95450-81-0Relevant academic research and scientific papers
5,6,7,8-TETRAHYDRO-IMIDAZO[1,5-A]PYRAZINE DERIVATIVES
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Page/Page column 57, (2008/12/06)
The invention relates to 5,6,7,8-tetrahydro-imidazo[1,5-a]pyrazine derivatives of formula (I),wherein X represents CH2 or O; R1 represents a phenyl group, which group is independently mono-, di-, or tri-substituted wherein the substituents are independently selected from the group consisting of (C1-4)alkyl, (C1-4)alkoxy, halogen, cyano, trifluoromethoxy and trifluoromethyl; R2 represents (C1-4)alkyl, (C1-4)alkoxy, (C2-4)alkenyl, halogen, cyano, hydroxymethyl, trifluoromethyl, C(O)NR5R6 or cyclopropyl; R3 represents (C1-4)alkyl, (C1-4)alkoxy-methyl or halogen; R4 represents (C1-4)alkyl; R5 represents hydrogen or (C1-4)alkyl; and R6 represents hydrogen or (C1-4)alkyl. The invention also relates to pharmaceutically acceptable salts of such compounds; and to the use of such compounds as medicaments; especially as orexin receptor antagonists.
Le polyphosphate d'ethyle, un reactif de choix pour la synthese de derives du benzofuranne dicarboxylate-2,3 de methyle
Belleney, Joel,Vebrel, Joel,Cerutti, Ernest
, p. 1431 - 1435 (2007/10/02)
The aim of this work is to develop a fast and effective method for the synthesis of methylated derivatives of dimethylbenzofuran-2,3-dicarboxylate.With this end in view, we can suggest significant improvements to the Koelsch and Whitney method, especially by using ethyl polyphosphate.This reagent is indeed well adapted to the cyclodehydration of the methyl 2-aryloxy-3-hydroxymaleate intermediates into benzofuran compounds, since the yield is often better than 80percent.
