Effective approach to a synthesis of fluorine-containing 4-acylamino-4,5,6,7-tetrahydrobenzisoxazoles
https://doi.org/10.29235/1561-8323-2019-63-6-716-720
Abstract
On the example of synthesis of 4-acetylamino-3-fluoroalkyl(aryl)-4,5,6,7-tetrahydro-1,2-benzisoxazoles, the effective approach to a synthesis of novel 4-acylamino-4,5,6,7-tetrahydro-1,2-benzisoxazoles is proposed. 3-Fluoroalkyl(aryl)- 6,7-dihydro-1,2-benzisoxazol-4-ones were reduced by a sodium borohydride in isopropanol to obtain 3-fluoroalkyl(aryl)- 4,5,6,7-tetrahydro-1,2-benzisoxazol-4-ols that in the conditions of the Ritter reaction (acetonitrile, acetic acid, sulfuric acid) gave target 4-acylamino derivatives with 80–94 % yields.
About the Authors
T. S. Khlebnicova
Institute of Bioorganic Chemistry of the National Academy of Sciences of Belarus
Russian Federation
Russian Federation
Khlebnicova Tatyana Stepanovna – Ph. D. (Chemistry), Leading researcher.
5/2, Kuprevich Str., 220141, Minsk
Yu. A. Piven
Institute of Bioorganic Chemistry of the National Academy of Sciences of Belarus
Russian Federation
Russian Federation
Piven Yuri Andreevich – Ph. D. (Chemistry), Senior researcher.
5/2, Kuprevich Str., 220141, Minsk
I. I. Gerus
V. P. Kuchar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine
Russian Federation
Russian Federation
Gerus Igor Ivanovich – Ph. D. (Chemistry), Head of the Department.
1, Murmanskaya, 02094, kiev
A. E. Sorochinsky
V. P. Kuchar Institute of Bioorganic Chemistry and Petrochemistry of the National Academy of Sciences of Ukraine.
Russian Federation
Russian Federation
Sorochinsky Alexander Evgenyevich − Ph. D. (Che mistry), Senior researcher.
1, Murmanskaya, 02094, kiev
F. A. Lakhvich
Institute of Bioorganic Chemistry of the National Academy of Sciences of Belarus
Russian Federation
Russian Federation
Lakhvich Fedor Adamovich – Academician, D. Sc. (Che mistry), Professor, Chief researcher.
5/2, kuprevich Str., 220141, Minsk
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