AROMATIC AMINO ACID DERIVATIVE AND POSITRON EMISSION TOPOGRAPHY (PET) PROBE UTILIZING SAME

摘要

A compound having the structure represented by general formula (I) (therein, n is either 0 or 1; R1 represents a hydrogen atom (only in cases where n=0), a halogen atom, a C1-C6 alkyl group, a C1-C6 haloalkyl group, an optionally substituted amino group, an optionally substituted phenyl group, a C1-C6 alkylthio group, a C1-C6 alkoxy group, a C1-C6 haloalkoxy group, or a C7-C12 aralkyloxy group; R2 represents -(CH2)p-[O(CH2)q]r-X (therein, X is a halogen atom, p is an integer from 1-6, q is an integer from 1-4, and r is an integer from 0-4); R3 represents a hydrogen atom, a C1-C6 alkyl group, a C7-C16 aralkyl group, or a C6-C14 aryl group; and R4 represents a hydrogen atom or a C1-C6 aralkyl group). The compound or pharmaceutically acceptable salt thereof exhibits a higher level of accumulation in cancer compared to fluorine-18-α-methyltyrosine (FAMT) and a strong affinity and selectivity to L-type amino acid transporter 1 (LAT1), and can be used in labeling in a medical setting; therefore the compound or pharmaceutically acceptable salt thereof is useful as a highly versatile PET imaging agent.