- Enantioselective Biocatalytic Reduction of 2 H-1,4-Benzoxazines Using Imine Reductases
-
A biocatalytic reduction of 2H-1,4-benzoxazines using imine reductases is reported. This process enables a smooth and enantioselective synthesis of the resulting cyclic amines under mild conditions in aqueous media by means of a catalytic amount of the cofactor NADPH as hydride source as well as glucose as the reducing agent used in stoichiometric amounts for in situ cofactor recycling. Several substrates were studied, and the 3,4-dihydro-2H-1,4-benzoxazines were obtained with up to 99% ee. In addition, the efficiency of this reduction process based on imine reductases as catalysts has been demonstrated for one 2H-1,4-benzoxazine on an elevated laboratory scale running at a substrate loading of 10 g L-1 in the presence of a tailor-made whole-cell catalyst.
- Zumbr?gel, Nadine,Machui, Paul,Nonnhoff, Jannis,Gr?ger, Harald
-
p. 1440 - 1447
(2019/02/07)
-
- Synthesizing method of novel ofloxacin intermediate
-
The invention relates to the field of medicine synthesizing, in particular to a synthesizing method of a novel ofloxacin intermediate as shown in structural formula (II). The synthesizing method includes: allowing 2,3,4-trifluoro nitrobenzene to have reac
- -
-
-
- Chemoenzymatic Asymmetric Synthesis of 1,4-Benzoxazine Derivatives: Application in the Synthesis of a Levofloxacin Precursor
-
A versatile and general route has been developed for the asymmetric synthesis of a wide family of 3-methyl-3,4-dihydro-2H-benzo[b][1,4]oxazines bearing different pattern substitutions in the aromatic ring. Whereas hydrolases were not suitable for resoluti
- López-Iglesias, María,Busto, Eduardo,Gotor, Vicente,Gotor-Fernández, Vicente
-
p. 3815 - 3824
(2015/05/04)
-
- Synthesis and antibacterial activities of substituted 7-oxo-2,3-dihydro-7h-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acids
-
As part of a search for new synthetic antibacterial agents to combat systemic infection, various analogues of 7-oxo-2,3-dihydro-7H-pyrido[1,2,3-de][1,4]benzoxazine-6-carboxylic acids were synthesized. Among the compounds newly synthesized, 9-fluoro-3-methyl-10-(4-methyl-1-piperazinyl)-7-oxo-2,3-dihydro-7H-pyrido[ 1,2,3-de][1,4]benzoxazine-6-carboxylic acid (DL-8280) showed potent antibacterial activity against Gram-positive and -negative pathogens, including Psedomonas aeruginosa, and its metabolic disposition was shown in separate experimentals to be favorable.
- Hayakawa,Hiramitsu,Tanaka
-
p. 4907 - 4913
(2007/10/02)
-
- Benzoxazine derivatives
-
Pyrido[1,2,3-de][1,4]benzoxazine derivatives are described having the formula (I) STR1 wherein X is a halogen atom, R is a hydrogen atom or an alkyl group of 1 to 6 carbon atoms and Z represents mono-substituted, di-substituted or cyclic-substituted amino group which may contain a hetero atom and may have a substituent such as hydroxyl, alkyl having 1 to 6 carbon atoms, amino, hydroxyalkyl having 1 to 6 carbon atoms or mono- or di-alkylamino having 1 to 6 carbon atoms in each alkyl moiety and the pharmaceutically acceptable salt thereof, having antibacterial activity.
- -
-
-