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Merck

A direct synthesis of 5,6-dihydroindolo[2,1-a]isoquinolines that exhibit immunosuppressive activity.

Bioorganic & medicinal chemistry letters (2009-09-05)
George A Kraus, Vinayak Gupta, Marian Kohut, Navrozedeep Singh
RÉSUMÉ

Dihydroindolo[2,1-a]isoquinolines were synthesized from tetrahydroisoquinolines and alpha-fluoroaldehydes by a novel two-step procedure. These compounds exhibited significant immunosuppressive activity against IL-2, IL-10 and IFN-gamma.

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Phosphazene base P4-t-Bu solution, ~0.8 M in hexane