Lin, Chin-Yu,Wu, Jian-Sung,Wu, Su-Ying,Liao, Chun-Chen,Hsieh, Hsing-Pang
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scheme or table
p. 3076 - 3080
(2011/06/25)
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- BICYCLIC PYRIDINES AND ANALOGS AS SIRTUIN MODULATORS
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Provided herein are novel sirtuin-modulating compounds and methods of use thereof. The sirtuin-modulating compounds may be used for increasing the lifespan of a cell, and treating and/or preventing a wide variety of diseases and disorders including, for example, diseases or disorders related to aging or stress, diabetes, obesity, neurodegenerative diseases, cardiovascular disease, blood clotting disorders, inflammation, cancer, and/or flushing as well as diseases or disorders that would benefit from increased mitochondrial activity. Also provided are compositions comprising a sirtuin-modulating compound in combination with another therapeutic agent.
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Page/Page column 140-141
(2011/06/16)
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- 7-AZAINDOLE DERIVATIVES AS COX2 INHIBITORS
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Compounds of formula (I) or pharmaceutically acceptable salts thereof are potent and selective inhibitors of COX-2 and are of use in the treatment of the pain, fever and inflammation of a variety of conditions and diseases.
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Page/Page column 19-20
(2010/02/11)
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- Regioselective functionalization of 1H-pyrrolo[2,3-b]pyridine via its N-oxide
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Selective functionalization of 1H-pyrrolo[2,3-b]pyridine (7-azaindole) at the 6-position was achieved by Reissert-Henze type reaction. Thus, halogeno (Cl, Br, I), cyano and thiocyanato groups were directly introduced to the pyridine ring of 7-azaindole.
- Minakata,Komatsu,Ohshiro
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p. 661 - 663
(2007/10/02)
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