143323-49-3Relevant articles and documents
Preparation method of (-) - Cytoxazone and (+) -4 - epi-Cytoxazone
-
, (2021/11/14)
The preparation method of (-) - Cytoxazone and (+) -4 - epi-Cytoxazone takes D - p-hydroxyphenylglycine as a raw material, the intermediate 2 is obtained through methyl esterification reaction under catalysis of thionyl chloride, and then the amino is protected with Boc anhydride to obtain the intermediate 3. The compound 4 is obtained by using potassium carbonate as a base and reacting with methyl iodide under reflux conditions. The methyl ester was reduced with sodium borohydride/lithium chloride to give the primary alcohol compound 5. An intermediate IBX is then obtained with 6 primary alcohol, then reacted with acetone cyanohydrin SN2 to give intermediate 7, and the intermediate 8 is obtained by reacting with the methanol solution of hydrogen chloride to obtain two five-membered ring compound compounds 9 and 10, respectively, with sodium borohydride to obtain (-) - Cytoxazone and its isomers (+) -4 - epi-Cytoxtoxtoxtoxol, respectively.
Compound, pharmaceutically acceptable salt thereof and medical application thereof
-
Paragraph 0357-0362, (2020/07/24)
The invention belongs to the field of medicines, and particularly relates to a compound shown as a formula I or medicinal salt thereof. The invention also relates to application of the compound or themedicinal salt thereof in selectively inhibiting LF activity, resisting anthrax toxin toxicity and preventing or treating anthracnose.
TYROSINE ANALOGUES DERIVATIVES AS RHO- KINASE INHIBITORS
-
Page/Page column 52, (2019/04/09)
The invention relates to compounds of formula (I) inhibiting Rho Kinase that are tyrosine analogues derivatives, methods of preparing such compounds, pharmaceutical compositions containing them and therapeutic use thereof. Particularly the compounds of the invention may be useful in the treatment of many disorders associated with ROCK enzymes mechanisms, such as pulmonary diseases including asthma, chronic obstructive pulmonary disease (COPD), idiopathic pulmonary fibrosis (IPF) and pulmonary arterial hypertension (PAH).