One pot synthesis of citalopram from 5-cyanophthalide

C - Chemistry – Metallurgy – 07 – D

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C07D 307/87 (2006.01)

Patent

CA 2559703

A process for one pot synthesis of citalopram is disclosed. The process comprises subjecting 5-cyano phthalide to Grignard reduction followed cyclization and followed by C-alkylation reaction to obtain citalopram without isolation and purification of any intermediates. In another embodiment, 5- cyano phthalide is subjected to sequential Grignard reactions followed by cyclization to obtain citalopram without isolation and purification of any intermediate stages.

Cette invention concerne une méthode de synthèse <= one-pot >= du citalopram. Cette méthode consiste à soumettre un 5-cyano phthalide à une réduction de Grignard suivie d'une cyclisation, puis d'une réaction de C-alkylation pour obtenir du citalopram sans isolement ni purification d'intermédiaires. Dans un autre mode de réalisation, on soumet un 5-cyano phthalide à des réactions séquentielles de Grignard suivies d'un cyclisation pour obtenir du citalopram sans isolement ni purification de stades intermédiaires.

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