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Preparation of butoconazole nitrate intermediate

A chlorophenyl, reaction technology, applied in the field of preparation of antifungal drug butoconazole nitrate, can solve the problems of unsuitability for large-scale industrial production, poor safety, and difficult control

Active Publication Date: 2014-02-05
万全万特制药(厦门)有限公司
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

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Problems solved by technology

[0005] The ether used in the above method is a solvent, the reaction is violent, the safety is poor, it is difficult to control, and it is not suitable for industrialized large-scale production

Method used

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  • Preparation of butoconazole nitrate intermediate
  • Preparation of butoconazole nitrate intermediate
  • Preparation of butoconazole nitrate intermediate

Examples

Experimental program
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Effect test

Embodiment 1

[0019] Add 15.4g of magnesium powder, 1g of methyl iodide and 250ml of tetrahydrofuran into a 2000ml three-necked flask and stir. Heat to reflux. Under reflux conditions, a mixture of 112 g of p-chlorophenethyl chloride and 500 ml of tetrahydrofuran was added dropwise to initiate the reaction. Heating was stopped and the residue was added dropwise. After the dropwise addition, the reaction was heated to reflux for 1 hour and cooled to room temperature.

[0020] Add 50.2g of chloroacetaldehyde and 250ml of tetrahydrofuran into a 3000ml three-necked flask and stir. The prepared Grignard reagent was added dropwise, the reaction was exothermic, and the solution was kept under reflux and added dropwise. After the dropwise addition was completed, it was heated to reflux for 1 hour. Add ice water and 1M hydrochloric acid, and separate the layers. The organic phase was dried with anhydrous magnesium sulfate, concentrated under reduced pressure, and the fraction at 134-138° C. (2 ...

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Abstract

The invention discloses a method for preparing 1-chloro-4-(4-chlorophenyl)-2-tutanol comprising reacting a compound of formula III with magnesium to prepare a grignard reagent at a proper temperature in one or several non protonic solvents, then reacting the grignard reagent with a compound of formula IV. The 1-chloro-4-(4-chlorophenyl)-2-tutanol is an important intermediate for preparing butoconazole nitrate.

Description

technical field [0001] The invention relates to a preparation method of compound 1-chloro-4-(4-chlorophenyl)-2-butanol (compound of formula I), which can be used for preparing antifungal drug butoconazole nitrate. Background technique [0002] Butoconazole nitrate is an imidazole antifungal drug, and its antibacterial effect on Candida albicans is equal to or due to other imidazole derivatives, such as clotrimazole, miconazole and nystatin; its clinical use is 3 days and 8 days The cure rate is obviously due to the commercially available "Daknine", "Canitine" and "Micodine". [0003] According to incomplete statistics of the World Health Organization, the incidence of various gynecological diseases among women is over 65%, and the incidence of gynecological diseases among women of childbearing age is over 70%. More than 100% of them have seriously affected their normal work and life due to the illness, while gynecological inflammation also has the characteristics of recurre...

Claims

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Application Information

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Patent Type & Authority Patents(China)
IPC IPC(8): C07C33/46C07C29/40C07C233/58A61K31/4164A61P31/10
Inventor 张志强
Owner 万全万特制药(厦门)有限公司
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