- Kinetic resolution of racemic benzofused alcohols catalysed by HMFO variants in presence of natural deep eutectic solvents
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5-Hydroxymethylfurfural oxidase (HMFO) has demonstrated to be a useful biocatalyst for the selective oxidation of alcohols employing oxygen as mild oxidant with no requirement of expensive organic cofactors. This wild-type HMFO biocatalyst and an engineered thermostable variant have been tested in the kinetic resolution of different benzofused alcohols. The use of natural deep eutectic solvents was also explored in HMFO-catalysed oxidation of alcohols. The oxidation of racemic 1-indanol showed a higher conversion and selectivity in presence of 60% v/v of different NADES, especially for those containing carbohydrates. By choosing properly the biocatalyst and the NADES, good enantioselectivity values can be obtained, demonstrating the advantages of employing these neoteric solvents in biocatalysed processes.
- Fraaije, Marco,Lon?ar, Nikola,de Gonzalo, Gonzalo
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- Efficient synthesis and resolution of novel 2-(hydroxymethyl)-7,8-dihydro- 1H-indeno[5,4-b] furan-6(2H)-one by lipase Pseudomonas cepacia
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Lipase Pseudomonas cepacia catalyzed acylation of (±)-2- (hydroxymethyl)-7,8-dihydro-1H-indeno[5,4-b] furan-6(2H)-one using vinyl acetate as the acyl donor in acetone gave (-)-(R)-2-acetoxy-2-(methyl)-7,8-dihydro-1H- indeno[5,4-b] furan-6(2H)-one and (+)-(S)-2-(hydroxymethyl)-7,8-dihydro-1H- indeno[5,4-b] furan-6(2H)-one with high enantiomeric excess. Enantiomerically pure 2-(hydroxymethyl)-7,8-dihydro-1H-indeno[5,4-b] furan-6(2H)-one are useful intermediates for the preparation of Ramelteon, an FDA approved drug for the treatment of insomnia.
- Nagarapu, Lingaiah,Vulupala, Hanmanth Reddy,Bantu, Rajashaker,Sajja, Yashodakrishna,Nanubolu, Jagadeesh Babu
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p. 578 - 582
(2014/05/06)
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- 5- substituted tetralones as inhibitors of ras farnesyl trransferase
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The present invention provides novel 5-substituted tetralones of Formulas (I), (II), (III) and (IV) and pharmaceutically acceptable salts, esters, amides, and prodrugs thereof, which are useful for treating and preventing uncontrolled or abnormal proliferation of tissues, such as cancer, atherosclerosis, restenosis, and psoriasis. Specifically, the present invention relates to compounds that inhibit the farnesyl transferase enzyme.
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- Predicting the Claisen rearrangement regioselectivity of allylindanyl and allyltetrahydronaphthalenyl ether derivatives by 1H NMR experiments
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The regioselectivity of the Claisen rearrangement of allylindanyl and allyltetrahydronaphthalenyl ether derivatives can be predicted by conformational preference detected by 1H NMR NOE difference spectra and T1 measurements. Copyright
- Rodrigues, Denise C.,Fernandes, Sergio A.,Marsaioli, Anita J.
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p. 970 - 974
(2007/10/03)
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