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A highly effective synthesis of 2-alkynyl-7-azaindoles: Pd/C-mediated alkynylation of heteroaryl halides in water |
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| Authors: | Mohosin Layek Vikas Gajare Aminul Islam Manojit Pal |
| Affiliation: | a Custom Pharmaceuticals Services, Dr. Reddy's Laboratories Ltd, Bollaram Road, Miyapur, Hyderabad 500049, Andhra Pradesh, India b Chemistry Division, Institute of Science and Technology, JNT University, Kukatpally, Hyderabad 500072, Andhra Pradesh, India c New Drug Discovery, R&D Center, Matrix Laboratories Ltd, Anrich Industrial Estate, Bollaram, Jinnaram Mandal, Medak District, Jinnaram Mandal 502 325, Andhra Pradesh, India |
| Abstract: | The reaction of 4-chloro-2-iodo-7-azaindole with terminal alkynes was investigated using 10% Pd/C-PPh3-CuI as a catalyst system in water. This study afforded a new, mild and selective process for the preparation of 2-alkynyl-4-chloro-7-azaindole in good yields via C-C bond forming reaction. The resulting chloro derivative can be functionalized further via another Pd-mediated C-C bond forming reaction with arylboronic acid. |
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