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Reliable and practical computational description of molecular crystal polymorphs

Journal Article · · Science Advances

Reliable prediction of the polymorphic energy landscape of a molecular crystal would yield profound insight into drug development in terms of the existence and likelihood of late-appearing polymorphs. However, the computational prediction of molecular crystal polymorphs is highly challenging due to the high dimensionality of conformational and crystallographic space accompanied by the need for relative free energies to within 1 kJ/mol per molecule. In this study, we combine the most successful crystal structure sampling strategy with the most successful first-principles energy ranking strategy of the latest blind test of organic crystal structure prediction methods. Specifically, we present a hierarchical energy ranking approach intended for the refinement of relative stabilities in the final stage of a crystal structure prediction procedure. Such a combined approach provides excellent stability rankings for all studied systems and can be applied to molecular crystals of pharmaceutical importance.

Research Organization:
Argonne National Lab. (ANL), Argonne, IL (United States); Lawrence Berkeley National Laboratory (LBNL), Berkeley, CA (United States). National Energy Research Scientific Computing Center (NERSC); Princeton Univ., Princeton, NJ (United States); Univ. of California, Oakland, CA (United States)
Sponsoring Organization:
USDOE Office of Science (SC)
Grant/Contract Number:
AC02-05CH11231; AC02-06CH11357; SC0008626
OSTI ID:
1544000
Journal Information:
Science Advances, Journal Name: Science Advances Journal Issue: 1 Vol. 5; ISSN 2375-2548
Publisher:
AAASCopyright Statement
Country of Publication:
United States
Language:
English

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Cited By (12)

Quantum mechanics of proteins in explicit water: The role of plasmon-like solute-solvent interactions journal December 2019
Polymorphism of l -Tryptophan journal November 2019
Computational polymorph screening reveals late-appearing and poorly-soluble form of rotigotine journal June 2019
Crystal-energy landscapes of active pharmaceutical ingredients using composite approaches journal January 2019
The interplay among molecular structures, crystal symmetries and lattice energy landscapes revealed using unsupervised machine learning: a closer look at pyrrole azaphenacenes journal January 2019
Revised values for the X23 benchmark set of molecular crystals journal January 2019
Overcoming the difficulties of predicting conformational polymorph energetics in molecular crystals via correlated wavefunction methods journal January 2020
Isotope effects in liquid water via deep potential molecular dynamics journal October 2019
Elastic properties of the molecular crystals of hydrocarbons from first principles calculations journal November 2019
Growth and Property Investigations of Two Organic–Inorganic Hybrid Molecular Crystals with High Thermal Stability: 4-Iodoanilinium perchlorate 18-crown-6 and 4-Iodoanilinium Borofluorate 18-crown-6 journal April 2019
Isotope Effects in Liquid Water via Deep Potential Molecular Dynamics text January 2019
Quantum Mechanics of Proteins in Explicit Water: The Role of Plasmon-Like Solute-Solvent Interactions text January 2019

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