Selective polymorph transformation via solvent-drop grinding

Trask, Andrew V.; Shan, Ning; Motherwell, W. D. S.; Jones, William; Feng, Song; Tan, Reginald B. H.; Carpenter, Keith

doi:10.1039/b416980h

Cited by 191 publications

(153 citation statements)

References 17 publications

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“…In the pharmaceutical context this was demonstrated by Trask et al [33,195] Cocrystallization of caffeine with glutaric acid in chloroform solution provided the cocrystal (caffeine)·(glutaric acid) as two concomitant polymorphs. However, LAG with either chloroform or cyclohexane gave each form selectively.…”

Section: Control Of Stoichiometric Composition and Polymorphismmentioning

confidence: 93%

Mechanochemistry: opportunities for new and cleaner synthesis

et al. 2012

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Citation for published item:tmesD F vF nd edmsD gF tF nd folmD gF nd frgD hF nd gollierD F nd pri § s § i¡ D F nd qrepioniD pF nd rrrisD uF hF wF nd ryettD qF nd tonesD F nd uresD eF nd wkD tF nd winiD vF nd yrpenD eF qF nd rkinD sF F nd herouseD F gF nd teedD tF F nd ddellD hF gF @PHIPA 9wehnohemistry X opportunities for new nd lener synthesisF9D ghemil soiety reviewsFD RI @IAF ppF RIQERRUF Further information on publisher's website: Use policyThe full-text may be used and/or reproduced, and given to third parties in any format or medium, without prior permission or charge, for personal research or study, educational, or not-for-prot purposes provided that:• a full bibliographic reference is made to the original source • a link is made to the metadata record in DRO • the full-text is not changed in any way The full-text must not be sold in any format or medium without the formal permission of the copyright holders.Please consult the full DRO policy for further details.

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Section: Control Of Stoichiometric Composition and Polymorphismmentioning

confidence: 93%

Mechanochemistry: opportunities for new and cleaner synthesis

et al. 2012

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“…LAG (which is also known as solvent-drop grinding (SDG) 24 and has been developed from the kneading 25 technique inaugurated by Braga and co-workers) is the result of molecular diffusion enhanced by substoichiometric amounts of the added liquid. The liquid additive is, however, present in sufficiently small amounts for the system to thermodynamically behave as if it were solvent-free.…”

Section: Mechanosynthesis In Organic Synthesis and Cocrystallizationmentioning

confidence: 99%

Clean and Efficient Synthesis Using Mechanochemistry: Coordination Polymers, Metal-Organic Frameworks and Metallodrugs

Friščić¹,

Halász²,

Štrukil³

et al. 2012

Croat. Chem. Acta

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Abstract. This review briefly discusses recent advances and future prospects in the mechanochemical synthesis of coordination compounds by ball milling and grinding, and highlights our contributions to the mechanosynthesis of porous metal-organic frameworks (MOFs) and zeolitic imidazolate frameworks (ZIFs), metal-organic pharmaceutical derivatives and metallodrugs using the recently developed mechanochemical methods of liquid-assisted grinding (LAG) and ion-and liquid-assisted grinding (ILAG). The role of mechanochemistry in the development of a solvent-free laboratory, cocrystal synthesis and new materials for luminescence and gas absorption is also highlighted. (doi: 10.5562/cca2014)

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“…This has been successfully used in the preparation of a drug in a pure form and it is an environmentally friendly procedure [33][34][35]. The role of solvent is that of a crystallization catalyst and it is believed to function as a lubricant for molecular diffusion [36].…”

Section: Solvent-drop Milling Of Sulfathiazole Fiiimentioning

confidence: 99%

Solid-State Transformations of Sulfathiazole Polymorphs: The Effects of Milling and Humidity

Erxleben

Hodnett

et al. 2013

Crystal Growth & Design

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The effect of milling on the solid-state transitions of sulfathiazole polymorphs in the absence and presence of solvent and excipients was monitored by X-ray powder diffraction (XRPD), attenuated total reflectance infrared (ATR-IR) and near-infrared (NIR) spectroscopy. Sulfathiazole forms FII-FV undergo a transformation toward the metastable FI, which involves an intermediate amorphous stage upon milling at ambient temperature. Milling FIII with catalytic amounts of solvent converts FIII to FIV or to mixtures of FI and FIV depending on the solvent used. Pure FIV can be easily prepared from FIII by this method. The physical stability of pure sulfathiazole forms in the presence of different levels of relative humidity (RH) was also investigated. At low RH all sulfathiazole forms are stable but at RH levels above 70% FII, FIII and FIV remain stable while FI and FV transform to mixtures of FII and FIV without any apparent change in the external form of the crystals. Co-milling FIII with a range of excipients gave results which depended on the excipient used and co-milling with cellulose gave samples which had an amorphous content that was stable at 10% RH for at least nine months at ambient temperature.

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Selective polymorph transformation via solvent-drop grinding

Abstract: A method of inducing specific polymorph transformations is exemplified with two single-component systems, whereby a given crystal form undergoes conversion when subjected to solid state grinding in the presence of a minor quantity of a certain solvent.

Cited by 191 publications

References 17 publications

Mechanochemistry: opportunities for new and cleaner synthesis

Mechanochemistry: opportunities for new and cleaner synthesis

Clean and Efficient Synthesis Using Mechanochemistry: Coordination Polymers, Metal-Organic Frameworks and Metallodrugs

Solid-State Transformations of Sulfathiazole Polymorphs: The Effects of Milling and Humidity

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