Vibha Tandona
Jawaharlal Nehru University, India
Title: Reformatsky reagent in a dual role: A highly efficient approach towards 1,2-dihydroisoquinolines
Biography
Biography: Vibha Tandona
Abstract
A dual role of Reformatsky reagent is disclosed here for the synthesis of 1,2-dihydroisoquinolines via 6-endo-dig cyclisation, without aid of any external Lewis acid catalyst. This expeditious approach was achieved by the dual nature of Reformatsky reagent i.e. activation of alkyne and then nucleophilic addition to the isoquinolinium salt. Synthetic pathway has high functional group tolerance and can be utilized on gram scale. A mechanistic pathway has been proposed. The 1,2-dihydroisoquinolines derivatives showed upto 90% inhibition of strand transfer activity of HIV integrase enzyme.The highly efficient tandem Reformatsky type reaction without aid of any external Lewis acid catalyst under mild condition has been disclosed. This time-efficient, economically green an expeditious versatile approach to 1, 2-dihydroisoquinolines proceeds with high functional group tolerance and excellent to moderate yield. Isoquinoline core tolerated diverse Reformatsky reagents. Interestingly, Fluorinated esters can also be incorporated by this methodology. These isoquinolines can be used for HIV-Integrase inhibitory activity.