- Synthesis of C4-Aminated Indoles via a Catellani and Retro-Diels-Alder Strategy
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Highly functionalized 4-aminoindoles were synthesized via the three-component cross-coupling of o-iodoaniline, N-benzoyloxyamines, and norbornadiene. The Catellani and retro-Diels-Alder strategy was used in this domino process. o-Iodoaniline, with electron-donating and sterically hindered protecting groups, made the reaction selective toward o-C-H amination. On the basis of density functional theory calculations, the intramolecular Buchwald coupling of this reaction underwent a dearomatization and a 1,3-palladium migration process. The reasons for the control of the chemical selectivity by the protecting groups are given. Moreover, synthetic applications toward 4-piperazinylindole and a GOT1 inhibitor were realized.
- Zhang, Bo-Sheng,Li, Yuke,Zhang, Zhe,An, Yang,Wen, Yu-Hua,Gou, Xue-Ya,Quan, Si-Qi,Wang, Xin-Gang,Liang, Yong-Min
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p. 9731 - 9738
(2019/06/24)
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- Synthesis of C4-Aminated Indoles via a Catellani and Retro-Diels-Alder Strategy
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Highly functionalized 4-aminoindoles were synthesized via the three-component cross-coupling of o-iodoaniline, N-benzoyloxyamines, and norbornadiene. The Catellani and retro-Diels-Alder strategy was used in this domino process. o-Iodoaniline, with electron-donating and sterically hindered protecting groups, made the reaction selective toward o-C-H amination. On the basis of density functional theory calculations, the intramolecular Buchwald coupling of this reaction underwent a dearomatization and a 1,3-palladium migration process. The reasons for the control of the chemical selectivity by the protecting groups are given. Moreover, synthetic applications toward 4-piperazinylindole and a GOT1 inhibitor were realized.
- Zhang, Bo-Sheng,Li, Yuke,Zhang, Zhe,An, Yang,Wen, Yu-Hua,Gou, Xue-Ya,Quan, Si-Qi,Wang, Xin-Gang,Liang, Yong-Min
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- AROMATIC HETEROCYCLIC DERIVATIVES AND PHARMACEUTICAL APPLICATIONS THEREOF
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Provided herein are aromatic heterocyclic derivatives or a stereoisomer, a tautomer, an N-oxide, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof used for treating Alzheimer's disease. Also provided herein are pharmaceutica
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Paragraph 00190
(2016/01/25)
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- Indoline derivative and application of indoline derivative in medicine
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The invention discloses an indoline derivative, application of the indoline derivative in medicine, and stereisomer, tautomer, nitric oxide, solvate, metabolite, pharmacy-acceptable salt or other prodrugs of the indoline derivative. The invention further relates to a medicine composition with the compound and application of the compound or the medicine composition in preparation of medicine for treating diseases related to 5-HT6 receptors especially the Alzheimer's disease.
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Paragraph 0179; 0180; 0181; 0182
(2016/10/09)
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- Deprotection of N-BOC compounds
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Organic compounds having nitrogen atoms protected with t-butoxycarbonyl are effectively deprotected by heating in a fluorinated alcohol solution.
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Page/Page column 5-6
(2009/08/18)
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- Deprotection of N-BOC compounds
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Organic compounds having nitrogen atoms protected with t-butoxycarbonyl are effectively deprotected by heating in a fluorinated alcohol solution.
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Page/Page column 9
(2009/07/10)
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- 4' SUBSTITUTED COMPOUNDS HAVING 5-HT6 RECEPTOR AFFINITY
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The present disclosure provides compounds having affinity for the 5-HT6 receptor which are of the formula (I): wherein R1, R2, R5, R6, B, D, E, G, Q, x and n are as defined herein. The disclosure also relates to methods of preparing such compounds, compositions containing such compounds, and methods of use thereof.
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Page/Page column 19-20
(2009/01/24)
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- Novel practical deprotection of N-Boc compounds using fluorinated alcohols
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The thermolytic deprotection of N-Boc compounds was accomplished using TFE (2,2,2-trifluoroethanol) or HFIP (hexafluoroisopropanol) as solvents. Even though the cleavage of the t-butylcarbamate (Boc) group can be achieved at solvent reflux temperature, the deprotection process was significantly accelerated under microwave-assisted conditions. The practicality of this methodology was demonstrated on alkyl, aryl, and heteroaromatic N-Boc-amines. Copyright Taylor & Francis Group, LLC.
- Choy, Jason,Jaime-Figueroa, Saul,Jiang, Laurence,Wagner, Paul
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p. 3840 - 3853
(2008/12/23)
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- Diarylalkylpiperazines active on the lower urinary tract
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Disclosed herein are novel compounds and methods for the treatment of disorders of the lower urinary tract. The novel compounds are diarylalkylpiperazine derivatives. The methods comprise the administration of the novel compounds of the invention, and other compounds that bind to 5HT1A receptors, for treating disorders of the lower urinary tract.
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Page/Page column 22
(2010/02/11)
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- 4,5,6 and 7-indole and indoline derivatitives, their preparation and use
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A substituted 4-, 5-, 6-, and 7-indole derivative of Formula (I) wherein A is a group having formula (IIA), (IIB), (IIC) wherein X, U, Y, R3to R12, Z, W, n and m are as defined above. The compounds are potent serotonin reuptake inhib
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- Piperazine derivatives
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Compounds are disclosed which have the general formula A: STR1 where Ra and Rb are each hydrogen or methyl and Rc is hydrogen, halo or C1-4 alkyl optionally in the form of a pharmaceutically acceptable acid addi
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