Three-step synthetic procedure to prepare dolutegravir, cabotegravir, and bictegravir

Autor:	Xianheng Wang, Song Chen, Hanqi Cui, Yuqi He, Changkuo Zhao
Jazyk:	angličtina
Rok vydání:	2022
Předmět:	Dolutegravir three-step cabotegravir bictegravir process optimization Science Chemistry QD1-999
Zdroj:	Green Chemistry Letters and Reviews, Vol 15, Iss 2, Pp 312-319 (2022)
Druh dokumentu:	article
ISSN:	17518253 1751-7192 1751-8253
DOI:	10.1080/17518253.2022.2057200
Popis:	Dolutegravir, cabotegravir, and bictegravir are three integrase inhibitors, which were used for HIV-1 in the clinic. In this paper, a continuous three-step synthetic strategy was developed to prepare dolutegravir, cabotegravir, and bictegravir in a better yield, compared to the initial step-by-step procedure. Different solvents, temperature, and times were optimized. In the course of industrial production of active pharmaceutical ingredient (API), this three-step synthetic protocol has several advantages, including low cost, time-saving, and better yield. This process was successfully scaled up to tens of grams.
Databáze:	Directory of Open Access Journals
Externí odkaz:	https://doaj.org/article/1cbe372ee7ad41fb8d32c7fd6a278cc6 Zobrazit plný text záznamu View record in DOAJ