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ChemicalBook CAS DataBase List Gramine
87-52-5

Gramine synthesis

9synthesis methods
-

Yield:87-52-5 90%

Reaction Conditions:

with acetic acid in 1,4-dioxane;water at 0 - 20; for 20 h;

Steps:

1 3-Dimethylaminomethylindoles 2:
To a mixture of formalin (37% in water, 0.61mL, 8.14mmol), 1,4-dioxane, and AcOH (7mL) Me2NH (40% in water, 1.03mL, 8.14mmol) was added at 0 °C. A solution of indole 1 (7.40mmol) in 1,4-dioxane (7mL) was added at 0 °C gradually. After stirring at 0 °C for 2 h and at room temperature for 18 h, water (9mL), charcoal (0.43g), and celite (0.43g) were added and the reaction mixture was filtered through a celite pad. The pH of the filtrate was adjusted to 12 by 2N NaOH in water. Filtration, washing (water), and drying of the precipitate afforded 2. Yields ca 90%

References:

Acousia Therapeutics GmbH;B?s, Michael EP2871181, 2015, A1 Location in patent:Paragraph 0057

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