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Method for preparing 3-methyl-5-amido-1-trtrahydropyranyl-indazole

A tetrahydropyranyl and amine-based technology, applied in organic chemistry and other fields, can solve problems such as not many compounds

Inactive Publication Date: 2009-11-04
NANCHANG HANGKONG UNIVERSITY
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

There are not many studies on this compound abroad, and there is no report on its synthesis in China

Method used

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Examples

Experimental program
Comparison scheme
Effect test

Embodiment Construction

[0010] 1. Preparation of intermediate 3-methylindazole

[0011] Add 25 grams of 2-fluoroacetophenone and 45 milliliters of ethylene glycol into a dry 500 milliliter four-necked bottle, stir the oil bath to heat up to 80 ° C, and add dropwise a solution made of 18 milliliters of hydrazine hydrate and 45 milliliters of ethylene glycol (It took about 30 minutes to finish dropping, and the system changed from an emulsion to a yellow solution). After the drop, the temperature was raised to 120°C and stirred for 0.5 hours, and then the temperature was raised to 180°C for reaction (sampling and inspection by liquid chromatography every 3 hours to track to 4.9 The minute species (intermediate) were all converted to the 5.5 minute species (product)). After completion of the reaction (light brown solution), extract three times with 100 ml of ethyl acetate, combine the organic phases, wash twice with 100 ml of water, wash twice with 100 ml of brine, and wash with anhydrous MgSO 4 Dry, f...

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PUM

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Abstract

The invention discloses a method for preparing 3-methyl-5-amido-1-trtrahydropyranyl-indazole, which is characterized in that 2-fluoro acetophenone is taken as raw material, intermediate 3-methylindazole is prepared by cyclization reaction, 3-methyl-5-nitroindazole is prepared by nitratlon reaction, and then the trtrahydropyranyl is introduced, finally, the reaction product is reduced and aminated, and the peachy powder target product can be obtained. The 3-methyl-5-amido-1-trtrahydropyranyl-indazole is an important pharmaceutical intermediate. The method has the advantages of easily obtained reaction raw material with lower price, mild reaction, simple condition, stable reaction, good reproducibility and expanded production.

Description

technical field [0001] The invention relates to a preparation method of 3-methyl-5-amino-1-tetrahydropyranyl-indazole. Background technique [0002] 3-Methyl-5-amino-1-tetrahydropyranyl-indazole is an important pharmaceutical and pesticide intermediate. It belongs to indazole drugs and has strong antibacterial pharmacological effects, so it has potential research and application value. There are not many studies on this compound abroad, and there is no report on its synthesis in China. In view of this fact, the present invention elaborates the whole preparation process in detail: using 2-fluoroacetophenone as raw material, through four-step reactions: ring-forming reaction, nitration reaction, introduction of tetrahydropyranyl reaction, reductive amination reaction , the target product was obtained. Contents of the invention [0003] The object of the present invention is to provide a preparation method of 3-methyl-5-amino-1-tetrahydropyranyl-indazole, which has signifi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D231/56
Inventor 谢宇胡金刚李明俊聂德润牟大吉
Owner NANCHANG HANGKONG UNIVERSITY