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2-METHOXY-ACETAMIDINE synthesis

4synthesis methods
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Yield: 88%

Reaction Conditions:

Stage #1:2-methoxyacetonitrile with sodium methylate in methanol at 20; for 48 h;
Stage #2: with ammonium chloride in methanol for 12 h;

Steps:

A.A-4.1
A-4: 2-Methoxymethyl-5-(pyrimidin-5-ylamino)-pyrimidine-4-carboxylic acid methyl esterStep 1: 2-Methoxy-acetamidineTo a solution of methoxy-acetonitrile (6 g, 84.4 mmol) in MeOH (60 ml) was added sodium methylate (0.86 g, 16.0 mmol) and the reaction mixture was stirred at ambient temperature for 48 hours. Ammonium chloride (4.52 g, 84.5 mmol) was added to the reaction mixture and stirring was continued for another 12 h. The solvent was removed under reduced pressure yielding the title compound which was used in the next step without any further purification. Yield: 6.5 g (88%)MS: M=89.1 (M+H)+

References:

Bleicher, Konrad;Flohr, Alexander;Zbinden, Katrin Groebke;Koerner, Matthias;Kuhn, Bernd;Peters, Jens-Uwe;Rodriguez-Sarmiento, Rosa Maria;Vieira, Eric US2011/183979, 2011, A1 Location in patent:Page/Page column 18

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