A method of producing an aminobutene derivative of formula (I) by allowing a butenol derivative of formula (II) to react with an amide derivative of formula (III) is disclosed. The aminobutene derivative of formula (I) can be deprotected to produce an aminobutene derivative of formula (I-A) or an aminobutene derivative of formula (I-B):
The aminobutene derivative of formula (I-A) can also be deprotected to produce the aminobutene derivative of formula (I-B). Any or all of the above aminobutene derivatives are useful as intermediates for producing anti-ulcer drugs, and anti-ulcer drugs having an inhibitory effect on gastric acid secretion based on the antagonism against histamine H₂ receptor.
本发明公开了一种通过使式(II)的
丁烯醇衍
生物与式(III)的酰胺衍
生物反应来生产式(I)的
氨基
丁烯衍
生物的方法。式(I)的
氨基
丁烯衍
生物可以通过脱保护来生成式(I-A)的
氨基
丁烯衍
生物或式(I-B)的
氨基
丁烯衍
生物:
式(I-A)的
氨基
丁烯衍
生物也可以进行脱保护反应,生成式(I-B)的
氨基
丁烯衍
生物。上述任何或所有
氨基
丁烯衍
生物均可作为生产抗溃疡药物和基于
组胺 H₂受体拮抗作用而对胃酸分泌具有抑制作用的抗溃疡药物的中间体。