53606-06-7Relevant articles and documents
SPIRO COMPOUNDS AS GLYCOSIDASE INHIBITORS
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Page/Page column 116, (2020/03/15)
Compounds of formula (I) wherein A, R, L, Z, Q1, Q2 and n have the meaning according to the claims can be employed, inter alia, for the treatment of tauopathies and Alzheimer's disease.
Synthesis of unsymmetrical 3,4-diaryl-3-pyrrolin-2-ones utilizing pyrrole weinreb amides
Greger, Jessica G.,Yoon-Miller, Sarah J. P.,Bechtold, Nathan R.,Flewelling, Scott A.,MacDonald, Jacob P.,Downey, Catherine R.,Cohen, Eric A.,Pelkey, Erin T.
, p. 8203 - 8214 (2011/12/04)
A regiocontrolled synthesis of unsymmetrical 3,4-diaryl-3-pyrrolin-2-ones has been achieved in three steps from 1,2-diaryl-1-nitroethenes with pyrrole-2-carboxamides (pyrrole Weinreb amides) serving as the key linchpin intermediates. Two different methods for the preparation of the requisite nitroalkenes were investigated: (1) modified Henry reaction between arylnitromethanes and arylimines; and (2) Suzuki-Miyaura cross-coupling reaction of 2-aryl-1-bromo-1-nitroethenes with arylboronic acids. Some difficulty was encountered in the preparation of arylnitromethanes, thus leading to the exploration of a cross-coupling strategy that proved more useful. A Barton-Zard pyrrole cyclocondensation reaction between 1,2-diaryl-1-nitroethenes and N-methoxy-N-methyl-2-isocyanoacetamide gave the corresponding pyrrole Weinreb amides, which were then converted into the desired 3-pyrrolin-2-ones in two steps. Overall, this method allowed for the construction of 3,4-diaryl-3- pyrrolin-2-ones with complete regiocontrol of the substituents with respect to the lactam carbonyl. The utility of this synthetic methodology was demonstrated by the preparation of eight unsymmetrical and symmetrical 3,4-diaryl-3-pyrrolin- 2-ones including the N-H lactam analogue of the selective COX-II inhibitor, rofecoxib.
Substituent effects on benzyl radical hyperfine coupling constants. Part 2. The effect of sulphur substituents
Wayner, Danial D. M.,Arnold, Donald R.
, p. 1164 - 1168 (2007/10/02)
Several 4-substituted benzyl radicals of the general form R(On)SC5H4CH2. (n=0, 1, 2; R=Me, Ph, Tol, COCH3, OCH3) have been investigated by electron spin resonance (esr) spectroscopy.In general, the ability to delocalize spin density onto the substituent decreases as n increases.The effect of R on the spin density depends on the oxidation state of the sulphur.These trends are explained by considering the sulphur to be eithr a spin donor or a spin acceptor, depending on the oxidation state.The ?.a valuesare determined.
