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A Reliable Synthesis of 3-Amino-5-Alkyl and 5-Amino-3-Alkyl Isoxazoles

Leland Johnson, James Powers, Fupeng Ma, Keith Jendza, Bing Wang, Erik Meredith, Nello Mainolfi*

*Novartis Institutes for Biomedical Research, Global Discovery Chemistry, 100 Technology Square, Cambridge, MA 02139, USA, Email:

L. Johnson, J. Powers, F. Ma, K. Jendza, B. Wang, E. Meredith, N. Mainolfi, Synthesis, 2013, 45, 171-173.

DOI: 10.1055/s-0032-1317935


In a reliable procedure that can be used to access a wide range of 3-amino-5-alkyl and 5-amino-3-alkyl isoxazoles, the reaction temperature and pH were key factors that determined the regioselectivity.

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Key Words

heterocycles, isoxazoles, regioselectivity, condensation, medicinal chemistry, imines

ID: J66-Y2013-0160