Atomic Energy Council-institute of Nuclear Energy Research

Institute of Nuclear Energy Research, Atomic Energy Council, Executive Yuan

Tsyh-Lang Lin

Cheng-Fang Hsu

Show-Wen Liu

Cheng-Hsien Lin

Yu Lung Chang

Lie-Hang Shen

Haw-Jan Chen

A bifunctional compound with a monosaccharide and a NSligand, and more particularly, a bifunctional compound with a NSligand and aminohexylacetyl galactosamine (ah-GalNAc) is provided. A method for preparing the bifunctional compound with a monosaccharide and a NSligand is also provided, including activating a carboxyl group in an organic ligand, reacting the activated carboxyl group with a galactopyranoside through amidation, and then hydrolyzing. The bifunctional compound of the present invention is widely useful in nuclear medicine for preparation of liver imaging agents for assisting in correct diagnosis of diseases.

Bifunctional compound with monosaccharide and N2S2 ligand, and preparation and use thereof

HLMN series compounds used as radioactive agents for treatment of liver cancer and a manufacturing method thereof are revealed. 2-thioethylamine hydrochloride is reacted with triphenylmethanol for protection of thiol to obtain 2-[(triphenylmethyl)thio]ethylamine. Then obtain N-[2-((triphenylmethyl)thio)ethyl]chloroacetamide by a transamidation reaction between 2-[(triphenylmethyl)thio]ethylamine and chloroactyl chloride. Next produce a amine-amide-thiol ligand-N-[2-((triphenylmethyl)thio)ethyl][2-((triphenylmethyl)thio)ethylamino]acetamide by a substitution reaction of N-[2-((triphenylmethyl)thio)ethyl]chloroacetamide and 2-[(triphenylmethyl)thio]ethylamine. After respective reaction with 1-bromotetradecane, 1-bromohexadecane and ethyl 16-bromohexadecanoate, HLMN series compounds are obtained. These amine-amide-dithiols quadridentate ligands can react with MO(M=Tc or Re) to produce electrically neutral complexes. The complexes have high lipophilicity, allowing them soluble in lipiodol to be applied to radiation therapy for liver cancer.

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A method for preparation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine is provided, which includes formation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine, useful as a precursor of a norepinephrine transporter (NET) contrast label [Iodine](R)&#x2014;N-methyl-3-(2-iodophenoxy)-3-phenylpropanamine ([I]MIPP) with a leaving group BuSn.

Method for preparation of N-methyl-3-(2-tributylstannylphenoxy)-3-phenylpropanamine, and use therof

A method for preparing a precursor of radioactive 3-iodobenzylguanidine- N,N'-bis(tert-butyloxycarbonyl)-3-(tri-n-butyltin)benzylguanidine) (MSnBG) is revealed. The method includes following steps. Firstly, obtain 3-iodobenzylguanidine bicarbonate by an addition reaction between 3-iodobenzylamine hydrochloride and cyanamide. Use di-tert-butyl dicarbonate as a protecting agent for NH group and convert 3-iodobenzylguanidine bicarbonate into N,N&#x2032;-bis(tert-butyloxycarbonyl)-N-(3-iodobenzyl) guanidine. At last, under catalysis of bis(triphenylphosphine) palladium dichloride, obtain a final product MSnBG by a substitution reaction between N,N&#x2032;-bis(tert-butyloxycarbonyl)-N-(3-iodobenzyl) guanidine and bis(tri-n-butyltin). MSnBG is used in no-carrier-added synthesis of [*l]MIBG.

Method for preparing precursor of radioactive 3-iodobenzylguanidine

A bifunctional compound containing an amino group and diaminedithiol ligand and a manufacturing method thereof are revealed, the bifunctional compound includes at least one amino group and a diaminedithiol (NS) ligand. The amino groups is for reacting with compounds containing carboxylic acids or halogens while the NSligand binds with technetium or rhenium so as to form an anion complex. The thiol group in the NSligand is protected by a protecting group for prevention of oxidation and easy storage. This protecting group is released easily during complex reactions. Due to the bifunctional property, the compound is applied to preparation of radiopharmaceuticals such as imaging agents and targeted agents.

Bifunctional compound containing amino group and diaminedithiol ligand and manufacturing method thereof

A compound containing carboxylate ester and N2S2 ligand bi-functional groups and a manufacturing method thereof are disclosed. The S in the N2S2 ligand of the compound containing carboxylate ester and N2S2 ligand bi-functional groups includes a protective group so as to avoid to be oxidized and easy storage. In a complex reaction, the protective group is automatically released As to the active carboxylate ester, it is for reacting with compounds having amino groups such as amines, amino acids, peptides, or protein etc while the N2S2 ligand is for bonding with technetium or rhenium so as to form neutral complex. The compound containing carboxylate ester and N2S2 ligand bi-functional groups is applied to radiopharmaceuticals such as contrast agents for tissues and target agents.

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Tsyh-Lang Lin