pyrazine derivatives are important class of compounds with diverse biological and cytotoxic activities and clinical applications. in this study, b3 p 86 / 6 – 31 + + g * was used to compute and map the molecular surface electrostatic potentials of a group of substituted amides of pyrazine-2-carboxylic acids to identify common features related to their subsequent cytotoxicities. several statisti...

zn/acoh on silica gel converts a range of structurally different sulfoxides to their corresponding thioethers in excellent yields under microwave irradiation. it has been found that chemoselective deoxygenation of sufoxides can be achieved in the presence of other reducible functional groups such as acetals, acids, amides,   esters, ketones and nitriles.

Oximes are highly crystalline materials and oximation is very efficient method for characterization and purification of carbonyl compounds. These compounds not only represent a useful series of derivatives of carbonyl compounds but also may be used as intermediates for the preparation of amides by the Beckmann rearrangement [1], nitrones [2], hydroximinoyl chlorides, nitrile oxide [3] and chi a...

Previously, we reported the Hsp90 inhibitory activity of radamide, an open chain amide chimera of geldanamycin and radicicol. Attempts to further expand upon structure-activity relationships for this class of Hsp90 inhibitors led to the preparation of a series of radamide analogues focused on differing tether lengths and quinone mimics. In addition, the cup-shaped conformation adopted by the tw...

The reaction of tertiary, secondary and benzylic alcohols with different nitriles in the presence of alumina-methanesulfonic acid (AMA) as a new reagent affords the corresponding amides in good yields (Table 1, 2). Conversion of 2,6-bis(hydroxymethyl)-4-halo anisoles into corresponding diamides in the range of 68-76% yields (Table 3) are also included in this paper.

A self-condensation cyclization reaction mediated by phosphorus pentoxide (P2O5) and catalyzed by zinc bromide (ZnBr2) is presented for the synthesis of polysubstituted 4-pyridones and 2-pyridones from β-keto amides. A variety of β-keto amides are used in this approach, and a wide range of functionalized 4-pyridones and 2-pyridones were obtained in good to excellent yields. When employing the N...

Secondary amides can be reduced by silane HSiMe2Ph into imines and aldehydes by a two-stage process involving prior conversion of amides into iminoyl chlorides followed by catalytic reduction mediated by the ruthenium complex [Cp(i-Pr3P)Ru(NCCH3)2]PF6 (1). Alkyl and aryl amides bearing halogen, ketone, and ester groups were converted with moderate to good yields under mild reaction conditions t...

Because of the importance of developing stereoselective syntheses for single enantiomers, a selected panel of racemic biologically active 1-aryl- and 1-heteroarylpropan-2-amines has been prepared, followed by a study of their behavior in enzymatic kinetic resolution (KR) processes. For this purpose, lipase B from Candida antarctica (CAL-B) proved to be an ideal biocatalyst allowing the preparat...