- Hydrogen Bond Directed Photocatalytic Hydrodefluorination and Methods of Use Thereof
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Methods of synthesizing compounds comprising fluorinated aryl groups are disclosed, wherein said methods utilize hydrogen bond directed photocatalytic hydrodefluorination.
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Paragraph 0182
(2021/01/22)
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- Optimization of benzyloxazoles as non-nucleoside inhibitors of HIV-1 reverse transcriptase to enhance Y181C potency
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Design of non-nucleoside inhibitors of HIV-1 reverse transcriptase with improved activity towards Tyr181Cys containing variants was pursued with the assistance of free energy perturbation (FEP) calculations. Optimization of the 4-R substituent in 1 led to ethyl and isopropyl analogs 1e and 1f with 1-7 nM potency towards both the wild-type virus and a Tyr181C variant.
- Bollini, Mariela,Gallardo-Macias, Ricardo,Spasov, Krasimir A.,Tirado-Rives, Julian,Anderson, Karen S.,Jorgensen, William L.
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p. 1110 - 1113
(2013/03/14)
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- [4,5]-fused-3,6-disubstituted-pyridazines with sulfur-containing substituents in position three for the treatment of neoplasia
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[4,5]-Fused-3,6 disubstituted-pydidazines of Formula I are useful for inducing or promoting apoptosis and for arresting uncontrolled neoplastic cell proliferation, and are specifically useful in the arresting and treatment of neoplasia: wherein Y1and Y2are independently selected from the group consisting of (CH2)n,—C(X)—NH—,—(CH2)n—C(X)—O—, and X is O or S; R1is selected from the group consisting of lower alkyl, lower alkenyl, lower alkynyl, and substituted or unsubstituted phenyl, pyridinyl, and the like; R2is selected from the group consisting of substituted or unsubstituted phenyl, benzyl, pyridinyl, and the like; “A” is a benzene ring fused with the pyridazine ring; and R3is independently selected in each instance form the group consisting of halogen, lower alkyl, and the like.
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- ORGANIC PHOSPHORUS COMPOUNDS 91. SYNTHESIS AND PROPERTIES OF 1-AMINO-2-ARYLETHYLPHOSPHONIC AND -PHOSPHINIC ACIDS AS WELL AS -PHOSPHINE OXIDES
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The preparation, physical and spectroscopic properties of 1-amino-2-arylethylphosphonic, and -phosphinic acids as well as -phosphine oxides, the phosphorus analogues of phenylalanine are described, and the reactions of 1-amino-2-(4-fluorophenyl)ethylphosphonates with acetals, isocyanides, esters, acid anhydrides, activated aromatic nitro- and halogen compounds, and with N-protected alanine are reported.It is shown that several of the 1-amino-2-arylethylphosphonic acids are strong inhibitors of PAL and anthocyanin synthesis and also are quite active botryticides.Among the active compounds were 1-amino-2-(4-fluorophenyl)ethylphosphonic acid, 3f, and the methyl-substituted compounds 3k, 3l, and 3m.The fluoroderivative 3f was also effective as a seed-dressing agent in barley showing a 100percent protection against the fungus Fusarium nivale at 600 ppm.
- Maier, Ludwig
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- Fluorine Magnetic Resonance Studies. VI. Fluorine-Fluorine Coupling Over Four Bonds in α-Fluoro- and α,α-Difluoro-toluenes
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The 4J fluorine-fluorine coupling over four bonds involving an sp3 carbon and two sp2 carbons has been studied by using constrained structures to calibrate the dependence of the size of coupling on the dihedral angle (θ).Both CF and CF2 groups follow the pattern established for CF3, with the largest couplings (38, 62 and 86 Hz respectively) arising from closest approaches of two fluorines (θ = 0 deg) and the zero couplings resulting from θ = 180 deg.
- Rae, Ian D.,Burgess, David A.,Bombaci, Sebastian,Baron, Margaret L.,Woolcock, Mark L.
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p. 1437 - 1446
(2007/10/02)
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