89088-55-1Relevant academic research and scientific papers
Pyrazolothiadiazoles from 3-Aminopyrazoles: The Hetero-Herz Reaction
Chenard, B. L.
, p. 1224 - 1227 (1984)
The reaction of sulfur monochloride with pyrazoleamines gives good to excellent yields of pyrazolodithiazolium chlorides from a hetero-Herz reaction.No chlorination of the pyrazole nucleus was observed - a normal occurrence in Herz reactions.The Herz salts were converted to novel pyrazolothiadiazoles.
Synthesis method of 5-bromine-1-methyl-1H-pyrazole-3-amine
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Paragraph 0017, (2020/12/30)
The invention discloses a synthesis method of 5-bromine-1-methyl-1H-pyrazole-3-amine. The method comprises the steps of condensing diethyl butynedioate serving as a raw material with methylhydrazine to obtain 5-hydroxyl-1-methyl-1H-pyrazole-3-carboxylic acid ethyl ester, and reacting the 5-hydroxyl-1-methyl-1H-pyrazole-3-carboxylic acid ethyl ester with phosphorus oxybromide to obtain 5-bromine-1-methyl-1H-pyrazole-3-carboxylic acid ethyl ester; hydrolyzing in a sodium hydroxide alcohol solution to obtain 5-bromine-1-methyl-1H-pyrazole-3-carboxylic acid, reacting the 5-bromine-1-methyl-1H-pyrazole-3-carboxylic acid with dimethyl azide phosphate and tert-butyl alcohol to obtain tert-butyl (5-bromine-1-methyl-1H-pyrazole-3-yl) carbamate, and hydrolyzing in trifluoroacetic acid to obtain the5-bromine-1-methyl-1H-pyrazole-3-amine. The method has the advantages of simple synthesis route, reasonable process selection, low raw material cost, simple and easily available raw materials, convenient operation and post-treatment, and no use of highly toxic reagents, and overcomes the defects of expensive and unavailable raw materials, unsafe operation, difficult amplification and the like in the existing synthesis process.
UREA DERIVATIVE HAVING PI3K INHIBITORY ACTIVITY
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Page/Page column 117, (2012/03/26)
Provided is a compound or a pharmaceutically acceptable salt thereof which inhibits the activity of PI3K to regulate many biological processes including the growth, differentiation, survival, proliferation, migration, metabolism, and the like of cells and is therefore useful for the prophylaxis/therapy of diseases including inflammatory diseases, arteriosclerosis, vascular/circulatory diseases, cancer/tumors, immune system diseases, cell proliferative diseases, infectious diseases, and the like. The above problem was solved by providing a urea derivative shown in the present specification, or a pharmaceutically acceptable salt thereof.
INDOLE DERIVATIVES AS CRAC MODULATORS
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Page/Page column 32, (2012/01/30)
Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and R4 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with calcium release-activated calcium channels (CRAC).
PYRAZOLE INHIBITORS OF PHOSPHATIDYLINOSITOL 3-KINASE
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Page/Page column 15; 16, (2011/04/24)
The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3Kγ. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of variou
8-substituted pyrazolopentathiepins and related compounds
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, (2008/06/13)
Heteropentathiepins including pyrazolopentathiepins substituted in the 8-position; intermediate pyrazolo-1,2,3-thiadiazoles, pyrazolothiazathiolium chlorides, and 5-substituted aminopyrazoles; process for making the pentathiepins by reacting the corresponding 1,2,3-thiadiazoles with sulfur at elevated temperatures; process for making the thiazathiolium chlorides; and use of the pentathiepins as fungicides or as sulfur sensitizers in photographic emulsions.
