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Crystal Structure and Physicochemical Properties of the Crystalline Form of a Novel 15-membered Azalide Derivative

Objective

  • To prepare and characterize the crystalline form of  2’-O-{3-[(7-chloro-4-quinolinyl)amino]propyl}-9-deoxo-9a-methyl-9a-aza-9a-homoerythromycin A, a novel 15-membered azalide

Single crystal structure determination

           1     

Solid state characterisation

XRPD

DVS

DSC

TGA

Summary

  • On the basis of a limited crystallization screen acetonitrile was selected as solvent of choice.
  • Crystalline material was obtained on 10 mg scale as well as on 30 g scale in high yield (86.9%) and purity (98.9%).
  • According to the solved crystal structure, XRPD, DSC, TGA  and DVS analyses, 1 exists as a non-solvated, non-hydrated and non-hygroscopic crystalline form.

References

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