Toxicology

Applications 2-Iodo-4-(1-methylethyl)-6-(trifluoromethyl)pyrimidine is a pyrimidine compound, generally used in the synthesis of pharmaceutical compounds, it may be used in the synthesis of cycloindoles for the treatment of hepatitis C.

Applications Sofosbuvir 3',5'-Bis-(S)-phosphate is an impurity of PSI-7977 (P839640), a prodrug that is metabolized to the active antiviral agent 2'-deoxy-2'-α-fluoro-β-C-methyluridine-5'-monophosphate and is currently being investigated in phase 3 clinical trials for the treatment of hepatitis C. Studies have profiled PSI-7977 as a nucleotide inhibitor of hepatitis C virus, exerting selective inhibitory effects towards HCV NS5B polymerase.
References Lam, A.M.,et al.: Antimicrob. Agents. Chemotherapy., 56, 3359 (2012); Lam, A.M., et al.: J. Virol., 85, 12334 (2011); Sofia, M.J., et al.: J. Medn. Chem., 53, 7202 (2010)

Applications (1R,​4S)​-3-​Oxo-2-​azabicyclo[2.2.1]​hept-​5-​ene-​2-​carboxylic acid 1,​1-​Dimethylethyl Ester is an intermediate in synthesizing ent-Abacavir (Abacavir EP Impurity A) (A105015), an enatiomer of Abacavir (A105000). Abacavir is a carbocyclic 2'-deoxyguanosine nucleoside reverse transcriptase inhibitor and an anti-HIV drug used to treat HIV infection (1). Intracellular enzymes convert Abacavir to its active form, carbovir-triphosphate (CBV-TP), which then selectively inhibits HIV reverse transcriptase by incorporating into viral DNA (2). Abacavir is metabolized in the liver by uridine diphosphate glucuronyltransferase and alcohol dehydrogenase resulting in inactive glucuronide and carboxylate metabolites, respectively.

Applications 5-Amino-1-N-methylindole (CAS# 102308-97-4) is an indole derivative and building block, used in the copper-catalyzed synthesis of sulfonamides.
References Chen, Y.; et al.: J. Am. Chem. Soc., 140, 8781 (2018);

Applications 2-methoxy-3-pyridinesulfonyl chloride is patented as a reactant used to prepare erythromycin macrolide antibiotics as antibacterial and antiprotozoal agents.

Applications U 75875, is a peptidomimetic inhibitor, that inhibits HIV-1 gag-pol protein. In human peripheral blood mononuclear cells and in a continuous cell line, U-75875 completely blocked HIV replication, so it can be used as therapeutic potential of protease inhibitors for treatment of HIV infection.
References Ashorn, P., et al.: Proceedings of the National Academy of Sciences of the United States of America, 87, 7472 (1990);

Applications 12β-Deoxycholic Acid Methyl Ester 3α-Benzoate is an intermediate in the synthesis of 3α,12β-Dihydroxycholanoic Acid is a bile acid that may decrease of the toxic effects of deoxycholic acid on lipid peroxidn.
References Hino, A., et. al.: J. Biochem., 129, 683 (2001)