An unusual intramolecular trans-amidation

Enantioselective synthesis of almorexant via iridium-catalysed intramolecular allylic amidation.

An enantioselective synthesis of almorexant, a potent antagonist of human orexin receptors, is presented. The chiral tetrahydroisoquinoline core structure was prepared via iridium-catalysed asymmetric intramolecular allylic amidation. Further key catalytic steps of the synthesis include an oxidative Heck reaction at room temperature and a hydrazine-mediated organocatalysed reduction.

Highly diastereo- and enantioselective intramolecular amidation of saturated C-H bonds catalyzed by ruthenium porphyrins.

An amidation a day keeps apoptosis away

ot all isoforms are created equal. New results from Christiana Ruhrberg, David Shima (Cancer Research UK, London, UK), and colleagues reveal that the stickiness of vascular endothelial growth factor (VEGF) can make all the difference between blood vessels growing larger or finding new territory. VEGF initiates the formation and expansion of the vascular system. VEGF isoforms differ in their abi...

Lactone-directed intramolecular Diels-Alder cyclization: synthesis of trans-dihydroconfertifolin.

Trienes 1 and 3 were obtained in five steps from ethyl 4-acetoxy-3-oxobutanoate and 6-iodo-3-methyl-1,3-hexadiene. Intramolecular Diels-Alder cyclization of 1 and 3 gave tricyclic lactones 2 and 4 as the major products, respectively. The key intermediate 4 was converted in two steps to trans-dihydroconfertifolin (5).

Kimura’s Disease – An Unusual Presentation

Introduction: Kimura’s disease is a rare chronic inflammatory disease of unknown etiology, presenting as painless subcutaneous nodules with lymphadenopathy and peripheral eosinophilia, mainly disturbing the head and neck region. It mainly affects Asian males in their 2nd to 4th decade of life. One such case of Kimura’s disease, which is uncommon in Indian natives, is reported.   Case Report: A ...