クマリン誘導体の薬品的研究 (第15報)

6-Chlorocoumarin-³⁶Clの合成および生体内分布について

抄録

6-Chlorocoumarin-³⁶Cl was synthesized by the modified diazotization from 6-amino-coumarin hydrochloride-³⁶Cl. Diazotization was carried out with sodium nitrite and 3N hydrochloric acid in ether or with isoamyl nitrite in dioxane. The diazonium chloride-³⁶Cl formed was decomposed in ether (with addition of hydrogen chloride gas) or with copper powder in acetone.
Oral administration of this 6-chlorocoumarin-³⁶Cl to a rabbit resulted in decrease of urine on the 2nd and 3rd day but the amount of urine returned to normal on the 4th day. Radioactivity decreased progressively irrespective of the urinary amount and 22.8% of the original radioactivity was found in the urine excreted during 96 hours after the administration.
A part of 6-chlorocoumarin-³⁶Cl is distributed in various organs and the incorporation ratio per gram of the organ decreases in the order of (excreta), small intestine, kidneys, pancreas, spleen, skeletal muscles, heart, bladder, and brain. Incorporation ratio to total weight of organs decreased in the order of kidneys, pancreas, liver, heart, spleen, and brain.