Short synthesis of tert-butyl-hydroxylated 3,5-di-tert-butyl-4-hydroxybenzaldehyde: Synthesis of tert-butyl-hydroxylated S-2474 |
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Authors: | Inagaki Masanao Matsumoto Saichi Tsuri Tatsuo |
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Affiliation: | Discovery Research Laboratories, Shionogi & Company, Ltd., Fukushima-ku, Osaka 553-0002, Japan masanao.inagaki@shionogi.co.jp |
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Abstract: | We have developed a very short synthesis of tert-butyl-hydroxylated di-tert-butyl-4-hydroxybenzaldehyde in which the HBr-DMSO system is used as an effective oxidant (overall yield of 45% for the entire four-step process from 2-tert-butyl-p-cresol). We also accomplished the synthesis of a major metabolite of the antiarthritic drug candidate S-2474. |
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