Predictive catalysis was applied to the reaction of pyridinium 1,4-zwitterionic thiolates with a copper carbene. Theoretical calculations were first performed determine suitability their annulation and make predictions about performance different salts, diazo species, derivatives. With in hand, experimental conditions optimized, scope assessed, precision evaluated. Yields up 90% obtained for sy...

Arylhydrazonomalononitriles 1a,b react with phenylhydrazine to yield amidrazones 2a,b that cyclize to give 2-aryl-5-phenylhydrazono-2,5-dihydro-[1,2,4]-triazine-6-carbonitriles 5a,b upon reaction with dimethylformamide dimethylacetal (DMFDMA). Refluxing 5a,b in glacial acetic acid resulted in the formation of the pyrazolo-1,2,4-triazines 6a,b. Compounds 6a,b were also formed upon treatment of 3...

In the title mol-ecule, C16H14N4O, the indolizine ring system is essentially planar, with a maximum deviation of 0.013 (3) Å, and forms a dihedral angle of 7.52 (12)° with the pyrazole ring. In the crystal, weak C-H⋯O hydrogen bonds and π-π stacking inter-actions, with a centroid-centroid distance of 3.6378 (16) Å, link mol-ecules along [001].

In the title compound, C(37)H(34)N(2)O(2), the pyridinone ring adopts a half-chair conformation. In the octa-hydro-indolizine fused-ring system, the piperidine ring is in a chair conformation and the pyrrole ring is twisted about the N-C(piperidine) bond. The mol-ecular structure features a weak intra-molecular C-H⋯O inter-action.

In the title compound, C(14)H(17)NO(2), the six-membered ring of the indolizine system adopts a chair conformation. In the crystal, mol-ecules form chains parallel to the b axis via inter-molecular O-H⋯O hydrogen bonds. The absolute mol-ecular configuration was assigned from the synthesis.

In the title compound, C(28)H(29)NO(3), the fused pyrrolidine and piperidine rings of the octa-hydro-indolizine unit exhibit envelope and chair conformations, respectively. The dihedral angle between the naphthalene ring system and the benzene ring is 40.37 (5)°. The crystal packing is stabilized by weak inter-molecular C-H⋯O inter-actions.

Treatment of pyridine-2-carboxaldehyde with activated alkenes such as alkyl vinyl ketones and cyclic enones in the presence of trimethylsilyl trifluoromethanesulfonate (TMSOTf) provides a novel facile one-pot synthesis of indolizine derivatives, thus for the first time describing an electrophile induced Baylis-Hillman reaction.

A direct and regioselective C1-acyloxylation of indolizines was developed via palladium-catalyzed C-H functionalization. A series of indolizines were successfully acyloxylated at the C1 position with the tolerance of a broad range of functional groups. In this reaction, high regioselectivity was achieved in the absence of a directing group. This work represents the first example of indolizine a...

The development of resistance poses a serious problem in the therapy cancer due to necessity multiple-drug and unlimited treatment affected patients. In chronic myeloid leukemia (CML), introduction imatinib has revolutionized therapy. persistence an untreatable stem cell pool other resistance-causing factors, however, also impede cure this malignancy. New therapeutic approaches are therefore es...