A new efficient synthetic strategy for N-(dialkylamino)azacycle as a tetrasubstituted hydrazine derivative using sodium triacyloxyborohydride |
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| Authors: | Hideya Mizufune Hiroaki Yamamoto Minoru Nakamura Shokyo Miki |
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| Affiliation: | Chemical Development Laboratories, Pharmaceutical Production Division, Takeda Pharmaceutical Company Limited, 2-17-85 Jusohonmachi, Yodogawaku, Osaka 532-8686, Japan |
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| Abstract: | A new efficient and convergent method has been developed to construct a N-(dialkylamino)azacyclic system as a tetrasubstituted hydrazine via reductive alkylation of the corresponding hydrazone using sodium triacyloxyborohydride [NaBH(OCOR)3], which is tolerant of various substituents (e.g., phenol, conjugated olefin, amide, and thioamide) on the substrate and useful for organization of the N-aminoazacycle array. |
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| Keywords: | Sodium triacyloxyborohydride Hydrazine |
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