Preparation of 4-heteroaryl-4-cyanopiperidines via SNAr substitution reactions |
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| Authors: | Ronald K Chang Scott D Kuduk |
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| Institution: | Department of Medicinal Chemistry, Merck Research Laboratories, WP 14-3, Sumneytown Pike, PO Box 4, West Point, PA 19486, USA |
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| Abstract: | The scope and limitations of SNAr substitution reactions of metalated 4-cyanopiperidines with heterocyclic halides were explored. These facile reactions provide rapid access to a wide range of 4-heteroaryl-4-cyanopiperidines and have resulted in improved yields, faster reaction times, and lower temperatures than previously published synthetic methods. |
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