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Process for purification of anastrozole

一种阿那曲唑、阿那曲唑碱的技术，应用在阿那曲唑的纯化领域，能够解决很难、除去杂质质量标准等问题

Inactive Publication Date: 2009-10-28
SYNTHON BV
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

[0035] [0019] In a word, it is difficult to sufficiently remove impurities from the crude product of Anastrozole to reach a pharmaceutically acceptable quality standard

Method used

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  • Process for purification of anastrozole
  • Process for purification of anastrozole
  • Process for purification of anastrozole

Examples

Experimental program
Comparison scheme
Effect test

preparation example Construction

[0057] [0034] In particular, the present invention can provide pharmaceutical grade anastrozole by using the method of the above invention in operative combination. Especially preferred are the following steps corresponding to the synthesis method of anastrozole.

[0058] [0035] The first step in the process is to provide a reaction mixture containing anastrozole. The reaction mixture comprising the anastrozole molecule is provided according to any known method, but preferably by condensation reaction of a bromomethyl compound of formula (3) or a chloromethyl compound of formula (6) with 1,2,4-triazole get. These starting materials are either commercially available or may be prepared by methods known in the art. Preferably the starting materials are used in a purified state. Although the purification of bromomethyl compounds of formula (3) is sufficiently disclosed in the prior art, no purification process for chloromethyl compounds of formula (6) has been found. However, ...

experiment Embodiment 1

[0079] Stability of Anastrozole Base in Dilute Hydrochloric Acid Aqueous Solution

[0080] [0054] 0.5 g of anastrozole base was suspended in 10 ml of distilled water at room temperature and stirred, and 0.155 ml (1.1 equivalent) of concentrated hydrochloric acid was added under stirring. The mixture was stirred at room temperature for 1 hour, and the solid was filtered and washed with 5 ml of water. Dry in air at room temperature for 2 days.

[0081] Melting point (capillary) 82.6°C.

[0082] Structure: Anastrozole Base

experiment Embodiment 2

[0084] Conversion of anastrozole base to anastrozole hydrochloride in excess of hydrochloric acid

[0085] [0055] 0.5 g of anastrozole base was suspended in 5 ml of 10% aqueous hydrochloric acid at room temperature with stirring. Some of the solids dissolved. For complete dissolution, a further 3 ml of the same acid were added and the mixture was heated to 42°C. The solution was filtered and the filtrate was washed with 2 ml of the same acid. The solution was treated with 10 ml of distilled water with stirring at 20-25°C and stirred for 30 minutes. The solution became cloudy and the crystalline product separated. The mixture was cooled to 5°C and stirred for 1 hour. The solid was filtered, washed with 5ml of water and air dried.

[0086] Yield: 0.633 g of Anastrozole hydrochloride (dihydrate)

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Abstract

Anastrozole can be purified by crystallization from an aqueous-based solvent system. The aqueous-based solvent system can contain dilute acid, or an alcohol or both.

Description

[0001] [0001] This application claims the benefit of priority to U.S. Provisional Patent Application 60 / 747,787 (filed May 19, 2006) at 35 U.S.Cε119(e). The entire contents of which are hereby incorporated by reference. [0002] [0002] The present invention relates to a method for purifying the compound Anastrozole to achieve a pharmaceutically acceptable level of purity. Background of the invention [0003] [0003] Anastrozole, the chemical name is (2,2'-5[(1H-1,2,4-triazol-1-ylmethyl)-1,3-phenylene] two (2-methyl Propionitrile) has a chemical structure such as formula (1): [0004] [0005] is a pharmaceutically active agent that acts as a selective non-steroidal inhibitor of aromatase, an enzyme that regulates the levels of certain female hormones, such as estrogen. [0006] [0004] In pharmaceutical applications, Anastrozole is used for the treatment of advanced breast cancer in postmenopausal women. It is used in pharmaceutical ingredients in the form of free base. ...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07D249/08
CPCC07D249/08
Inventor J·皮斯R·斯姆尔日
Owner SYNTHON BV
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