Synthesis and Characterization of a Boronated Metallophthalocyanine for Boron Neutron Capture Therapy.
中子俘获
放射化学
硼同位素
核化学
碳化硼
作者
Stephen B. Kahl,Jing Li
出处
期刊:Inorganic Chemistry [American Chemical Society] 日期:1996-06-19卷期号:35 (13): 3878-3880被引量:53
标识
DOI:10.1021/ic9600240
摘要
Synthesis of the first fully characterized, water-soluble boronated phthalocyanine is reported. Reaction of 4-nitrophthalonitrile with dimethyl malonate in the presence of base yielded dimethyl (3,4-dicyanophenyl)malonate which was converted into dimethyl (3,4-dicyanophenyl)propargylmalonate by sequential treatment with potassium hydroxide and propargyl bromide. Formation of the o-carborane cage was accomplished by reaction of the alkyne with decaborane in acetonitrile at reflux. High-temperature solid state condensation of the resulting o-carboranylphthalonitrile with cobalt(II) chloride followed by ester deprotection and cation exchange provided the water-soluble closo-carbonylphthalocyanine product. The product contains 40 boron atoms (27% boron by weight) and may be useful as a tumor-seeking boron delivery agent for boron neutron capture therapy of cancer.