127369-30-6Relevant articles and documents
Preparation method of (-) - Cytoxazone and (+) -4 - epi-Cytoxazone
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Paragraph 0090-0094, (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.
Intermediate of RORgamma inhibitor and preparation method thereof
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Paragraph 0161; 0162; 0163; 0164; 0165, (2019/04/27)
The invention belongs to the technical field of drugs, in particular to an intermediate of a RORgamma inhibitor and a preparation method thereof. The intermediate is as shown in a formula (I). The method has the advantages of being easily available in raw material, concise in process, economic and environment-friendly, high in yield and the like. The formula is as shown in the description.
NOVEL ANTIESTROGENIC HETEROCYCLIC COMPOUNDS
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Page/Page column 64; 65, (2018/08/20)
The present invention provides novel heterocyclic compounds of Formula I wherein A, B, E, ring Z, Y, L, ring X, D, m, n, R7 and R8 are as defined in the specification as estrogen receptor antagonists/degraders. The compound of Formula I can be used for the treatment of cancers mediated by estrogen receptors. (Formula I ).