- Reductive alkylation of hydrazine derivatives with α-picoline-borane and its applications to the syntheses of useful compounds related to active pharmaceutical ingredients
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An efficient method for the direct reductive alkylation of hydrazine derivatives with α-picoline-borane has been developed to synthesize a variety of N-alkylhydrazine derivatives. This method provided N,N-dialkylhydrazine derivatives and N-monoalkylhydrazine derivatives upon fine-tuning of the substrates and the reagent equivalency in a one-pot manner. The method was applied to the synthesis of active pharmaceutical ingredients of therapeutic drugs such as isocarboxazid.
- Kawase, Yasushi,Yamagishi, Takehiro,Kato, Jun-Ya,Kutsuma, Teruo,Kataoka, Tadashi,Iwakuma, Takeo,Yokomatsu, Tsutomu
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p. 455 - 464
(2014/03/21)
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- Synthesis and antibacterial activities of 1,3,4-oxadiazole derivatives containing 5-methylisoxazole moiety
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5-(5-Methylisoxazol-3-yl)-4-substituted aminomethyl-2-thio-1,3,4-oxadiazoles 3a-e and 4-acetyl-2-(5-methylisoxazol-3-yl)-5-substituted-1,3,4-oxadiazoles 5a-c have been synthesized by Mannich reaction of 5-(5-methylisoxazol-3-yl)-1,3,4-oxadiazol-2-thiol 2 with amines and cyclization of hydrazones with acetic anhydride, respectively. Moreover, 2-aryl-5-(5-methylisoxazol-3-yl)-1,3,4-oxadiazoles 6a-c have been obtained by direct condensation of 5-methylisoxazol-3-acetic acid hydrazizide with aromatic acid in the presence of POCl3. The compounds synthesized have been confirmed by their elemental analyses and spectral data. Their antibacterial activities have also been evaluated.
- Hui, Xin-Ping,Chu, Chang-Hu,Zhang, Zi-Yi,Wang, Qin,Zhang, Qi
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p. 2176 - 2179
(2007/10/03)
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