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The synthesis of low molecular weight pyrrolo[2,3-c]pyridine-7-one scaffold |
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| Authors: | Maxim A Nechayev Nikolay Yu Gorobets Alexander V Borisov Sergiy M Kovalenko Andrey A Tolmachev |
| Institution: | 1. National University of Pharmacy, Pushkinska Str. 53, Kharkiv, 61002, Ukraine 2. Laboratory for Physicochemical Processes, SSI ??Institute for SingleCrystals?? of NAS of Ukraine, Lenina Ave 60, Kharkiv, 61001, Ukraine 3. Enamine Ltd., Alexandra Matrosova Street, 23, Kiev, 01103, Ukraine |
| Abstract: | A facile method for the synthesis of substituted pyrrolo2,3-c]pyridine-7-ones is developed that applies an acid-promoted intramolecular cyclization of 2-pyrrolecarboxylic acid amidoacetals as key step. The synthesis is easily scaled up to 1.5?mol quantity with no yield decrease. The alkylation/arylation reaction of the pyrrolo2,3-c]pyridine-7-ones proceeds regioselectively giving N6-substituted derivatives. |
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