2-aMinothieno[2,3-d]pyriMidin-4(3H)-one synthesis

Yield:1010068-13-9 71%

Reaction Conditions:

with dimethylsulfone at 130; for 0.5 h;

Steps:

349 Example 349 Synthesis of 2-amino-thieno[2,3-d]pyrimidin-4-(3H)-one

Example 349
Synthesis of 2-amino-thieno[2,3-d]pyrimidin-4-(3H)-one
A suspension of ethyl 2-amino-thiophene-3-carboxylate (0.4 g, 2.34 mmol), chloroformamidine hydrochloride (0.67 g, 5.84 mmol) and dimethylsulfone (0.53 g, 11.7 mmol) was heated at 130° C. for 30 minutes.
After cooling down to room temperature, water (10 ml) was added and ammonium hydroxide was used to neutralize the suspension till pH=8.
The solid was filtered off, washed with water and dried, yielding the crude title compound (71%, 277 mg).
The crude residue was used as such for further reaction.
MS m/z (%): 168 ([M+H]⁺, 100)

References:

US2013/190297,2013,A1 Location in patent:Paragraph 1315; 1316