- Simple chemoenzymatic access to enantiopure pharmacologically interesting (R)-2-hydroxypropiophenones
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A chemoenzymatic synthesis of pharmacological interesting (R)-2-hydroxypropiophenones starting from propiophenone derivatives is described. Manganese(III) acetate-mediated acetoxylation followed by fungus-mediated hydrolysis of propiophenone derivatives affords (R)-2-hydroxypropiophenones in high enantiomeric excess.
- Demir, Ayhan S.,Hamamci, Haluk,Sesenoglu, Ozge,Aydogan, Feray,Capanoglu, Doga,Neslihanoglu, Rahsan
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p. 1953 - 1956
(2007/10/03)
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- Stereoselective synthesis of antifungal agent threo-2-(2,4-difluorophenyl)-3-methylsulfonyl-1-(1H-1,2,4-triazol-1-yl )-2-butanol (SM-8668)
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The stereoselective synthesis of antifungal agent threo-2-(2,4-difluorophenyl)-3-methylsulfonyl-1-(1H-1,2,4-triazol-1-yl )-2-butanol (SM-8668) is described. The key step is the selective synthesis of intermediate threo-2-(2,4-difluorophenyl)-2-(1-substituted ethyl)oxirane. threo-2-(2,4-difluorophenyl)-2-(1-methylthioethyl)oxirane was synthesized threo-selectively by the reaction of 1-(2,4-difluorophenyl)-2-methylthio-1-propanone with dimethyloxosulfonium methylide in a heterogeneous media consisting of a hydrophobic solvent and aqueous alkaline solution.
- Saji,Tamoto,Tanaka,Miyauchi,Fujimoto,Ohashi
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p. 1427 - 1433
(2007/10/02)
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- Decomposition of α-hydroxyaryl ketones and characterization of some unusual products
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α-Hydroxyaryl ketones such as 2-hydroxypropiophenone and 1-(2,4- difluorophenyl)-2-hydroxy-1-propanone, the key intermediates in the preparation of antifungal agents, decompose into oxidized, rearranged, and condensed products. These products were isolated and characterized. The possible mechanisms for the formation of the products are discussed.
- Gala,Puar,Das,Kugelman,DiBenedetto
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p. 1199 - 1203
(2007/10/02)
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