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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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Supplementary files

Article information


Submitted
16 Feb 2018
Accepted
06 Mar 2018
First published
12 Mar 2018

This article is Open Access
All publication charges for this article have been paid for by the Royal Society of Chemistry

Chem. Sci., 2018,9, 3716-3722
Article type
Edge Article

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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