An efficient route to N-alkylated 3,4-dihydroisoquinolinones with substituents at the 3-position |
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| Authors: | Aoi Tazawa Junki Ando Kohei Ishizawa Isao Azumaya Hidemasa Hikawa Minoru Tanaka |
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| Institution: | Sohyaku Innovative Research Division, Mitsubishi Tanabe Pharma Corporation, 1000 Kamoshida-cho, Aoba-ku, Yokohama-shi Kanagawa 227-0033 Japan.; Faculty of Pharmaceutical Sciences, Toho University, 2-2-1 Miyama, Funabashi Chiba 274-8510 Japan, |
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| Abstract: | A facile synthetic procedure for the production of N-alkylated 3,4-dihydroisoquinolinone derivatives is described. The desired products were obtained by N-alkylation of 3,3′-dimethyl-3,4-dihydroisoquinoline derivatives followed by oxidation of the resulting iminium salts. Reaction conditions for both steps were very mild and the desired cyclization products could be obtained in good yield. This strategy allows the generation of N-substituted 3,4-dihydroisoquinolinone derivatives with substituents at the 3-position. N-Alkylated 3,4-dihydroisoquinolinone derivatives could be synthesized by N-alkylation of 3,3′-dimethyl-3,4-dihydroisoquinoline derivatives followed by oxidation of the resulting iminium salts. |
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