Highly Diastereoselective One-Pot Synthesis of 4,5-Dihydrofuro[2,3-b]azocin-6-one Derivatives through Cyclization/[4+4] Annulation Reactions.

A variety of 4,5-dihydrofuro[2,3-b]azocin-6-one derivatives were expediently assembled through Au(I)-catalyzed cyclization and 2-(tert-butyl)-1,1,3,3-tetramethylguanidine (BTMG)-mediated [4+4] annulation reactions of enyne-amides and ynones. The reactions exhibit high efficiency with excellent regio- and diastereoselectivity. A broad spectrum of substrates was utilized. The products with an eight-membered ring might be useful in biological chemistry and medicinal science. Furthermore, the products could be facilely converted into various derivatives.

One-pot synthesis of 4-(imidazol-1-yl)indole derivatives through a sequential dearomatization and Ag-catalyzed cyclization/Cs2CO3-mediated addition/aromatization reaction.

A convenient one-pot assembly of 4-(imidazol-1-yl)indole derivatives from easily accessible o-alkynylanilines and imidazoles has been developed. The sequential dearomatization and Ag(I)-catalyzed cyclization/Cs2CO3-mediated conjugate addition/aromatization cascade reactions exhibit high efficiency and excellent selectivity. The combined use of a silver(I) salt and cesium carbonate is significant for facilitating this domino transformation. The 4-(imidazol-1-yl)indole products could be easily converted to the corresponding derivatives and might be valuable in biological chemistry and medicinal science.

Synthesis of Furo[2,3-e][1,4]diazepin-3-one Derivatives through Tandem Cyclization/[4 + 3] Annulation Reactions.

A variety of furo[2,3-e][1,4]diazepin-3-one derivatives were facilely synthesized through one-pot tandem cyclization/[4 + 3] annulation reactions between enynamides and α-bromohydroxamates. The reactions proceeded efficiently at room temperature, and various functional groups were well tolerated. The obtained furo[2,3-e][1,4]diazepin-3(2H)-ones containing a 7-membered dinitrogen-fused ring might be of biological and medicinal value. The products could be further derived using convenient procedures.

One-Pot Synthesis of Benzimidazo[2,1-b]thiazoline Derivatives through an Addition/Cyclization/Oxidative Coupling Reaction.

A novel and efficient approach to the synthesis of benzimidazo[2,1-b]thiazoline derivatives has been developed through an addition/cyclization/intramolecular oxidative C-H functionalization process. A variety of alkylene benzimidazo[2,1-b] thiazolines were conveniently assembled from the reaction of aryl isothiocyanate and propargylic amine in the presence of Cu(OAc)2 and PIFA at room temperature. The product could be further converted to substituted benzimidazo[2,1-b]thiazole derivatives.

One-pot synthesis of 2-azolylimidazole derivatives through a domino addition/A3 coupling/cyclization process under copper catalysis.

A novel one-pot approach for the synthesis of multi-substituted 2-imidazolylimidazoles, 2-pyrazolylimidazoles and 2-indazolylimidazoles was developed through a domino addition/A3 coupling/cyclization process under copper catalysis. A variety of aminoethyl- or hydroxylethyl-tethered 2-azolylimidazole derivatives were conveniently and efficiently assembled in one pot using N-propargylcarbodiimides, azoles, paraformaldehyde and secondary amines as starting materials. The products containing an o-iodoaryl group could be further converted to imidazo[1,2-c]imidazo[1,2-a]quinazoline derivatives through a copper-catalyzed intramolecular C-H arylation.

One-Pot Synthesis of 4-Sulfonyliminotetrahydropyrimidin-2-one Derivatives through a Copper-Catalyzed Tandem Reaction.

A novel and efficient synthesis of 4-iminotetrahydropyrimidin-2-one derivatives was developed through a Cu(I)-catalyzed three-component tandem reaction employing propargylamines, isocyanates, and sulfonyl azides as starting materials. A wide range of polysubstituted 4-sulfonyliminotetrahydropyrimidin-2-ones, which might be useful in biological chemistry and medicinal science, were conveniently and efficiently assembled in one pot.

One-pot synthesis of thiazino[2,3,4-hi]indole derivatives through a tandem oxidative coupling/heteroannulation process.

A novel and expedient one-pot synthesis of thiazino[2,3,4-hi]indole derivatives from o-haloaryl enamines and o-bromothiophenols has been developed. The tandem oxidative coupling/heteroannulation reactions exhibit high selectivity and good efficiency. The polycyclic heterocyclic products obtained might be useful in medicinal chemistry and materials science.

Crystal structure of poly[{µ3-(E)-3-[3-(carboxyl-atometh-oxy)phen-yl]acrylato-κ3O,O':O'':O'''}[µ2-3-(pyridin-4-yl)-1H-pyrazole-κ2N:N']cobalt(II)].

The title compound, [Co(C11H8O5)(C8H7N3)] n , which is based on (E)-3-[3-(carb-oxy-meth-oxy)phen-yl]acrylic acid (H2L) and 3-(pyridin-4-yl)pyrazole (pp) ligands, has been synthesized under solvothermal conditions. The dihedral angle between pyrazole and pyridine rings in the pp ligands is 23.1 (2)°. In the crystal, helical chains formed by pp and L ligands connected to the CoII atom propagate parallel to the c axis. CoII atoms of adjacent chains are bridged by the acrylic acid groups of L ligands into corrugated polymeric sheets in the ac plane.