| 摘要 |
<p>Benzimidazoles of formula (I) and their acid-addition salts are new:- In the formula, R' is H, alkyl or cycloalkyl; R2 is alkyl or cycloalkyl; R3 is H, primary or secondary alkyl; Y is O or S; also new are the tautomeric thiols of (I) when Y is S. 16 Cpds. are specifically claimed 4-(2-hydroxy-3-methylaminopropoxy)-2-benzimidazolinone and 1-t-butylamino-3-(2-mercapto-7-methyl-4-benzimidazolyloxy)-2-prop- anol. (I) are beta-blockers with low intrinsic stimulating activity for treating cardiovascular disorders, also having antihypertensive activity. Daily adult dose 5-100 mg. A typical cpd., 4-(3-t-butylamino-2-hydroxypropoxy)-2-benzimidazolinone hydrochloride, was prepd. in 56.3% yield by hydrogenation of 1-t-butylamino-3-(2,3-dinitrophenoxy)-2-propanol and treating the diamino prod. with phosgene.</p> |
