Registration Number
0221U105841,
0120U104907
, R & D reports
Title
Study of polymorphic transitions of molecular crystals for the needs of the pharmaceutical industry.
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Head
Shyshkina Svitlana V.,
Registration Date
06-09-2021
Organization
State Scientific Institution Scientific and Technological Complex" Institute of Single Crystals "of the National Academy of Sciences of Ukraine
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The polymorphic transition of a benzothiasine derivative (analogue of pyroxicam) from a monoclinic structure in triclinic one for four weeks after grinding is studied. The monoclinic polymorph crystallizes from a more volatile solvent, has a layered structure and exhibits high anti-diuretic and analgesic activity. Polymorphic transition occurs solely as a result of orientational factors and leads to loss of biological activity.
For 3- (1- (tert-butoxycarbonyl) azetidine-3-yl) -1,2-oxazol-4-carboxylic acid, a polymorphic transition as a result of grinding occurs due to conformational and orientational factors. The prerequisite for the transition is the high conformational flexibility of the molecule, low barriers of nitrogen inversion and rotation of the substituents around the single bonds, as well as the ability of the carboxyl group to form two types of supramolecular synthons. Polymorphic modifications are constructed from molecular (metastable structure) or dimeric (stable structure) building units.
Product Description
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2021-09-06
