Analogs of cortistatins, a series of anti-angiogenic compounds isolated from the Indonesian marine sponge Cortisium simplex, were synthesized from estrone by using the Suzuki-Miyaura coupling reaction as the key step. The estrone-isoquinoline hybridized compound showed selective inhibitory activity against the proliferation and VEGF-induced migration of HUVEC.

In the title compound, C(19)H(21)NO(4), an organocatalyst with a tetra-hydro-isoquinoline backbone, the heterocyclic ring assumes a half-boat conformation. The dihedral angle between the aromatic rings is 82.93 (8)°. In the crystal, mol-ecules are linked via N-H⋯O and C-H⋯O hydrogen bonds, forming a layer parallel to (10[Formula: see text]).

The rhodium-catalyzed intramolecular direct arylation of imidazole and benzimidazole derivatives via double C-H bond activation is described. This approach provides new access to a wide range of imidazo and benzimidazo[2,1-a]isoquinoline derivatives in moderate to high yields. This reaction provides an alternative method to the known Pd-catalyzed intramolecular oxidative cross-coupling reactions.

An efficient iridium-catalyzed asymmetric hydrogenation of the fluorinated isoquinoline derivatives has been successfully developed for the synthesis of chiral fluorinated tetrahydroisoquinoline derivatives with up to 93% ee. This methodology features the use of a hydrochloride salt as well as a catalytic amount of halogenated hydantoin which were vital for the reactivity, enantioselectivity, a...

Pyrrolo[2,1-a]isoquinoline alkaloids have been prepared via a visible light photoredox catalyzed oxidation/[3 + 2] cycloaddition/oxidative aromatization cascade using Rose Bengal as an organo-photocatalyst. A variety of pyrroloisoquinolines have been obtained in good yields under mild and metal-free reaction conditions.

Chapter Outline Introduction 123 Therapeutic Potential of Monoamine Oxidase Inhibition in Neurological Disorders 124 Depression 125 Parkinson’s Disease 126 Other Neurodegenerative Diseases 126 Smoke and Alcohol Cessation 127 Alkaloids as Monoamine Oxidase Inhibitors 127 Indole Alkaloids 128 Isoquinoline Alkaloids 134 Piperidine Alkaloids 137 Desoxypeganine 138 Other Alkaloids 139 Conclusion 141...

Benzyl selenocyanates can be made from the corresponding benzylic bromides or chlorides in 30-60 minutes using acetonitrile as a solvent. The products may be obtained pure in satisfactory yields without recourse to chromatography.