Method for producing beta crystal system anhydrous aztreonam

Abstract

The invention relates to a production method of anhydrous beta-type aztreonam, which comprises dissolving alpha-crystal-system aztreonam in the mixture of absolute ethyl alcohol and acetone at -10-+25DEG C, filtering without germ, heating the solution to 30-55DEG C, or seriously mixing to obtain anhydrous beta-type aztreonam crystals.

Description

technical field

[0001] The invention relates to a production method of anhydrous β crystal form aztreonam crystal. Background technique

[0002] Aztreonam (Aztreonam) shown in molecular formula I is a synthetic monocyclic β-lactam antibiotic, which has antibacterial activity against Gram-negative bacteria.

[0003]

[0004] Molecular formula I

[0005] Some references report the preparation technology of aztreonam, for example: US Patent Nos. 4,775,670 and 5,194,604. Aztreonam has polymorphism, and US Pat. No. 4,826,973 reports four different crystals of aztreonam, namely α-, β-, γ-, and δ-types. The α crystal form is a hydrous crystal, usually containing 7-15% water, and has poor stability. Therefore, it should be transformed into the β crystal form, which has the characteristics of anhydrous, non-hygroscopic, good fluidity, smaller surface area, and better stability, and is more suitable for pharmaceutical use.

[0006] U.S. Patent No. 4,946,838 reports the preparat...

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