623577-33-3Relevant articles and documents
Consecutive Three-Component Coupling-Addition Synthesis of β-Amino Enoates and 3-Hydroxypyrazoles via Ethyl 3-Arylpropiolates
Niedballa, Jonas,Reiss, Guido J.,Müller, Thomas J. J.
supporting information, p. 5019 - 5024 (2020/07/24)
Two consecutive three-component syntheses furnishing β-amino enoates or 3-hydroxypyrazoles based upon the Sonogashira alkynylation of aryl iodides and ethyl propiolate were established in mostly excellent yields. The ethyl 3-arylpropiolate intermediates are Michael systems which are suited for concatenation with conjugate addition or cyclocondensation giving access to libraries of 21 different β-amino enoates and 17 different 3-hydroxypyrazoles. The rotational barrier of β-pyrrolidino enoates was assessed by studying the coalescence of pyrrolidinyl protons in VT-NMR spectra of electronically different substituted derivatives showing that the electronic substituent effect on the aryl group does not affect the height of the rotational barrier. This indicates that the substituents are essentially oriented orthogonally to the plane of the β-pyrrolidino enoates.
PYRAZOLE DERIVATIVES AS GAMMA-SECRETASE INHIBITORS USEFUL IN THE TREATMENT OF ALZHEIMER’S DISEASE
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Page 34; 35, (2010/02/09)
The compounds of formula (I): inhibit gamma-secretase and hence are of utility in the treatment or prevention of Alzheimer's disease.
SULFONAMIDES, SULFAMATES AND SULFAMIDES AS GAMMA-SECRETASE INHIBITORS
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Page/Page column 15, (2008/06/13)
Compounds of formula I inhibit the processing of APP by gamma-secretase, and hence are useful in treating or preventing Alzheimer's disease.