广州化工
廣州化工
엄주화공
GUANGZHOU CHEMICAL INDUSTRY AND TECHNOLOGY
2015年
2期
1-3
,共3页
周盼红%李成龙%王碧佳
週盼紅%李成龍%王碧佳
주반홍%리성룡%왕벽가
4-碘-L-苯丙氨酸%氮-氟试剂%二芳基碘鎓盐%氧化
4-碘-L-苯丙氨痠%氮-氟試劑%二芳基碘鎓鹽%氧化
4-전-L-분병안산%담-불시제%이방기전옹염%양화
L-4-Iodophenylalanine%N-F reagents%diaryliodonium salts%oxidation
报道了一种无酸条件下合成二芳基碘鎓盐的方法。以4-碘-L-苯丙氨酸为原料，经酯化、氨基保护、无酸组合试剂氮-氟试剂/乙酰基三甲基硅烷反应、苯基三氟硼酸钾/三甲基硅三氟乙酸发生金属转移反应和在离子交换反应成功制得了目标产物4-(氮，氮-二叔丁氧羰基苯丙氨酸甲酯)苯基碘鎓六氟磷酸盐。该碘鎓盐与氟-18标记的氟离子反应可制备氟18-氟代苯丙氨酸，是一种潜在的正电子发射断层显像显像剂。
報道瞭一種無痠條件下閤成二芳基碘鎓鹽的方法。以4-碘-L-苯丙氨痠為原料，經酯化、氨基保護、無痠組閤試劑氮-氟試劑/乙酰基三甲基硅烷反應、苯基三氟硼痠鉀/三甲基硅三氟乙痠髮生金屬轉移反應和在離子交換反應成功製得瞭目標產物4-(氮，氮-二叔丁氧羰基苯丙氨痠甲酯)苯基碘鎓六氟燐痠鹽。該碘鎓鹽與氟-18標記的氟離子反應可製備氟18-氟代苯丙氨痠，是一種潛在的正電子髮射斷層顯像顯像劑。
보도료일충무산조건하합성이방기전옹염적방법。이4-전-L-분병안산위원료，경지화、안기보호、무산조합시제담-불시제/을선기삼갑기규완반응、분기삼불붕산갑/삼갑기규삼불을산발생금속전이반응화재리자교환반응성공제득료목표산물4-(담，담-이숙정양탄기분병안산갑지)분기전옹륙불린산염。해전옹염여불-18표기적불리자반응가제비불18-불대분병안산，시일충잠재적정전자발사단층현상현상제。
A metal-free synthesis of [2-[ ( di-tert-butoxycarbonyl)-amino]-3-methoxy-3-o-xopropyl-phenyl]-( phenyl) iodonium hexafluorophosphate from the corresponding iodoarene was reported. Trimethylsilyl acetate ( TMSOAc) was used to tame the reactive I( III) intermediate formed from oxidation of 2-amino-3-(4-iodophenyl) propanoic acid by N-F reagents. The corresponding diacetoxyiodoarene could be obtained without damaging the acid-sensitive Boc protecting groups. The I( III) intermediate could be converted to the corresponding diaryliodonium salts by reacting with benzenetrifluoroboric acid potassium salt and potassium hexaflourophosphate in excellent isolated yield. The iodonium salt was a useful precursor for synthesis of 18 F-fluorophenalanine, an 18 F-labled amino acid to be used as a radio tracer for positron emission tomography ( PET) . The structure of the product was confirmed by 1 H-NMR, 13 C-NMR and mass spectroscopy.
