Reactions of  N-isocyaniminotriphenylphosphorane with α- chloroketones in the presence ofaromatic carboxylic acids proceed smoothly at room temperature and in neutral conditions toafford new disubstituted 1,3,4-oxadiazole derivatives in high yields.

The rhodium-catalyzed regio- and enantioselective amination of racemic tertiary allylic trichloroacetimidates with a variety of aniline nucleophiles is a direct and efficient route to chiral α,α-disubstituted allylic N-arylamines. We describe the first dynamic kinetic asymmetric transformations of racemic tertiary allylic electrophiles with anilines utilizing a chiral diene-ligated rhodium cata...

www.experimentjournal.com 1254 Synthesis, biological activity and docking studies of N,N'-(3S,4S)bis(3,4-disubstituted pyrrolidine)-1-sulfonamide derivatives as β-gluscosidase inhibitors Abstract Starting with L-tartaric acid the chiral 3,4-disubstituted pyrrolidine analogue sulfonamide derivatives were prepared. These compounds were examined for anti-bacterial and anti-fungal activity. Further...

A number of 3-amino-1, 2, 4-triazin-5 (2H)- ones(1) were synthesized and condensed with a-haloketones to give 2,6-disubstituted imidazo [1, 2-b] [1, 2, 4]-triazin-3 (4H)-ones (2). These compounds were reacted further with a - haloketones to yield N-alkylated products (3).

Soluble epoxide hydrolase (sEH) is a therapeutic target for treating hypertension and inflammation. 1,3-Disubstituted ureas functionalized with an ether group are potent sEH inhibitors. However, their relatively low metabolic stability leads to poor pharmacokinetic properties. To improve their bioavailability, we investigated the effect of incorporating various polar groups on the ether functio...

Reactions of N,N;-disubstituted hydrazinecarbothioamides 8a-c and substituted thioureidoethylthioureas 9a-c with 2,3,5,6-tetrachloro-1,4-benzoquinone (chloranil, 10a) and 2,3,5,6-tetrabromo-1,4-benzoquinone (bromanil, 10b) to form N,N;-disubstituted [1,3,4]thiadiazole-2,5-diamines 11a-c, 6,7-dichloro-3-substituted amino-1H-benzo[1,3,4]- thiadiazine-5,8-diones 12a-c, 2,3,7,8-tetrahalothianthrene...

The asymmetric Pictet–Spengler reaction (PSR) with aldehydes is well known. However, PSR involving ketones as electrophilic partners far-less developed. We report herein the first examples of catalytic enantioselective tryptamines α-ketoamides. A new class easily accessible prolyl-urea organocatalysts bearing a single H-bond donor function catalyzes title to afford 1,1-disubstituted tetrahydro-...