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    • 9. 发明授权
    • Radiohalogenated small molecules for protein labeling
    • 用于蛋白标记的放射性卤代小分子
    • US5609848A
    • 1997-03-11
    • US764001
    • 1991-09-23
    • D. Scott WilburAlan R. Fritzberg
    • D. Scott WilburAlan R. Fritzberg
    • C07F3/12C07F7/22A61K51/02C07D207/40C07C25/02
    • C07F7/2212C07F3/12
    • Haloaryl compounds are lithiated and thereafter metalated with one of the following organometallic groups: Sn(n--Bu).sub.3 or SnMe.sub.3. The resulting aryltin compound can be transmetalated in site-specific reaction with one of the following organometallic groups: HgX, Hg(OAc).sub.2, BX.sub.3, or BZ.sub.2, wherein X is Cl, Br, or I, and Z is alkyl or alkoxy. The metalated compounds are subsequently radiohalogenated via a demetalation reaction. A functional group suitable for conjugation to protein can be added subsequent or preferably prior to the radiohalogenation.Also compounds of the formula: R.sub.1 --Ar--R.sub.2, wherein R.sub.1 is either a radiohalogen or any one of the organometallic groups stated above, Ar is aromatic or heteroaromatic ring, and R.sub.2 is a short-chain substituent that does not activate the aromatic ring and that bears a functional group, or a precursor thereof, suitable for conjugation to protein under conditions that preserve the biological activity of the protein.The radiohalogenated small molecules are conjugated to proteins such as monoclonal antibodies for use in diagnosis and therapy.
    • 卤代芳基化合物被锂化,然后用以下有机金属组之一金属化:Sn(n-Bu)3或SnMe 3。 所得的芳基锡化合物可以在以下有机金属基团之一的位置特异性反应中转金属:HgX,Hg(OAc)2,BX3或BZ2,其中X为Cl,Br或I,Z为烷基或烷氧基。 金属化合物随后通过脱金属反应放射卤化。 适于与蛋白质缀合的官能团可以随后或优选在放射性卤化之前添加。 还有下式的化合物:R1-Ar-R2,其中R1是放射性卤素或上述有机金属基团中的任何一个,Ar是芳族或杂芳族环,R2是不活化芳环的短链取代基 并且在保持蛋白质的生物活性的条件下具有适合于与蛋白质缀合的官能团或其前体。 放射性卤化的小分子与蛋白质缀合,例如用于诊断和治疗的单克隆抗体。