YAKUGAKU ZASSHI
Online ISSN : 1347-5231
Print ISSN : 0031-6903
ISSN-L : 0031-6903
スルファイソオキサゾール合成に関する研究 (第6報)
2-Acetylpropionamidine の合成とその副生物について
谷口 幹二
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ジャーナル フリー

1958 年 78 巻 4 号 p. 329-333

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抄録

2-Acetylpropionimidate hydrochloride, an intermediate in the synthesis of sulfisoxazole, does not form the corresponding amidine by ethanolic ammonia but forms a free imido ester. Examination of this amidination reaction showed that the objective 2-acetylpropionamidine (II) can be obtained by warming the free 2-acetylpropionimidate (I) with ammonia water, in the presence of a small amount of ammonium chloride, for 1 hour at 30°. Extension of the period of heating to 4 hours results in the formation of 2-(1-acetylethyl)-4, 5-dimethyl-6-aminopyrimidine (III) and the heating for 4 hours at 60°, in the formation of 2-(1-methyl-2-iminopropyl)-4, 5-dimethyl-6-aminopyrimidine (IV).

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© by the PHARMACEUTICAL SOCIETY OF JAPAN
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