An asymmetric normal-electron-demand aza-Diels-Alder cycloaddition of 2-aryl-3H-indol-3-ones and 2,4-dienals was explored via trienamine catalysis of a chiral secondary amine. Multifunctional tricyclic polyhydropyrido[1,2-a]indoles were efficiently constructed in good stereoselectivity (up to 92% ee, >19 : 1 dr).

Chiral N-heterocyclic carbenes were found to be efficient catalysts for the formal [2+2] cycloaddition reaction of alkyl(aryl)ketenes and nitroso compounds to give the corresponding 1,2-oxazetidin-3-ones in moderate to good yields with high enantioselectivities. Reductive ring-opening of the oxazetidinones give the corresponding α-hydroxy acid derivatives in good yields.

A direct oxidative cross-dehydrogenative coupling (CDC) of N-aryl tetrahydroisoquinolins with 5H-oxazol-4-ones catalyzed by CuBr using air as the only oxidant has been developed, which could also proceed smoothly under a metal-free oxidative system with PhI(OAc)2 as the oxidant. A series of alkylated tetrahydroisoquinolin derivatives were obtained in good yields and excellent diastereoselectivi...

Reaction of the doubly-bridged biscyclopentadienes (C5H4(EMe2))(C5H4(SiMe2)) (E = Si(1a), or C(1b)) with Re2(CO)10 in refluxing mesitylene gave the corresponding dirhenium carbonyl complexes [(η(5)-C5H3)2(EMe2)(SiMe2)][Re(CO)3]2 (trans-2a,b and cis-2a,b), and the desilylated products [(η(5)-C5H4)2(EMe2)][Re(CO)3]2 (3a,b). Photolysis of trans-2a,b with a series of aryl halides in benzene results...

Compounds containing aryl/heteroaryl acetic acid and aryl/heteroaryl ethylamine cores play important roles in the pharmaceutical field. Compounds containing aryl/heteroaryl acetic acid units form a large group of non-steroidal anti-inflammatory drugs such as Indomethacin [1], Diclophenac [2], Sulindac [3], Ketorolac [4], and many others. Also, this subunit appears in a number of antifungal [5],...

today, the bidentate ligands 3-hydroxypyridin-4-ones (hpos) as orally active iron chelating agents have been demonstrated to possess potential for treatment of some human diseases such as iron-overload in thalassaemic patients and malaria. in this research, a series of hpos with different substitutes and position were theoretically invest

7 ABSTRACT: β-Amino acids are emerging as an important class of 8 compounds in medicinal chemistry. β-Aryl-β-alanines show antiepilepto9 genesis activity, while others have been used to synthesize antibiotic β10 peptides. To assess the utility of a methylidene imidazolone-dependent 11 Pantoea agglomerans phenylalanine aminomutase (PaPAM) for making 12 non-natural β-amino acids, we surveyed the ...