2-Methylquinazolin-5-amine → HCID 66969534, Verbindung

Beteiligte Stoffe

Reaktionsschritte

In the same way as in Example 61, 280 mg (0.87 mmol) of 4-(3-fluoro-2-methoxyphenyl)-2-hydroxy-5-methyl-2-(trifluoromethyl)hexanal, 175 mg (1.1 mmol) of 5-amino-2-methylquinazoline and 0.45 ml of titanium tetraethoxide are reacted to give 4-(3-fluoro-2-methoxyphenyl)-1-[(2-methylquinazolin-5-yl)imino]-5-methyl-2-(trifluoromethyl)hexan-2-ol. 360 mg of resulting crude imine are cyclized in the same way as in Example 61 at −30° C. with 6 ml (6 mmol) of 1 M boron tribromide solution in dichloromethane to give the desired product. Column chromatography on silica gel (hexane/ethyl acetate 0-70%) and subsequent preparative HPLC (SunFire C18, water/methanol) yield 6 mg of product.

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