Lactones phenoliques halomethylees,inhibiteurs bifonctionnels de proteases—II : Preparation de derives halomethyles de la dihydro-3,4 coumarine et de la benzofuranone-2 |
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Authors: | M Wakselman J-F Hamon M Vilkas |
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Abstract: | o-Hydroxy phenyl propionic and o-hydroxy phenyl acetic acids give mixtures of ortho- and para-hydroxymethylated phenolic acid sodium salts which with thionyl chloride undergo benzylic chlorination and lactonisation; para- and ortho-chloromethylated derivatives of 3,4-dihydrocoumarin and of benzofuran-2-one are thus obtained in two steps. The bromomethylation of (nitro-3 hydroxy-2 phenyl) and (nitro-5 hydroxy-2 phenyl) propionic acids yields 3,4-dihydro-8-nitro-6-bromomethyl- and 3,4-dihydro-6-nitro-8-bromomethyl-coumarins. Some radioactive derivatives have also been synthesised. |
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