Synthesis and antimicrobial activity of new (4,4,4-trihalo-3-oxo-but-1-enyl)-carbamic acid ethyl esters, (4,4,4-trihalo-3-hydroxy-butyl)-carbamic acid ethyl esters, and 2-oxo-6-trihalomethyl-[1,3]oxazinane-3-carboxylic acid ethyl esters

N -Alkylation of 4-Trichloromethylpyrimidinones: Synthesis of Some New and Interesting Modified Nucleoside Analogues

“…In this report, a modified procedure using a large excess (5-10 times) of the primary amines in acetonitrile was carried out and an unexpected result was found. Instead of the Michael addition of the amines followed by the elimination of the alkoxy group, as is usually observed for parent enones, [41][42][43][44][45][46][47][48][49] the substitution of the CCl 3 group by the primary amines also occurred simultane- Figure 3. So far, no evidence of such a double-substitution has been observed for trichloro-or trifluoromethylated enones.…”

Synthesis of Oxazinanones: Intramolecular Cyclization of Amino Acid-Derived Diazoketones via Silica-Supported HClO4 Catalysis

“…Some important examples are the anti-HIV drug Efavirenz (Staszewski et al, 1999) and the potent anticancer agent Maytansine (Rao et al, 1979) and its synthetic derivatives Maytansinoid (Blanc et al, 2011) and Ansamitocin P3 (Taft et al, 2012). Other significant biological activities described for this class of compounds are: antibacterial (Zanatta et al, 2006; Wang, 2008), anti-influenza (Kuznetsov et al, 2017), anti-inflammatory (Ullrich et al, 2004), antidiabetes [11β HSD1 inhibitor (BI 135585)] (Zhuang et al, 2017), antithrombotic (Jin and Confalone, 2000), antialzheimer (Fuchs et al, 2007), and enzyme inhibiting [(Latli et al, 2017); Figure 1]. Furthermore, they are extensively used as valuable synthetic intermediates in fine chemicals (Woodward et al, 1981; Wang et al, 1982; Hilborn et al, 2001; Takahata et al, 2002; Wang and Tunge, 2006), cosmetics (Zofchak, 2003), and pesticides (Hino et al, 2008).…”