Ziwei Feng, Beiqian Tian, Guangyan Li, Li Wang, Na Wang, Xin Huang, Lina Zhou, Shuangxi Li, Hao Wang, Ting Wang* and Hongxun Hao*,
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引用次数: 0
Abstract
In this work, two anhydrates (form A and form B) and one dihydrate (form C) of aztreonam were found and were characterized by powder X-ray diffraction (PXRD), thermogravimetric analysis, differential thermal analysis, and Fourier transform infrared spectroscopy. Dynamic vapor adsorption and variable-temperature PXRD experiments were carried out to study their thermal stability and moisture absorption stability. Furthermore, the critical water activity of aztreonam at 10–45 °C was determined, and it was found that the water activity determines the dehydration process of form C. The solubility of form A and form B in methanol solvent was measured at 10–45 °C to decide the thermodynamic stability of the polymorphs, and it was found that form B is thermodynamically stable below 28 °C, while form A is thermodynamically stable above 28 °C. The competitive suspension experiments further proved that form A and form B are enantiotropic polymorphs. In addition, the solution-mediated phase transition (SMPT) process of aztreonam form C was in situ monitored using Raman spectroscopy. The results show that the SMPT process is jointly controlled by the dissolution of the dihydrate and the nucleation of anhydrates, in which temperature plays a very important role. Finally, the SMPT mechanism of the dihydrate form is proposed.
期刊介绍：
The journal Organic Process Research & Development serves as a communication tool between industrial chemists and chemists working in universities and research institutes. As such, it reports original work from the broad field of industrial process chemistry but also presents academic results that are relevant, or potentially relevant, to industrial applications. Process chemistry is the science that enables the safe, environmentally benign and ultimately economical manufacturing of organic compounds that are required in larger amounts to help address the needs of society. Consequently, the Journal encompasses every aspect of organic chemistry, including all aspects of catalysis, synthetic methodology development and synthetic strategy exploration, but also includes aspects from analytical and solid-state chemistry and chemical engineering, such as work-up tools，process safety, or flow-chemistry. The goal of development and optimization of chemical reactions and processes is their transfer to a larger scale; original work describing such studies and the actual implementation on scale is highly relevant to the journal. However, studies on new developments from either industry, research institutes or academia that have not yet been demonstrated on scale, but where an industrial utility can be expected and where the study has addressed important prerequisites for a scale-up and has given confidence into the reliability and practicality of the chemistry, also serve the mission of OPR&D as a communication tool between the different contributors to the field.
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