| 摘要 |
The invention comprises 2-[(21-methylbenzothienyl-31)-methyl]-D 2-imidazoline and acid addition salts thereof, and their preparation by reacting (2-methylbenzothienyl-3)-acetic acid or a derivative thereof with ethylene diamine or an N-acyl derivative of ethylene diamine, or with 2-mercaptoimidazoline, optionally followed by salt formation. The ethylene diamine or N-acyl derivative of ethylene diamine may be formed in situ. Other processes for preparing the compounds of the invention are described. 3-Chloromethyl-2-methylbenzothiophene is prepared by passing hydrogen chloride into a mixture of 2-methylbenzothiophene, paraformaldehyde and hydrochloric acid at 60 DEG C,. and is converted to the corresponding nitrile by refluxing with sodium cyanide in acetone and in the presence of sodium iodide. The nitrile affords (2-methylbenzothienyl-3)-acetiminoether hydrochloride upon treatment with ethanol and dry hydrogen chloride. (2-Methylbenzothienyl-3)-acetyl chloride is prepared by treating the corresponding acid with thionyl chloride. The compounds of the invention have vaso-constricting and blood pressure-increasing properties, and may be administered in the form of pharmaceutical preparations containing the active ingredient and a carrier, e.g. by injection or by continuous drip infusion of a solution in sterilized physiological saline. |
