- Triflic anhydride-mediated synthesis of oxazoles
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N-Acyl amino acid esters undergo triflic anhydride-mediated cyclodehydration to form oxazoles and bisoxazoles in a simple one-pot transformation.
- Thalhammer, Armin,Mecinovi?, Jasmin,Schofield, Christopher J.
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supporting information; experimental part
p. 1045 - 1047
(2009/05/31)
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- PYRAZOLE DERIVATIVE
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A compound represented by Formula (I): wherein Ar1 represents Formula (II): Ar2 represents a 5- or 6-membered aromatic heterocyclic group which may be substituted; and X represents Formula (III): a salt thereof, or a solvate of the compound or the salt. A potent platelet aggregation suppressant which does not inhibit COX-1 and COX-2 is provided.
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Page/Page column 66
(2010/11/27)
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- Selective inhibition of factor inhibiting hypoxia-inducible factor
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A set of four non-heme iron(II) and 2-oxoglutarate-dependent enzymes catalyze the post-translational modification of a transcription factor, hypoxia inducible factor (HIF), that mediates the hypoxic response in animals. Hydroxylation of HIF both causes it
- McDonough, Michael A.,McNeill, Luke A.,Tilliet, Melanie,Papamicael, Cyril A.,Chen, Qiu-Yun,Banerji, Biswadip,Hewitson, Kirsty S.,Schofield, Christopher J.
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p. 7680 - 7681
(2007/10/03)
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- HIV INTEGRASE INHIBITORS
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Hydroxy (tetra- or hexa-)hydronaphthyridine dione compounds of Formula (I) are inhibitors of HIV integrase and inhibitors of HIV replication wherein X1, X2, R4 and R5 are defined herein. The compounds are useful in the prevention and treatment of infection by HIV and in the prevention, delay in the onset, and treatment of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
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Page/Page column 25-26
(2008/06/13)
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- A novel [2 + 3] cycloaddition reaction: Singlet oxygen mediated formation of 1,3-dipole from iminodiacetic acid dimethyl ester and its addition to maleimides
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Sensitized photolysis of iminodiacetic acid methyl ester and maleimides follows a [2 + 3] cycloaddition pathway yielding pyrrolidine derivatives. This is similar to the photochemical reaction between C60 and amines. A series of pyrrolidine derivatives are prepared by the method including multipyrrolidines from bis- and tris-maleimide starting materials. The yields range from 13% to 85%. The reaction is highly stereoselective. All the isolated products have the 1,3-dimethoxycarbonyl groups in the cis configuration. Various sensitizers may be used with slightly different yields. A plausible mechanism is proposed that involves the singlet oxygen abstraction of two α hydrogen atoms from the iminodiacetate and formation of a 1,3-dipole with a structure similar to the classical thermally generated 1,3-dipole.
- Cheng,Gan,Shi,Wei
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p. 6369 - 6374
(2007/10/03)
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- Novel inhibitors of prolyl 4-hydroxylase. 3. Inhibition by the substrate analogue N-oxaloglycine and its derivatives
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N-Oxaloglycine (3) is an α-ketoglutarate (1) analogue that is a competitive inhibitor of prolyl 4-hydroxylase (EC 1.14.11.2). A study of the structure-activity relationships of some other oxalo derivatives shows that substitution on the glycine moiety mod
- Cunliffe,Franklin,Hales,Hill
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p. 2652 - 2658
(2007/10/02)
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