1312784-58-9Relevant articles and documents
Preparation method of tert-butyl 1,7-diazaspiro[3.5]nonane-7-carboxylate and oxalate thereof
-
Paragraph 0026; 0028-0029; 0037, (2021/08/21)
The invention relates to the field of synthesis of medical intermediates, and particularly discloses tert-butyl 1,7-diazaspiro[3.5]nonane-7-carboxylate and oxalate thereof. The preparation method of tert-butyl 1,7-diazaspiro[3.5]nonane-7-carboxylate comprises the following steps: by taking N-tert-butyloxycarbonyl-4-piperidone, ethyl hydrogen malonate and ammonium acetate as initial raw materials, sequentially carrying out Mannich reaction, reduction reaction, halogenation, cyclization reaction and purification to obtain purified tert-butyl 1,7-diazaspiro[3.5]nonane-7-carboxylate. The preparation method disclosed by the invention is simple to operate and suitable for industrial mass production.
Synthesis method of 1,7-diazaspiro[3.5]nonane-7-tert-butyl formate
-
Paragraph 0048; 0051-0052, (2021/08/07)
The invention provides a process synthesis method of 1,7-diazaspiro[3.5]nonane-7-tert-butyl formate. The synthesis method comprises the following five steps: 1, reacting a compound 1 with a bromine compound 2 and ammonium acetate by a one-pot method to obtain a compound 2; 2, reducing a compound 3 by using lithium borohydride to obtain a compound 4; 3, using triethylamine is used as alkali, and reacting the compound 4 with p-toluene sulfonyl chloride to generate a compound 5; 4, under the catalysis of potassium iodide, taking cesium carbonate as alkali, and carrying out ring closing on the compound 5 to generate a compound 6; and 5, under the action of magnesium chips, removing p-toluene sulfonyl from the compound 6 to obtain a compound 7. The method mainly solves the technical problem that no method suitable for industrial synthesis exists at present, and has the advantages that raw materials are easy to obtain, the total yield is high, and the method is suitable for industrial production.
PROTEIN TYROSINE PHOSPHATASE INHIBITORS
-
Paragraph 00526, (2020/05/21)
Compounds of Formula la or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof are provided, which are useful for the treatment of hyperproliferative diseases in the view of their ability to inhibit SHP2. Methods of using compounds of Formula I or a stereoisomer, tautomer or pharmaceutically acceptable salt thereof, for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions are disclosed.
NOVEL THIENOPYRROLE COMPOUNDS
-
Page/Page column 39, (2011/07/06)
The invention provides a compound of Formula (I) pharmaceutically acceptable salts, pro-drugs, biologically active metabolites, stereoisomers and isomers thereof wherein the variable are defined herein. The compounds of the invention are useful for treati