New Approach for Preparation of 2,3,7-trisubstituted 3,4-dihydroisoquinolinone Libraries on Solid Phase
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Abstract
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.
References
1.
Grunewald G, Caldwell T, Li Q, Criscione K
. Synthesis and evaluation of 3-trifluoromethyl-7-substituted-1,2,3, 4-tetrahydroisoquinolines as selective inhibitors of phenylethanolamine N-methyltransferase versus the alpha(2)-adrenoceptor. J Med Chem. 1999; 42(17):3315-23.
DOI: 10.1021/jm980734a.
View
2.
Hutchinson J, COOK J, Brashear K, Breslin M, Glass J, Gould R
. Non-peptide glycoprotein IIb/IIIa antagonists. 11. Design and in vivo evaluation of 3,4-dihydro-1 (1H)-isoquinolinone-based antagonists and ethyl ester prodrugs. J Med Chem. 1996; 39(23):4583-91.
DOI: 10.1021/jm9604787.
View
3.
Ares J, Kador P, Miller D
. Synthesis and biological evaluation of irreversible inhibitors of aldose reductase. J Med Chem. 1986; 29(11):2384-9.
DOI: 10.1021/jm00161a040.
View
4.
Cheng C
. N-(Aminoalkyl)imide antineoplastic agents. Synthesis and biological activity. J Med Chem. 1985; 28(9):1216-22.
DOI: 10.1021/jm00147a016.
View
5.
Dolle R, Nelson Jr K
. Comprehensive survey of combinatorial library synthesis: 1998. J Comb Chem. 2000; 1(4):235-82.
DOI: 10.1021/cc9900192.
View