Matsuura, S.; Igarashi, K.; Azuma, M.; Ooshima, H. The Solid-Phase Transition of Carbapenem CS-023 Polymorphs and the Change in Helicity Observed in the Transition. Crystals2024, 14, 71.
Matsuura, S.; Igarashi, K.; Azuma, M.; Ooshima, H. The Solid-Phase Transition of Carbapenem CS-023 Polymorphs and the Change in Helicity Observed in the Transition. Crystals 2024, 14, 71.
Matsuura, S.; Igarashi, K.; Azuma, M.; Ooshima, H. The Solid-Phase Transition of Carbapenem CS-023 Polymorphs and the Change in Helicity Observed in the Transition. Crystals2024, 14, 71.
Matsuura, S.; Igarashi, K.; Azuma, M.; Ooshima, H. The Solid-Phase Transition of Carbapenem CS-023 Polymorphs and the Change in Helicity Observed in the Transition. Crystals 2024, 14, 71.
Abstract
The poor solvent crystallization of carbapenem CS-023 has been performed at 25 °C. The following results have been obtained: 1) A solvate crystal Form A (5/2 Ethanol·1/2 H2O) is recovered from 80 v/v% ethanol solution, 2) Form A transforms to Form H (4H2O) by the solid-phase transition through the solvate-free polymorph, Form A-2, and Form A also transformed to Form C (1Ethanol·3H2O) by the solvent-mediated transformation. In the present study, we found that Form C also transforms to Form H by the solid-phase transition through the solvate-free polymorph, Form C-2. The three polymorphs, Form A, H, and C, were composed of the helical-chain structures, respectively. However, there was an incomprehensible affair in the solid phase transition among the three polymorphs. Namely, Form A comprised a left-handed helix.On the other hand, Form C and Form H’s helix chains were in a left- and right-handed helix complex. The solid-phase transition of Form A into Form H suggested the switch of helicity in the solid. We attempted to explain the helicity change in the solid phase transition. As a result, it was suggested that the over-absorption of water of Form A-2 at high humidity plays a vital role in the helicity change.
Keywords
antibiotics; carbapenem; pharmaceutical crystallization; polymorphism of carbapenem crystal; solid phase polymorphic transition; helicity change, over-absorption of water of anhydrous crystal
Subject
Engineering, Chemical Engineering
Copyright:
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