Toxicologie

<p>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.<br></p>

<p>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.<br>References Chen, Y.; et al.: J. Am. Chem. Soc., 140, 8781 (2018);<br></p>

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

<p>Applications 4-(2-Propyn-1-yloxy) Trimethoprim is an analog of T795615, which is an antibacterial compound and a contaminant of emerging concern (CECs).<br>References Manius, G.J., et al.: Anal. Profiles Drug Subs., 7, 445 (1978), Roth, B., et al.: J. Med. Chem., 23, 379 (1980), Brogden, R.N., et al.: Drugs, 23, 405 (1982),<br></p>

<p>Applications Ganciclovir derivative.<br>References Albers, E., et al.: J. Pharm. Sci., 81, 756 (1992), Dias, C., et al.: J. Pharm. Sci., 91, 6607 (2002), Macha, S., et al.: Drug Metab. Dispos., 30, 670 (2002),<br></p>

<p>Applications Used in the preparation of triazole antifungal agents.<br></p>

<p>Applications α-[2-[Methyl(1-naphthalenylmethyl)amino]ethyl]-Benzenemethanol is an impurity of naftifine (N213100) an antifungal.<br>References Stuetz, A., et al.: Journal of Medicinal Chemistry, 29, 112 (1986)<br></p>

<p>Applications β-Amyrin is used as a protein tyrosine phosphatase 1B inhibitor with potential treatment towards diabetes. Also used in the synthesis of HIV-1 integrase inhibitory compounds based upon plant extracts.<br>References Zhang, Y. et al.: Bioorg, Med. Chem., 16, 8697 (2008); Tewtrakul, S. et al.: Phytother. Res., 17, 232 (2003);<br></p>

<p>Impurity Fluconazole EP Impurity B / Fluconazole USP Related Compound A<br>Applications 4-Defluoro-4-(1H-1,2,4-triazol-1-yl) Fluconazole (Fluconazole EP Impurity B) is an impurity of the antifungal agent Fluconazole (F421000).<br>References Ramesh, B. et al.: J. Pharm. Res., 4, 1401 (2011); Al-Rimawi, F.: Jor. J. Chem., 4, 357 (2009);<br></p>

<p>Applications Desmethylene seco-Benzoxadiazine Marbofloxacin is an impurity of Marbofloxacin (M197000); a fluorinated quinolone antibacterial.<br>References Gruet, P., et al.: Vet. Rec., 140, 199 (1977); Lefebvre, H.P., et al.: J. Vet. Pharmacol. Ther., 21, 453 (1998)<br></p>

<p>Applications cis-2-(2,4-Dichlorophenyl)-2-(1H-imidazol-1-ylmethyl)-1,3-dioxolane-4-methanol Benzoate (Ester) is an intermediate in the synthesis of trans-2-​(2,​4-​Dichlorophenyl)​-​2-​(1H-​imidazol-​1-​ylmethyl)​-​1,​3-​dioxolane-​4-​methanol (D431560). trans-2-​(2,​4-​Dichlorophenyl)​-​2-​(1H-​imidazol-​1-​ylmethyl)​-​1,​3-​dioxolane-​4-​methanol is an impurity of Ketoconazole (K186000).<br>References Ryu, J., et al. Bull. Korean Chem. Soc., 24, 460 (2003)<br></p>

<p>Applications Methoxy Cefadroxil is an impurity of Cefadroxil (C235750), a semi-synthetic cephalosporin antibiotic. Antibacterial.<br>References Buck, R.E., et al.: Antimicrob. Agents Chemother., 11, 324 (1977);<br></p>

<p>Applications N-Desdecanoyl, N-(Undecanoyl) Dapotmycin is an impurity of Daptomycin (D193350), cyclic lipopeptide antibiotic derived from a fermentation product of Streptomyces roseosporus; disrupts plasma membrane function in gram-positive bacteria. Antibacterial.<br>References Allen, N.E., et al.: Antimicrob. Agents Chemother., 31, 1093 (1987), Tully, F.P., et al.: Expert Opin. Invest. Drugs, 8, 1223 (1999),<br></p>

<p>Applications rel-(R*,R*)-Bicalutamide Sulfoxide is an diastereomeric bicalutamide (B382000) derivative.<br>References Li, Wei., et al.: Chirality., 21, 578 (2009);<br></p>

<p>Applications D-2'-Deoxyribopyranosyl-3-guanylurea (α/β-Mixture) can be obtained from 5-Aza-2’-deoxy Cytidine (A796950) which can be used as cancer treatment, in particular to inhibit the growth of pancreatic endocrine tumor cell lines.<br>References Deng, T., et al.: Life Sci., 84, 311 (2009), Horne, H., et al.: Mol. Cancer Res., 7, 199 (2009), Zinner, R., et al.: Mol. Cancer Ther., 8, 521 (2009),<br></p>

<p>Stability Light Sensitive<br>Applications Prifinium Bromide is a synthetic antispasmodic drug; parasympatholytic. Prifinium Bromide is used as a quartenary anticholinergic agent.<br>References Kumada, S. et al.: Arzneim.-Forsch., 20, 237 (1970); Nakai, T. et al.: Arzneim.-Forsch., 20, 1112 (1970); Bettini, V. et al.: Farm. Ed. Prat., 33, 392 (1978);<br></p>

<p>Stability Hygroscopic<br>Applications The hydrochloride salt of AZ 5104 (A795170), which is a derivative of AZD 9291 (A808075) and a selective EGFR inhibitor (epidermal growth factor receptor), used in the treatments of nonsmall-cell lung cancer (NSCLC).<br>References Finlay, M.R.V., et al.: J. Med. Chem., 57, 8249 (2014);<br></p>

<p>Applications 5-Allylidene-10,11-dihydro-5H-dibenzo[a,d][7]annulene is an impurity of Nortriptyline (N837000) and Amitriptyline (A552600), both of which are antidepressant.<br>References Hale, J. L., et al.: Anal. Profiles Drug Subs., 1, 233 (1972); Rubin, E.H., et al.: J. Clin. Psychiatry, 46, 418 (1985); Blessel, K.W., et al.: Anal. Profiles Drug Subs., 3, 127 (1974); Tobe, A., et al.: Arzneim.-Forsch., 31, 1278 (1981)<br></p>

<p>Applications The minor metabolite of Deflazacort.<br>References Bernareggi, A., et al.: J. Pharma. Biomed. Anal., 5, 177-81 (1987), Assandri, A., et al.: Xenobiotica, 13(3), 185 (1983), Martinelli, E., et al.: Drug Metab. Dispos., 7, 335 (1979),<br></p>

<p>Applications 2,6-Dimethoxybenzoyl Chloride is used in the synthesis of penicillins and cephalosporins.<br> Not a dangerous good if item is equal to or less than 1g/ml and there is less than 100g/ml in the package<br>References Newall, C. et al.: Comp. Med. Chem., 2, 609 (1990); Kanao, M. et al.: J. Med. Chem., 25, 1358 (1982);<br></p>