1010-68-0Relevant articles and documents
Agents useful for reducing amyloid precursor protein and treating demantia and methods of use thereof
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, (2008/06/13)
The present invention provides compounds and methods of administering compounds to a subject taht can reduce βAPP production and that is not toxic in a wide range of dosages. The present invention also provides non-carbamate compounds and methods of administering such compounds to a subject that can reduce βAPP production and that is not tocix in a wide range of dosages. It has been discovered that either the racemic or enantiomerically pure non-carbamate compounds can be used to decrease βAPP production.
Process for preparing 1,3-dialkyl-5-hydroxyoxindoles and the ether derivatives thereof
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, (2008/06/13)
The invention is directed to a process for preparing a 1,3-dialkyl-5-hydroxyoxindole of formula 1: STR1 comprising heating an N-alkyl-p-alkoxy-(α-haloacyl)anilide of formula 2: STR2 wherein the substituents are as defined herein, in the presence of an anhydrous zinc halide to a temperature in the range from about 120° C. to about 160° C., and isolating the 1,3-dialkyl-5-hydroxyoxindole prepared.
New asymmetric synthesis of (-)-esermethole
Pallavicini,Valoti,Villa,Resta
, p. 363 - 370 (2007/10/02)
A new synthesis of (-)-esermethole, based on the asymmetric alkylation at C(3) of racemic 1,3-dimethyl-5-methoxyoxindole (3), is described. The chloroacetyl derivatives of (-)-menthol and (S)-N-methyl-(1-phenylethyl) amine were chosen as chiral alkylating agents and used under different reaction conditions (temperature, solvent and base). In particular, the latter reacted with 3 in toluene at 10°C, in the presence of t-butyllitium, giving (3S,1'S)-N-methyl-N-(1'-phenylethyl)-1,3-dimethyl-5-methoxyoxindol-3-i lacetamide (10) with a 63% d.e.. This intermediate was easily separated from the undesired minor (3R,1'S) diastereomer (11) and converted to (-)-esermethole (99.6% e.e.) in two steps.