- Microwave-assisted benzyl mono- and dibromination in diethyl carbonate as environmentally friendly alternative to radical bromination in carbon tetrachloride
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An environmentally friendly benzyl mono- and di-bromination synthetic procedure was developed that is superior to the classic carbon tetrachloride bromination procedure in both reaction time and isolated yield. This new reaction was performed in diethyl carbonate as reaction media using microwave instead of conventional heating. Both the solvent and the brominating reagent N-bromosuccinimide (prepared from succinimide obtained from the reaction mixture) are recyclable. Practically, the preparation of our target compounds was completed in less than two hours. The Royal Society of Chemistry.
- Pingali, Subramanya R. K.,Upadhyay, Sunil K.,Jursic, Branko S
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p. 928 - 933
(2011/05/15)
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- Microwave-assisted NBS bromination of p-iminotoluenes: Preparation of new alcohol, mercapto, and amino protection groups
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A simple, efficient, safe, high-yielding and rapid microwave-assisted method for the preparation of protected p-bromomethyl and p- dibromomethylanilines was developed as new alcohol, thiol, and amine protection groups. The procedure involves microwave-assisted N-bromosuccinimide (NBS) radical bromination of readily available N-protected p-toluidine. The microwave-assisted radical bromination was found to be superior to the conventional NBS radical bromination. Copyright
- Upadhyay, Sunil K.,Jursic, Branko S.
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experimental part
p. 3177 - 3185
(2011/09/20)
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- SUBSTITUTED CYCLIC UREA DERIVATIVES AND THE USE THEREOF AS VANILLOID RECEPTOR 1 MODULATORS
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The invention relates to substituted cyclic urea derivatives, wherein X represents O, S or N-C=N; m is 1 or 2; n is 1 or 2; p1 and p2 represent independently 0, 1, 2 or 3, and the sum of p1 and p2 is 0, 1, 2 or 3. The invention also relates to methods for producing said derivatives, to drugs containing these compounds and to the use of these compounds for producing drugs. The inventive drugs are especially useful for vanilloid receptor 1 (VR1/TRPV1) regulation, preferably for vanilloid receptor 1 (VR1/TRPV1) inhibition and/or vanilloid receptor 1 (VR1/TRPV1) stimulation.
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Page/Page column 73-74
(2010/11/24)
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