1908-01-6Relevant articles and documents
Preparation methods of 1H-indazol-3-carboxylic acid derivative, granisetron and lonidamine
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Paragraph 0072-0077; 0116-0121, (2021/05/12)
The invention relates to preparation methods of a 1H-indazol-3-carboxylic acid derivative, granisetron and lonidamine. The 1H-indazol-3-carboxylic acid derivative is a compound with a structure shown in a formula (1) and a formula (2), and is mainly structurally characterized by having a 1H-indazol-3-carboxylic acid amide skeleton and a 1H-indazol-3-carboxylic ester skeleton. The 1H-indazol-3-carboxylic acid derivative can be synthesized by taking simple o-aminophenylacetic acid amide or o-aminophenylacetic acid ester as an initial raw material. The 1H-indazol-3-carboxylic acid derivative is a key intermediate for synthesizing a plurality of medicines, such as granisetron, lonidamine and the like. The synthesis method of the 1H-indazol-3-carboxylic acid derivative and the drug molecules glassetron and lonidamine is simple, the reaction condition is mild, the reaction speed is high, the yield is high, and purification is easy.
Facile and efficient synthesis of indazole derivatives by 1,3-cycloaddition of arynes with diazo compounds and azomethine imides
Jin, Tienan,Yang, Fan,Yamamoto, Yoshinori
scheme or table, p. 957 - 972 (2010/01/19)
N-Unsubstituted indazoles 3 and 1-arylindazoles 4 are readily available in good to high yields through [3+2] cycloaddition of 2-(trimethylsilyI)aryl triflates 1 and diazo compounds in the presence of KF or CsF under mild reaction conditions. Furthermore, we found that azomethine imides also underwent cycloaddition reaction with 2-(trimethylsilyl)phenyl triflates (la) in the presence of KF to afford indazolone derivatives 6 in moderate yields.
Synthesis of some derivatives of 5 methylindazole 3 carboxylic acid
Hannig,Kollmorgen,Geipel
, p. 720 - 723 (2007/10/07)
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