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The authors combined liquid-assisted grinding with MicroED to characterize olanzapine molecular salts that had resisted suitable single-crystal growth. The approach also identified minor impurity structures within bulk solids. This pharmaceutical example links mechanochemical preparation to structure determination, while showing that crystallinity alone does not guarantee success with conventional single-crystal X-ray analysis.
The authors incorporated multiple-scattering effects into continuous-rotation 3D electron diffraction refinement. Comparisons across 12 compounds improved structural models, and absolute-structure assignments were evaluated using 58 crystals of nine chiral compounds. The work provides a methodological basis for stereochemical assignment; its benchmark does not establish a universal success rate for pharmaceutical samples.
The crystal structure of levocetirizine dihydrochloride was determined by 3D ED/MicroED from crystalline powder extracted from commercially available tablets. Dynamical refinement also supported its absolute configuration. The study provides an example of identifying and characterizing an API within a microcrystalline mixture, without requiring the growth of large single crystals or implying that every formulated product is equally accessible.
This review connects advances in MicroED with examples spanning small molecules, peptides, and protein structures relevant to drug discovery. It explains how nanocrystalline material changes the range of accessible structural problems and surveys representative applications. The article is a guide to the evolving evidence base, rather than a new validation study or a general claim of routine success for every pharmaceutical sample.
This study combined virtual screening of chiral probes, experimental cocrystal screening, and MicroED structure determination to assign absolute configuration for two marketed API molecules. Known probe stereochemistry anchors the assignment. The workflow offers a route around difficult large-crystal growth while retaining an experimental screening step; computational propensity predictions alone do not establish absolute configuration.
Researchers determined the structures of five vemurafenib polymorphs directly from compact spherulites using 3D electron diffraction. Three matched known single-crystal X-ray structures, while the method resolved a difficult delta form and a newly observed epsilon form. The work expands access to melt-grown polymorphs whose morphology or instability can frustrate conventional single-crystal analysis.
MicroED determined a powder-derived cocrystal of 2-aminopyrimidine and succinic acid prepared by solid-state grinding. The mechanically generated phase was not accessible through the solution-crystallization route examined. This is a model organic cocrystal rather than an API efficacy study, illustrating how electron diffraction can characterize crystal-engineering products without first recreating them as large solution-grown crystals.
Researchers analyzed micron-sized powders of SMTP-7 and its diastereomer to resolve stereochemical assignments. Kinematical refinement combined with additional chiral information and dynamical refinement provided complementary routes. The work demonstrates absolute-configuration analysis for complex, hard-to-crystallize drug candidates with limited material, while distinguishing what can be inferred from conventional refinement and what requires dynamical treatment.
This review examines three-dimensional electron diffraction for beam-sensitive small-molecule nanocrystals, with a pharmaceutical-industry perspective. It discusses experimental strategies, diffraction completeness, dynamical scattering, and structural applications that extend beyond conventional large-crystal requirements. It provides a methods-oriented framework for interpreting published demonstrations; it does not establish a universal preparation method or replace sample-specific feasibility assessment.
Three-dimensional electron diffraction and scanning transmission electron microscopy resolved the layered structure and stacking variations of bismuth subsalicylate, a long-used pharmaceutical ingredient. Clustering compatible diffraction datasets helped obtain the ordered structural model, while imaging exposed disorder. The paper shows why complementary electron-crystallography techniques can be valuable when small crystals and structural defects obstruct conventional characterization.
The authors determined the absolute configuration of a preclinical API by forming a salt with a chiral reference and analyzing its microcrystalline powder using MicroED. This approach transfers known stereochemical information from the salt former to the API. It addresses situations where large crystals cannot be obtained, but depends on a suitable, well-characterized chiral reference.
The 2022 study delivered CAR-encoding mRNA with CD5-targeted lipid nanoparticles, generating transient CAR T cells in mice. The abstract reports reduced cardiac fibrosis and improved function after injury. This is preclinical evidence, not human efficacy.
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