Abstract We report the synthesis of 4‐aryl‐2‐piperidone, 4‐arylpiperidine motifs, antituberculosis molecule Q203 (Telacebec) and its analogues. Direct lactamization β ‐C−H arylated N ‐phthaloyl δ ‐aminopentanoic acid carboxamides yielded 4‐aryl‐2‐piperidone (4‐aryl‐ ‐valerolactam) scaffolds. The required were assembled via Pd(II)‐catalyzed, 8‐aminoquinoline‐aided, sp 3 activation arylation meth...

Preparations of N-[3-(hetero)aryl-aminocarbonyl]propanoyl-L-proline derivatives 12, 13, 22 and 23 are described. A novel approach consists of fusing (80-100 °C) N-(hetero)aryl-succinimides (7, 8, 20, 21) with unprotected L-proline and imidazole in the presence of dimethylformamide. In vitro tests for angiotensin converting enzyme (ACE) inhibition showed that all N-(arylaminocarbonyl)-propanoyl-...

In the crystal structure of the title compound, [Co(C(12)H(8)N(2))(3)](BF(4))(2)·CH(3)CN, the mol-ecular packing involves dimers of distorted octahedrally coordinated cations which are held together by one π-π [centroid-centroid = 3.542 (4) Å] and two C-H⋯π inter-actions [2.573 (4) Å] resulting in a P4AE (Parallel Fourfold Aryl Embrace) motif. The anions are found in aryl boxes formed from the ...

The title compound, C(46)H(24)F(12)O(8)·C(4)H(8)O, consists of a cyclic aryl ester dimer and a tetra-hydro-furan mol-ecule. In the structure of the cyclic dimer, one carbonyl group stretches above the cavity and the other below.

Z. Naturforsch. 56 b, 1172-1177 (2001); received July 13, 2001 Aryl Formates, Formylation, Hydroxyarenes Aryl formates 4a-u, 6 , 8 , 10, 12, 14, 16, 18, 20, 22, 24, 26 are prepared by formylation of hydroxyarenes 3a-u, 5, 7, 9, 11, 13, 15, 17, 19, 21, 23, 25 with /V,Af-diformylacetamide (1) or triformamide (2), respectively, in fairly good yields. The reactions can be catalyzed by sodium diform...

The asymmetric unit of the title compound, C(12)H(12)O(5)P(2), contains four independent mol-ecules, generating two dimers via pairs of inter-molecular O-H⋯O hydrogen bonds, forming R(2) (2)(8) rings. The two aryl rings of each mol-ecule form dihedral angles of 108.6 (1), 103.2 (1), 12.5 (2) and 8.1 (2)° in the four mol-ecules.

Toll-like receptors (TLRs) are pattern recognition receptors that recognize specific molecular patterns present in molecules that are broadly shared by pathogens but are structurally distinct from host molecules. The TLR7-agonistic imidazoquinolines are of interest as vaccine adjuvants given their ability to induce pronounced Th1-skewed humoral responses. Minor modifications on the imidazoquino...

In the title compound, C(12)H(8)F(2)O(2)S, which is a precursor of functionalised poly(aryl-ene ether sulfone) polymers, the dihedral angle between the aromatic ring planes is 84.43 (8)°. In the crystal structure, aromatic π-π stacking [centroid-centroid separations = 3.808 (3) and 3.867 (3) Å] helps to establish the packing. A short C-H⋯F contact also occurs.