890655-08-0Relevant articles and documents
NOVEL PROCESSES FOR THE PREPARATION OF 2-OXY-BENZOXAZINONE DERIVATIVES
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Page/Page column 17, (2018/02/28)
Provided herein are novel, commercially viable and industrially advantageous processes for the preparation of 2-hexadecyloxy-6-methyl-4H-3,1-benzoxazin-4-one, and its intermediates, in high yield and purity.
Preparation method of cetilistat
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Paragraph 0051; 0052; 0053, (2016/10/09)
The invention discloses a preparation method of cetilistat; the method has the advantages of concise process, easily obtained raw materials, and mild reaction conditions, and is suitable for industrialized production. According to a reaction route, 2-amino-5-methyl benzoic acid and hexadecyl chloroformate serve as starting raw materials, firstly, amino acylation is carried out, an intermediate is purified, then cyclization is carried out, and the target compound is obtained through a two-step reaction.
Method for preparing cetilistat
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Paragraph 0047; 0048; 0049; 0050; 0051; 0052; 0053, (2016/12/12)
The invention provides a method for preparing cetilistat. According to the method, 2-amidogen-5-methyl benzoic acid is adopted as an initial raw material, under existence of pyridine, the 2-amidogen-5-methyl benzoic acid reacts with chlorine acid cetyl alcohol ester in the first place, a midbody 2-(((hexadecane oxygroup) carbonyl) amidogen)-5-methyl benzoic acid is obtained, then dehydrogenation cyclization reagent is utilized to obtain the cetilistat, and the feeding sequence in step 1 is the 2-amidogen-5-methyl benzoic acid, alkali and the chlorine acid cetyl alcohol ester in sequence. The method has the remarkable advantages that the route is simple, operation is less, atom economy is better than that of other routes, and the cetilistat is suitable for large-scale production; the purity of the cetilistat at the reaction endpoint is larger than 98%, and through simple postprocessing, a final product which meets medical standards can be obtained, wherein the purity is larger than 99.5%, and the single impurity is smaller than 0.1%; the utilized solvent including dichloromethane and pyridine can be recycled for mechanical application, and the method is environmentally friendly.