Nitrogen (N) Containing Building Blocks

Applications 2,3-Piperazinedione is a metabolite of Ketoconazole (K186000), a broad-spectrum antifungal drug that inhibits steroid synthetic pathways and is used to treat patients with seborrheic dermatitis.
References Brown, M., et al.: Clin. Pharm. Ther., 37, 290 (1985); Edlund, P. & Baranczewski, P.: J. Pharm. Biomed. Anal., 34, 1079 (2004); Skinner Jr., R., et al.: J. Am. Acad. Derm., 12, 852 (1985); Trachtenberg, J., et al.: J. Urology, 130, 152 (1983)

Applications 2Z-Nalfurafine is a geometric isomer of Nalfurafine (N255600), a on-narcotic opioid drug for intractable itch caused by hemodialysis. It showed significant opioid κ-agonist activity and induced neither aversion nor preference in rats on the CPP (Conditioned Place Preference) test. Nalfurafine is a new therapeutic agent for the treatment of uremic pruritus in hemodialysis patients.
References Fujii, H., et al.: Bioorg. Med. Chem., 12, 4133 (2004); Mori, T., et al.: Life Sci., 75, 2433 (2004); Fujii, H., et al.: Curr. Med. Chem., 13, 1109 (2006); Nagase, H., et al.: Bioorg. Med. Chem. Lett., 20, 6302 (2010)

Applications N-Methylacetoacetamide is a starting material in the synthesis of 1-Carbamoyl-2-oxopropyl acetate with the aid (diacetoxyiodo)benzene (DIB) as the oxidant. Also, it is a reagent used in the synthesis of 10H-Phenothiazines, which possesses for their biological activity against the regulatory enzymes involved in inflammatory diseases.
References Liu, W., et al.: Beilstein J. Org. Chem., 7, 1436-1440 (2011); Sadanandam, Y. S., et al.: Eur. J. Med. Chem., 44, 197-202 (2009)

Applications 2-​Aminoindan-​2-​carboxylic Acid can be used as a potential tyrosine hydroxylase inhibitor.
References Pinder, R., et al.: J. Med. Chem., 14, 892 (1971)

Applications Reagent used for asymmetric syntheses.
References Schlessinger, R., et al.: J. Org. Chem., 28, 3070 (1986)