The author of 《Cocrystals of Leflunomide: Design, Structural, and Physicochemical Evaluation》 were Cadden, Joseph; Klooster, Wim T.; Coles, Simon J.; Aitipamula, Srinivasulu. And the article was published in Crystal Growth & Design in 2019. Synthetic Route of C6H5NO2 The author mentioned the following in the article:
The use of cocrystn. as a tool to improve the pharmaceutical profile of the low-solubility drug leflunomide, used in the treatment of arthritis, is herein evaluated. Judicious selection of coformers based upon knowledge-based strategy and crystal engineering principles resulted in new cocrystals with pyrogallol, 3-hydroxybenzoic acid, 2-picolinic acid, and 2-aminopyrimidine. Characterization and structure determination of these systems were performed using x-ray diffraction. Crystal structure anal. revealed that the H bonding in the crystal structures corroborates well with the knowledge-based prediction tool. Physicochem. properties such as thermal behavior, stability, solubility, and dissolution rate of the pharmaceutically acceptable cocrystals were evaluated to assess their impact on the pharmaceutical profile of leflunomide. When compared with their parent compound leflunomide and the phys. mixtures, cocrystals exhibit improved physicochem. properties, showing their potential for development of new solid dosage forms. In the experiment, the researchers used many compounds, for example, Picolinic acid(cas: 98-98-6Synthetic Route of C6H5NO2)
Picolinic acid(cas: 98-98-6) is used in the preparation of 2-Aminodihydro[1,3]thiazines as BACE 2 inhibitors and their preparation and use in the treatment of diabetes.Synthetic Route of C6H5NO2