Continuous flow Aza-Michael reaction for preparing the fast-acting synthetic opioid drug Remifentanil
Braz. J. Pharm. Sci. (Online)
; 59: e22764, 2023. graf
Article
in English
| LILACS
| ID: biblio-1439499
Responsible library:
BR40.1
Localization: BR40.1
ABSTRACT
Abstract Remifentanil is a modern fentanyl analogue with ultrashort-action granted by an esterase-labile methyl propanoate chain. Here, we present the development of a continuous flow methodology for the key N-alkylation step of remifentanil preparation in a biphasic, "slug-flow" regime. We screened parameters under microwave-assisted reactions, translated conditions to flow settings, and obtained remifentanil under 15-min residence time in a 1-mL microreactor, with a space-time yield of 89 mg/mL·h and 94% yield.
Full text:
Available
Collection:
International databases
Database:
LILACS
Main subject:
Pharmaceutical Preparations
/
Remifentanil
/
Analgesics, Opioid
Language:
English
Journal:
Braz. J. Pharm. Sci. (Online)
Journal subject:
Farmacologia
/
Teraputica
/
Toxicologia
Year:
2023
Document type:
Article
Affiliation country:
Brazil
Institution/Affiliation country:
Universidade de São Paulo/BR