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One-Pot Transannulation of N-Sulfonyl-1,2,3-triazoles to Dihydro-β-carbolines and Dihydroisoquinolines via Rhodium-Catalyzed C-H Insertion-cum-Base-Mediated Aza-Michael Reaction
Shanmugam Rajasekar,
Published in American Chemical Society
2019
PMID: 31132245
Volume: 84
   
Issue: 12
Pages: 7747 - 7761
Abstract
Efficient one-pot rhodium-catalyzed and base-mediated transannulation of N-sulfonyl-1,2,3-triazoles with a Michael acceptor-tethered indole derivative have been achieved for the synthesis of dihydro-β-carboline derivatives. The present methodology involves an efficient rhodium-catalyzed insertion of azavinyl carbenes to C3-H bond of indole followed by base-mediated intramolecular aza-Michael reaction. The optimized conditions tolerate various functional groups and afford the diverse dihydro-β-carbolines in good yield. The method was successfully extended to the synthesis of dihydroisoquinolines employing Michael acceptor-tethered aniline derivatives. The potential of the developed method was demonstrated through one-pot cascade synthesis of dihydro-β-carbolines from alkyne and their conversion to vital carboline derivatives. © 2019 American Chemical Society.
About the journal
JournalData powered by TypesetJournal of Organic Chemistry
PublisherData powered by TypesetAmerican Chemical Society
ISSN00223263
Open AccessNo
Concepts (57)
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    Addition reactions
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    Aniline
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    Polycyclic aromatic hydrocarbons
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    Pyridine
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    ANILINE DERIVATIVES
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    AZA-MICHAEL REACTION
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    CARBOLINE DERIVATIVES
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    DIHYDROISOQUINOLINES
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    Indole derivatives
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    Michael acceptors
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    Optimized conditions
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    Rhodium-catalyzed
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    Catalysis
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    1,2,3 TRIAZOLE DERIVATIVE
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    2 [4 (4 FLUOROPHENYL) 9 METHYL 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]ACETATE
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    BETA CARBOLINE DERIVATIVE
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    DIHYDROISOQUINOLINE DERIVATIVE
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    ETHYL 2 (6 METHOXY 9 METHYL 4 PHENYL 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 ACETATE
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    ETHYL 2 (9 ALLYL 4 PHENYL 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL)ACETATE
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    ETHYL 2 (9 BENZYL 4 PHENYL 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL)ACETATE
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    ETHYL 2 (9 ETHYL 4 PHENYL 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL)ACETATE
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    ETHYL 2 (9 ETHYL 4,6 DIPHENYL 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL)ACETATE
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    ETHYL 2 (9 METHYL 4 PHENYL 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL)ACETATE
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    ETHYL 2 [4 (3 FLUOROPHENYL) 9 METHYL 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]ACETATE
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    ETHYL 2 [4 (4 ACETYLPHENYL) 9 METHYL 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]ACETATE
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    ETHYL 2 [4 (4 BROMOPHENYL) 9 METHYL 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]ACETATE
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    ETHYL 2 [4 (4 CHLOROPHENYL) 9 METHYL 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]ACETATE
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    ETHYL 2 [4 (4 CYANOPHENYL) 9 METHYL 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]ACETATE
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    ETHYL 2 [4 (4 METHOXYPHENYL) 9 METHYL 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]ACETATE
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    ETHYL 2 [4 [4 (TERT BUTYL)PHENYL] 9 METHYL 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]ACETATE
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    ETHYL 2 [9 METHYL 2 (METHYLSULFONYL) 4 PHENYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]ACETATE
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    ETHYL 2 [9 METHYL 2 TOSYL 4 [3 (TRIFLUOROMETHYL)PHENYL] 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]ACETATE
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    ETHYL 2 [9 METHYL 4 (4 NITROPHENYL) 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]ACETATE
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    ETHYL 2 [9 METHYL 4 (4 OLYL) 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]ACETATE
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    ETHYL 2 [9 METHYL 4 (NAPHTHALEN 1 YL) 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]ACETATE
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    ETHYL 2 [9 METHYL 4 (THIOPHEN 3 YL) 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]ACETATE
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    ETHYL 2 [9 METHYL 4 PHENYL 2 (PHENYLSULFONYL) 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]ACETATE
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    Isoquinoline derivative
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    METHYL 2 (9 METHYL 4 PHENYL 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL)ACETATE
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    METHYL 4 [1 (2 ETHOXY 2 OXOETHYL) 9 METHYL 2 TOSYL 2,9 DIHYDRO 1H PYRIDO[3,4 B]INDOL 1 YL]ACETATE
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    N SULFONYL 1,2,3 TRIAZOLE DERIVATIVE
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    Rhodium
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    Unclassified drug
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    Unindexed drug
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    Aromatization
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    Article
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    Crystal structure
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    Decarboxylation
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    Drug structure
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    Drug synthesis
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    Electron transport
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    Isomer
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    Mannich reaction
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    Michael addition
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    One pot synthesis
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    Reaction temperature
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    X ray analysis