One-Pot Primary Aminomethylation of Aryl and Heteroaryl Halides with Sodium Phthalimidomethyltrifluoroborate
Norio Murai, Masayuki Miyano, Masahiro Yonaga* and Keigo Tanaka*
*Discovery Research Laboratories, Eisai Co., Ltd., 5-1-3 Tokodai, Tsukuba, Ibaraki 300-2635, Japan, Email: k6-tanakahhc.eisai.co.jp, m-yonagahhc.eisai.co.jp
N. Murai, M. Miyano, M. Yonaga, K. Tanaka, Org. Lett., 2012, 14, 2818-2821.
DOI: 10.1021/ol301037s
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Abstract
Suzuki-Miyaura cross-coupling enables a one-pot primary aminomethylation of aryl halides, triflates, mesylates, and tosylates via coupling with sodium phthalimidomethyltrifluoroborate followed by deamidation with ethylenediamine.
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Key Words
Suzuki Coupling, benzylamines, phthalimides
ID: J54-Y2012-1750