We report an enantioselective Ni-catalyzed cross coupling of arylzinc reagents with pyridiniumions formed in situ from pyridine and a chloroformate. This reaction provides enantioenriched 2-aryl-1,2-dihydropyridine products that can be elaborated to numerous piperidine derivatives with little or no loss in ee. This method is notable for its use of pyridine, a feedstock chemical, to build a vers...

In order to study the effect of heterocyclic core conformational state of leucamide A on its anti-influenza virus A activity, five conformational analogues were prepared by replacing the Pro-Leu dipeptide in the molecule with various amino acids. The amino acids used were of 2 to 6 carbons. The results showed that these replacements not only changed the conformational relationship between the 4...

In the title compound, C(32)H(26)BN(5) or [(C(14)H(11)N(5))B(C(6)H(5))(3)], the B atom is approximately tetra-hedrally coordinated. The diazo unit is in a trans conformation, which is generally more stable than a cis one for aromatic azo compounds. The crystal structure features very weak C-H⋯π inter-actions. The dihedral angles between the central benzene ring and the terminal rings in the het...

In the title compound, C(21)H(19)NO(2), the six-membered heterocycle assumes a screw-boat conformation. The phenyl ring is oriented with respect to the pyrrole ring at a dihedral angle of 64.76 (10)°. An intra-molecular C-H⋯O hydrogen bond helps to stabilize the mol-ecular structure. There are weak C-H⋯π inter-actions between inversion-related mol-ecules in the crystal.

The copper(II) atom in the title compound, [Cu(C(5)H(10)NS(2))I(C(12)H(8)N(2))], is chelated by the N-heterocycle and the dithio-carbamate anion in a slightly distorted tetragonal coordination. The tetragonal-pyramidal coorination is completed by the iodine atom in the apical position. One ethyl group is disordered over two positions with site occupancies of 0.31 (2) and 0.69 (2).

The title compound, C(7)H(7)N(11)O(11) (PNMFIW), is a caged heterocycle substituted with five nitro and one formyl groups. It is related to the hexa-azaisowurtzitane family of high-density high-energy polycyclic cage compounds. Four nitro groups are appended to the four N atoms of the two five-membered rings, while a nitro group and a formyl are attached to the two N atoms of the six-membered r...

Importance of DNA-Damaging Cytotoxins. DNAdamaging agents have historically played a central role in cancer therapy (1). Even as new approaches to cancer therapy become available, it seems likely that there will be a continued need for the study and development of novel DNA-damaging cytotoxins. These agents will see continued use due to their well-established role in treating various types of c...

A straightforward and reliable method for the regioselective synthesis of steroidal 1,4-disubstituted triazoles and 1,5-disubstituted tetrazoles via copper(I)-catalyzed cycloadditions is reported. Heterocycle moieties were efficiently introduced onto the starting azide compound 3β-acetoxy-16β-azidomethylandrost-5-en-17β-ol through use of the "click" chemistry approach. The antiproliferative act...