N-(8-Amino-6-fluoro-5-methyl-1-oxo-1,2,3,4-tetrahydronaphthalen-2-yl)acetamide Chemische Eigenschaften,Einsatz,Produktion Methoden
Beschreibung
N-(8-Amino-6-fluoro-5-methyl-1-oxo-1,2,3,4-tetrahydronaphthalen-2-yl)acetamide is an intermediate of Exatecan. Exatecan is used as a component of antibody-drug conjugates for cancer research.
Verwenden
N-(8-Amino-6-fluoro-5-methyl-1-oxo-1,2,3,4-tetrahydronaphthalen-2-yl)acetamide is an important pharmaceutical raw material that is a by-product of the ezetimibe preparation process.
Synthese
N-(8-Amino-6-fluoro-5-methyl-1-oxo-1,2,3,4-tetrahydronaphthalen-2-yl)acetamide is synthesised from N,N'-(3-fluoro-4-methyl-8-oxo-5,6,7,8-tetrahydronaphthalene-1,7-diyl)diethanamide by reaction in the presence of inert gas. The steps are as follows:
Add compound (15.5 g) to a solution of 2N hydrochloric acid (620 mL) and methanol (620 mL), protect with argon, and react at 60°C for 0.5 hours. The temperature is reduced to 010°C, and sodium carbonate (65.7 g ) In water (1314 mL) solution to pH=34, and then neutralized to pH=67 with saturated sodium bicarbonate solution, filtered, washed with 100 mL water, and dried to obtain N-(8-Amino-6-fluoro-5-methyl-1-oxo-1,2,3,4-tetrahydronaphthalen-2-yl)acetamide as a solid powder (12.4 g , 93%).
N-(8-Amino-6-fluoro-5-methyl-1-oxo-1,2,3,4-tetrahydronaphthalen-2-yl)acetamide Upstream-Materialien And Downstream Produkte
Upstream-Materialien
Downstream Produkte
