380380-64-3Relevant articles and documents
Tedizolid phosphate impurity as well as preparation method and application thereof
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Paragraph 0016; 0096; 0101-0105; 0120; 0125-0129, (2020/12/10)
The invention provides a tedizolid phosphate impurity as well as a preparation method and application thereof, and belongs to the field of chemical pharmacy. The structural formula of the impurity isshown as a formula I in the specification. The impurity is generated in the process of synthesizing a 2-(2-methyl-2H-tetrazole-5-yl)-5-(4, 4, 5, 5-tetramethyl-1, 3, 2-dioxaborocyclopentane-2-yl) pyridine intermediate, and the quality of a product is seriously influenced by the impurity. The impurity is synthesized and separated, the purity is higher than 96%, and the quality requirements of impurity reference substances related to national pharmacopoeia and Chinese pharmacopoeia are met. The impurity preparation process is simple and stable and good in repeatability; and the prepared impurity2-(2-methyl-tetrazole)-5-azido pyridine can be used as a reference substance to be applied to quality control of tedizolid phosphate API, crude drugs and preparations, can also provide a reliable monitoring means for process research and promote the process optimization and determination procedures and has a good application prospect.
TRIAZOLOTRIAZINE DERIVATIVES AS A2A RECEPTOR ANTAGONISTS
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Page/Page column 45-46, (2020/01/24)
The present invention provides triazolotriazine derivatives of formula (1) as A2A receptor antagonists. Compounds of formula (1) and pharmaceutical compositions including the compounds can be used for the treatment of disorders related to A2A receptor hyp
Synthesis method of tedizolid intermediate
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, (2017/04/19)
The invention provides a synthesis method of a tedizolid intermediate. The synthesis method comprises the following steps: Step A: generating a compound (II) or acidic salt of the compound (II) through addition reaction of a cyano group in a compound (I) and alcohol; Step B: generating a compound (III) by replacing an alkoxy on the compound (II) or the acidic salt of the compound (II) with a hydrazine group or a methylhydrazine group; Step C: generating a tedizolid intermediate (IV) through reaction of the compound (III) and sodium nitrite under an acidic condition. The overall reaction formula is shown in the original specification. According to the synthesis method disclosed by the invention, the problems of easy explosion and poison of reaction reagent, difficulty in separation of a methyl-isomer by-product and so on are solved.