Process for synthesizing remifentanil

Abstract

An improved process for synthesizing opiate or opioid analgesics and anesthetics, and intermediates thereof is provided. In particular, processes of synthesizing intermediates for use in the preparation of synthetic opiate or opioid compounds such as, for example, remifentanil, carfentanil, sufentanil, fentanyl, and alfentanil are disclosed. The preparation process requires fewer steps, and results in reduced costs and higher efficiency than processes known in the art for producing remifentanil and carfentanil.

Description

field of invention In general, the present invention relates to methods of synthesizing opiate or opioid analgesics and anesthetics and precursors thereof. In particular, the present invention relates to methods for the synthesis of intermediates used in the preparation of synthetic opiates or opioid compounds such as remifentanil, carfentanil, sufentanil fentanyl, fentanyl and alfentanil. In particular, the present invention relates to methods of preparation which require fewer steps, reduce costs and result in higher efficiencies compared to methods known in the art for the preparation of remifentanil and carfentanil. Background of the invention Analgesics, such as remifentanil and carfentanil, have been prepared using synthetic methods involving 6 and 7 steps. Examples of these methods are listed in US Patent Nos. 5,106,983 and 5,019,583. However, these syntheses often require multiple protection and deprotection steps for the active moiety, leading to increased proces...

AI Technical Summary

Problems solved by technology

However, these syntheses often require multiple protection and deprotection steps for the active moiety, leading to increased process cost due to reduced production efficiency and increased raw material costs

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