151213-40-0Relevant articles and documents
(S, S)-2, 8-diazabicyclo[4.3.0]nonane intermediate, and preparation method and application thereof
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Paragraph 0107-0112, (2021/06/13)
The invention discloses a (S, S)-2, 8-diazabicyclo[4.3.0]nonane intermediate, and a preparation method and application thereof. New compounds, namely compounds II-V, are taken as key intermediates, a new route for synthesizing (S, S)-2, 8-diazabicyclo[4.3.0]nonane is developed, and in the route, dialkoxy acetate taken as an initial raw material in the route sequentially undergoes Claisen condensation, substitution reaction, intramolecular dehydration cyclization, catalytic hydrogenation reduction, chiral resolution, dissociation, hydrolysis, intramolecular dehydration cyclization and catalytic hydrogenation to obtain the(S, S)-2, 8-diazabicyclo[4.3.0]nonane. The preparation method is simple, the total reaction yield is high, the product quality is good, the process route is green and environment-friendly, and the method has a good industrial application prospect.
Method for preparing moxifloxacin intermediate (S, S)-2, 8-diazabicyclo [4, 3, 0] nonane
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, (2021/06/09)
The invention provides a method for preparing a moxifloxacin intermediate (S, S)-2, 8-diazabicyclo [4, 3, 0] nonane, and relates to the technical field of organic synthesis. According to the method, the azaphthalide is used as a raw material, and due to the ring structure of the azaphthalide, the other two non-corresponding chiral isomers which are not needed in chiral reduction are almost not generated; the chiral purity of the intermediate obtained through reduction is very high, resolution is not needed, and (S, S)-2, 8-diazabicyclo [4, 3, 0] nonane can be obtained directly through ammonolysis, reduction, chlorination and cyclization subsequently. According to the method provided by the invention, chiral resolution is not needed, the process is simple, the process steps are short, the cost is low, and the product is high in chiral purity and high in total yield. Furthermore, in the subsequent product salifying and refining step, carboxylic acid with a chiral structure does not need to be used for salifying, and common achiral carboxylic acid can be used for refining, so the product purity is further improved.
Preparation method of moxifloxacin intermediate
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, (2020/05/14)
The invention discloses a preparation method of a moxifloxacin intermediate. The invention provides a preparation method of a compound as shown in a formula III, which comprises the following step: ina solvent, in the presence of alkali, carrying out cyclization reaction as shown in the specification on a compound as shown in a formula II to obtain the compound as shown in the formula III. The method is simple to operate, high in chiral selectivity, simple in process, high in yield and high in purity.