[EN] METHOD FOR THE PREPARATION OF DIARYLISOXAZOLE SULFONAMIDE COMPOUNDS AND INTERMEDIATES [FR] PROCEDES DESTINES LA PREPARATION D'UN COMPOSE DE DIARYLISOXAZOLE SULFONAMIDE ET D'INTERMEDIAIRES
Compounds and methods which modulate feeding behavior and related diseases
申请人:Amgen Inc.
公开号:US06187777B1
公开(公告)日:2001-02-13
There are provided compounds, compositions and methods of use thereof in the modulation of feeding behavior, obesity, diabetes, cancer (tumor), inflammatory disorders, depression, stress related disorders, Alzheimer's disease and other disease conditions.
[EN] METHOD FOR THE PREPARATION OF DIARYLISOXAZOLE SULFONAMIDE COMPOUNDS AND INTERMEDIATES<br/>[FR] PROCEDES DESTINES LA PREPARATION D'UN COMPOSE DE DIARYLISOXAZOLE SULFONAMIDE ET D'INTERMEDIAIRES
申请人:PHARMACIA CORP
公开号:WO2005123701A1
公开(公告)日:2005-12-29
The disclosure provides a method for the preparation of a diarylisoxazolé sulfonamide compound comprising contacting a deoxybenzoin with a secondary amine to form a diarylenamine compound; contacting the diarylenamine compound with an acetylating agent to form an acetyl diarylenamine compound; contacting the acetyl diarylenamine compound with a source of hydroxylamine to form an diaryl isoxazolol compound; eliminating water from the diaryl isoxazolol compound to form a diaryl isoxazole compound, chlorosulfonating the diarylisoxazole compound to form a chlorosulfonyl diaryl isoxazole compound; and contacting the chlorosulfonyl diaryl isoxazole compound with a source of ammonia to form the diarylisoxazole sulfonamide compound.
Alkali metal and stoichiometric effects in intermolecular hydroamination catalysed by lithium, sodium and potassium magnesiates
作者:Laia Davin、Alberto Hernán-Gómez、Calum McLaughlin、Alan R. Kennedy、Ross McLellan、Eva Hevia
DOI:10.1039/c9dt00923j
日期:——
neutral Mg(CH2SiMe3)2, even when harsher reaction conditions are employed (24 h, 80 °C). A pronounced alkalimetal effect is also uncovered proving that the alkalimetal (Li, Na, or K) is not a mere spectating counterion. Through stoichiometric reactions, and structural and spectroscopic (DOSY NMR) investigations we shed some light on the potential reaction pathway as well as the constitution of key