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Issue 15, 2018
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A high throughput screening method for the nano-crystallization of salts of organic cations

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Abstract

The generation of solid salts of organic molecules is important to the chemical and pharmaceutical industry. Commonly used salt screening methods consume a lot of resources. We employed a combination of ion exchange screening and vapour diffusion for crystallization. This technique is semi-automatic and requires just nanoliters of the solution of the analyte to be crystallized. This high throughput screening yielded single crystals of sufficient size and quality for single-crystal X-ray structure determination using an in-house X-ray diffractometer. The broad scope of our method has been shown by challenging it with 7 very different organic cations, whose aqueous solubilities vary by a factor of almost 1000. At least one crystal structure for 6 out of 7 tested cations was determined; 4 out of the successful 6 ones had never been crystallized before. Our method is extremely attractive for high throughput salt screening, especially for active pharmaceutical ingredients (APIs), as about 40% of all APIs are cationic salts. Additionally, our screening is a new and very promising procedure for the crystallization of salts of organic cations.

Graphical abstract: A high throughput screening method for the nano-crystallization of salts of organic cations

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Publication details

The article was received on 16 Feb 2018, accepted on 06 Mar 2018 and first published on 12 Mar 2018


Article type: Edge Article
DOI: 10.1039/C8SC00783G
Citation: Chem. Sci., 2018,9, 3716-3722
  • Open access: Creative Commons BY-NC license
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    A high throughput screening method for the nano-crystallization of salts of organic cations

    P. P. Nievergelt, M. Babor, J. Čejka and B. Spingler, Chem. Sci., 2018, 9, 3716
    DOI: 10.1039/C8SC00783G

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