Facile synthesis of 7-10 membered rings by intramolecular condensation using dialkylcarbonate as solvent
A convenient large-scalable synthesis of 1-benzazepines 19 as an important intermediate of CCR5 antagonist, oral HIV-1 therapy, was established. The anilination of o-halogenobenzaldehyde 9 with alkylamino-acid 16 gave o-formylaniline-acid 17. Compound 17
PROCESS FOR THE PREPARATION OF 2,3-DIHYDROAZEPINE COMPOUNDS
As a process for preparing 2,3-dihydroazepine compounds at low cost in a simple and easy manner, there is provided a process for the preparation of compounds of the formula: or salts thereof, characterized in that compounds of the formula: or salts thereof are reacted with compounds of the formula: or salts thereof to give compounds of the formula: or salts thereof, which are then subjected to esterification and ring-closing reaction.
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(2008/06/13)
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