- Nickel-catalyzed synthesis of oxazoles via C-S activation
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The synthesis of 2-substituted oxazoles is achieved via nickel-catalyzed cross-coupling reaction of 2-methylthio-oxazole and various organozinc reagents. An extension of this method is demonstrated with a chemoselective, one-pot synthesis of unsymmetrical
- Lee, Kyoungsoo,Counceller, Carla M.,Stambuli, James P.
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supporting information; experimental part
p. 1457 - 1559
(2009/08/08)
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- Total synthesis of neooxazolomycin
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Two sides to the story: Neooxazolomycin, a member of the oxazolomycin family of antibiotics, was synthesized in naturally occurring form by a convergent approach. This highly stereoselective strategy consists of a Tamao hydrosilylation, palladium-catalyzed enolate alkenylation, dihydroxylation accompanied by lactonization, and a Nozaki-Hiyama-Kishi reaction to construct the right-hand segment as well as an improved route to the left-hand segment. (Chemical Equation Presented).
- Onyango, Evans Otieno,Tsurumoto, Joji,Imai, Naoko,Takahashi, Keisuke,Ishihara, Jun,Hatakeyama, Susumi
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p. 6703 - 6705
(2008/09/18)
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- Compounds containing a N-heteroaryl moiety linked to fused ring moieties for the inhibition of NAD(P)H oxidases and platelet activation
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The invention relates to compounds containing a N-heteroaryl moiety, which is linked via oxygen, sulfur or nitrogen, or via a methylene bridge and oxygen, sulfur or nitrogen to a fused ring moiety, in particular to the 1,2,3-triazolo[4,5-d]pyrimidine-7-yl radical. The invention also relates to a process for the preparation of said compounds and the use thereof in drugs for the treatment of NAD(P)H oxidases-related diseases and disorders and inhibition of platelet activation.
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Page/Page column 87
(2008/06/13)
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- Nematicidal trifluorobutenes
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The present invention relates to novel trifluorobutenes of the formula (I) 1wherein R1 represents hydrogen, halogen, or alkyl which may be unsubstituted or substituted with halogen, hydroxy, alkoxy, alkylthio, alkylcarbonyloxy, haloalkylcarbonyloxy or cyano, or represents alkylsulfonyloxy or represents phenyl which may be unsubstituted or substituted with halogen, alkyl, haloalkyl, alkoxy, alkylthio, alkylsulfonyl, haloalkoxy, haloalkylthio, phenyl, phenoxy, cyano or nitro. R2 represents hydrogen, halogen, or alkyl which may be unsubstituted or substituted with alkoxy or halogen, or represents alkoxycarbonyl, and n represents 0, 1 or 2, provided that if R1 represents alkyl, R2 does not represent halogen, processes for their preparation and their use as nematicides.
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- Cephalosporin derivatives, and antibacterial agents
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A compound having the formula: STR1 wherein R is a straight chain or branched chain lower alkyl, cyclic lower alkyl, lower alkenyl (except for 1-carboxy-1-vinyl), lower alkynyl, aralkyl, phenyl or 2-pyrrolidon-3-yl group which may be substituted, and Q is STR2 (wherein R1 is a hydrogen atom or an acetyl group, R2 is a hydrogen atom, a carboxyl group or a carboxymethyl group, Y is a sulfur atom or an oxygen atom, Z is a sulfur atom, an oxygen atom or an imino group which may be substituted by a lower alkyl group); or a pharmaceutically acceptable salt, physiologically hydrolyzable ester or solvate thereof.
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- PYRIDYL-ALKYLAMINOETHYLENE COMPOUNDS
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The compounds are ethylene derivatives which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A compound of this invention is 1-nitro-2-2-((4-methyl-5-imidazolyl) methylthio)ethylamino!-2-2-((3-chloro-2-pyridyl)methylthio) ethylamino!ethylene.
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- IMIDAZOLE ALKYLAMINOETHYLENE COMPOUNDS
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The compounds are ethylene derivatives which are inhibitors of histamine activity, in particular, inhibitors of H-2 histamine receptors. A compound of this invention is 1-nitro-2-methylamino-2-2-((4-methyl-5-imidazolyl)methylthio)-ethylamino!ethylene.
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- PHARMACOLOGICALLY ACTIVE THIOUREA AND UREA COMPOUNDS
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The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
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- PHARMACOLOGICALLY ACTIVE GUANIDINE COMPOUNDS
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The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-guanidines which are inhibitors of histamine activity.
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- PHARMACEUTICAL COMPOSITIONS AND METHODS OF INHIBITING H-1 AND H-2 HISTAMINE RECEPTORS
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Pharmaceutical compositions and methods of inhibiting H-1 and H-2 histamine receptors by administering an antihistamine and an H-2 histamine receptor inhibitor. Exemplary of the antihistamine in the compositions and methods of this invention is mepyramine and exemplary of the H-2 histamine receptor inhibitor is N-cyano-N'-methyl-N"-2-((4-methyl-5-imidazolyl)-methylthio)ethyl!guanidine. "
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- PHARMACEUTICAL COMPOSITIONS AND METHOD OF INHIBITING H-1 AND H-2 HISTAMINE RECEPTORS
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Pharmaceutical compositions and methods of inhibiting H-1 and H-2 histamine receptors by administering an antihistamine and an H-2 histamine receptor inhibitor. Exemplary of the antihistamine in the compositions and methods of this invention is mepyramine and exemplary of the H-2 histamine receptor inhibitor is N-methyl-N'-4-(5)-imidazolyl) butyl!thiourea.
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- PHARMACOLOGICALLY ACTIVE GUANIDINE COMPOUNDS
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The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-guanidines which are inhibitors of histamine activity.
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- PHARMACOLOGICALLY ACTIVE THIOUREA AND UREA COMPOUNDS
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The compounds are substituted thioalkyl-, aminoalkyl-and oxyalkyl-thioureas and ureas which are inhibitors of histamine activity.
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