Winn M, Rasmussen R, Minard F, Kyncl J, Plotnikoff N
J Med Chem. 1975 Apr;18(4):434-7. doi: 10.1021/jm00238a024.
Starting from 3,4-dimethoxyphenacyl bromide, 2-amino-4-(3,4-dihydroxyphenyl)butyric acid (homodopa) was synthesized in six steps. 5-Hydroxyhomodopa was similarly prepared. alpha-Methylhomodopa was synthesized in four steps from zingerone [4-(4-hydroxy-3-methoxyphenyl)-2-butanone]. alpha-Methylhomodopa showed no antihypertensive activity in the genetic hypertensive rat. Homodopa did not potentiate the behavioral effect of Dopa or inhibit Dopa decarboxylase. Homodopamine, unlike dopamine, did not increase renal blood flow in the dog.
以3,4-二甲氧基苯甲酰溴为起始原料，经六步反应合成了2-氨基-4-(3,4-二羟基苯基)丁酸（高多巴）。5-羟基高多巴也采用类似方法制备。从姜油酮[4-(4-羟基-3-甲氧基苯基)-2-丁酮]经四步反应合成了α-甲基高多巴。α-甲基高多巴在遗传性高血压大鼠中未显示出降压活性。高多巴不能增强多巴的行为效应，也不能抑制多巴脱羧酶。与多巴胺不同，高多巴胺不会增加犬的肾血流量。
