tert-butyl (2Z)-2-[(dimethylamino)methylidene]-3-oxobutanoate synthesis

Yield:-

Reaction Conditions:

in 1,4-dioxane at 20; for 16 h;Inert atmosphere;

Steps:

64.1 1. Preparation of tert-butyl (Z)-2-((dimethylamino)methylene)-3-oxobutanoate

To a mixture of tert-butyl 3-oxobutanoate (5.4 g, 6.3 mmol) in dioxane (30 mL) was added l, l-dimethoxy-N,N-dimethylmethanamine (19.5 g, 164 mmol). The reaction mixture was stirred at r.t. for 16 h under N₂atmosphere. After completion of the reaction, the resulting mixture was added to water and extracted with EA. The combined organic layers was washed with brine, dried over anhydrous Na₂S0₄, and concentrated to give crude tert-butyl (Z)-2- ((dimethylamino)methylene)-3-oxobutanoate (, 7.2 g), which was used in the next step without further purification.

References:

WO2019/118612,2019,A1 Location in patent:Paragraph 0391