New approach for preparation of 2,3,7-trisubstituted 3,4-dihydroisoquinolinone libraries on solid phase

Yidong Ni1,2, Viktor Krchnak1,3, Michal Lebl1,4
1Trega Biosciences Inc., San Diego, U.S.A.
2The Kenan-Flagler Business School, The University of North Carolina at Chapel Hill, Chapel Hill, U.S.A.
3Encore International Corporation, Tucson, U.S.A.
4Spyder Instruments, Inc., San Diego, U.S.A.

Tóm tắt

In an attempt to prepare 7-substituted 3,4-dihydroisoquinolinone family of compounds, we observed an unexpected decarboxylation. The reaction of 4-nitrohomophthalic anhydride with a Schiff base formed on solid support leads to the formation of core structure. LC-MS and 1H NMR analysis confirmed the structure of unexpected intermediate. A library of 38,400 compounds was produced using this new synthetic approach.

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Tài liệu tham khảo

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