- Functional activity of the mouse flavin-containing monooxygenase forms 1, 3, and 5
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Three functional mouse flavin-containing monooxygenases (mFMOs) (i.e., mFMO1, mFMO3, and mFMO5) have been reported to be the major FMOs present in mouse liver. To examine the biochemical features of these enzymes, recombinant enzymes were expressed as mal
- Zhang, Jun,Cerny, Matt A.,Lawson, Matt,Mosadeghi, Ruzbeh,Cashman, John R.
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- A practical procedure for the synthesis of Esonarimod, (R,S)-2-acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid, an antirheumatic agent. II
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An efficient large-scale synthesis of Esonarimod, (R,S)-2-acetylthio-methyl-4-(4-methylphenyl)-4-oxobutanoic acid (1), a new antirheumatic drug, was established. A small amount of water increased the yield of the Michael addition of thioacetic acid (4) to
- Noguchi, Toshiya,Onodera, Akira,Ito, Masato,Yoshida, Mamoru,Yokomori, Sadakazu
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- A practical procedure for the synthesis of esonarimod, (R,S)-2-acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid, an antirheumatic agent (part 1).
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An efficient and practical procedure for the synthesis of esonarimod, (R,S)-2-acetylthiomethyl-4-(4-methylphenyl)-4-oxobutanoic acid (1), a new antirheumatic drug, has been developed. The intermediate, 2-methylene-4-(4-methylphenyl)-4-oxobutanoic acid (2), was prepared by Friedel-Crafts acylation of toluene with itaconic anhydride (3) in the presence of aluminum trichloride and nitrobenzene in 63% yield without silica gel column purification. Compound 1 was prepared by Michael addition of 2 with thioacetic acid (4) in 74% yield. Overall, 1 was obtained in 47% yield from 3. The structures and synthetic mechanisms of by-products (five compounds) of 2 were also clarified.
- Noguchi, Toshiya,Onodera, Akira,Tomisawa, Kazuyuki,Yokomori, Sadakazu
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p. 1407 - 1412
(2007/10/03)
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