Development of an unit operation under continuous flow conditions for the production of a high potency drug

• Grant number: 20/13732-3
• Support Opportunities: Research Grants - Innovative Research in Small Business - PIPE
• Start date: September 01, 2021
• End date: May 31, 2022
• Field of knowledge: Physical Sciences and Mathematics - Chemistry - Organic Chemistry
• Principal Investigator: Kevin de Aquino Dias
• Grantee: Kevin de Aquino Dias
• Company: Fluxofarma Pesquisa e Desenvolvimento Ltda
• CNAE: Fabricação de produtos farmoquímicos ; Fabricação de medicamentos para uso humano
• City: São Paulo
• Associated researchers: Marcio Henrique Zaim
• Associated scholarship(s): 21/09625-0 - Development of an unit operation under continuous flow conditions for the production of a high potency drug, BP.PIPE

Abstract

Ethinylestradiol (EE) is a bioactive synthetic estrogen administered orally, currently categorized as a high potency and high added value drug (US $ 3,750.00 kg-1), being widely used in formulations of combined contraceptive drugs. It is known that even with the constant updating of good manufacturing practices (GMP), the production of EE is of high occupational risk and, to date, all of its production is carried out in batches. Therefore, the present project aims to develop a unit operation under continuous flow conditions to obtain EE via stereoselective ethynylation of estrone (1) using lithium acetylide - ethylenediamine complex (LiCCH / EDA). It is intended to converge advantages inherent to organic synthesis under flow conditions, such as better rates of heat and mass transfer, increased productivity due to reduced downtime and increased operational safety by minimizing the handling of reagents and products. To characterize the drug following the quality standards required by the United States Pharmacopeia (USP) is also the objective of this proposal (AU)