75235-71-1Relevant academic research and scientific papers
Aromatic heterocyclic borate and its preparation method, use (by machine translation)
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Paragraph 0069-0073, (2017/06/02)
The invention relates to a hydroxyalkylation heterocyclic borate and its preparation method, use; said additive structural formula such as formula (I) or (II) shown; the invention also relates to the above-mentioned aromatic heterocyclic borate lubricating additive preparation method, the method comprises the following steps: step a, in the organic solvent and catalyst under the condition of, heterocyclic compounds and alkyl epoxide reaction, generating compounds A; make stated, in the organic solvent and catalyst under the condition of the, compound B with compound A, or by the reaction of the cyclic ethers, can be; the invention also relates to the use of alkylated heterocyclic borate fore-mentioned hydroxy. (by machine translation)
Asymmetric reduction of 1-(benzoazol-2-ylsulfanyl)propan-2-ones using whole cells of Mortierella isabellina, Debaryomyces hansenii, Geotrichum candidum and Zygosaccharomyces rouxii
Borowiecki, Pawe?,W?oczewska, Ma?gorzata,Ochal, Zbigniew
, p. 9 - 16 (2014/11/08)
Growing cells of four fungal strains were used in reduction of 1-(benzoazol-2-ylsulfanyl)propan-2-ones 3a-c to corresponding (R)-(+)-1-(benzoazol-2-ylsulfanyl)propan-2-ols (R)-(+)-4a-c. All of the investigated yeast strains displayed a very high activity toward prochiral ketones 3a-c converting them to the desired alcohols after relatively short reaction time (1-3.5 h). The biotransformation products were isolated with moderate to good yields (45-89%) and in highly enantioenriched forms (94-99% ee). Stereoselective bioreduction of 1-(1H-benzimidazol-2-ylsulfanyl)propan-2- one 3a by D. hansenii DSM 3428 growing cells provided the respective (R)-alcohol with >99% yield, in reasonable 65% isolated yield and in a highly stereoselective manner (98% ee) after 3 h of cultivation. In the same culture, bioreduction of 1-(1,3-benzoxazol-2-ylsulfanyl)propan-2-one 3b led to a 76% yield, 65% isolated yield and very high 94% ee of the formed (R)-alcohol. Similar 1.5 h incubation of 1-(1,3-benzothiazol-2-ylsulfanyl)propan-2-one 3c in G. candidum LOCK 105 culture resulted in the corresponding (R)-alcohol preparation in moderate 45% isolated yield with excellent enantiomeric purity (99% ee).
Asymmetric reduction of 1-(benzoazol-2-ylsulfanyl)propan-2-ones using whole cells of Mortierella isabellina, Debaryomyces hansenii, Geotrichum candidum and Zygosaccharomyces rouxii
Borowiecki, Pawel,Wloczewska, Malgorzata,Ochal, Zbigniew
, p. 9 - 16 (2015/01/09)
Growing cells of four fungal strains were used in reduction of 1-(benzoazol-2-ylsulfanyl)propan-2-ones3a-c to corresponding (R)-(+)-1-(benzoazol-2-ylsulfanyl)propan-2-ols (R)-(+)-4a-c. All of the investi-gated yeast strains displayed a very high activity toward prochiral ketones 3a-c converting them tothe desired alcohols after relatively short reaction time (1-3.5 h). The biotransformation products wereisolated with moderate to good yields (45-89%) and in highly enantioenriched forms (94-99% ee). Ste-reoselective bioreduction of 1-(1H-benzimidazol-2-ylsulfanyl)propan-2-one 3a by D. hansenii DSM 3428growing cells provided the respective (R)-alcohol with >99% yield, in reasonable 65% isolated yield andin a highly stereoselective manner (98% ee) after 3 h of cultivation. In the same culture, bioreduction of1-(1,3-benzoxazol-2-ylsulfanyl)propan-2-one 3b led to a 76% yield, 65% isolated yield and very high 94%ee of the formed (R)-alcohol. Similar 1.5 h incubation of 1-(1,3-benzothiazol-2-ylsulfanyl)propan-2-one3c in G. candidum LOCK 105 culture resulted in the corresponding (R)-alcohol preparation in moderate45% isolated yield with excellent enantiomeric purity (99% ee).
Lipase-catalyzed kinetic resolution of 1-(1,3-benzothiazol-2-ylsulfanyl) propan-2-ol with antifungal activity: A comparative study of transesterification versus hydrolysis
Borowiecki, Pawe?,Fabisiak, Marcin,Ochal, Zbigniew
, p. 4597 - 4602 (2013/06/27)
A study of chemoenzymatic synthesis of both enantiomers of 1-(1,3-benzothiazol-2-ylsulfanyl)propan-2-ol was carried out. Several commercially available lipase preparations were tested as biocatalysts in the kinetic resolution process of target compound by enantioselective transesterification and/or hydrolysis. CAL-B (Novozym 435) was found to be the optimal catalyst. The lipase-mediated hydrolysis approach appeared to be superior to the transesterification reaction. Absolute configuration of the obtained alcohol was postulated, applying modified Mosher's methodology. The inhibitory activity of the synthesized benzothiazole derivatives against pathogenic fungi was checked.
