(2R*, 3S*)-1-[18F]fluoro-2,3-bis(4-hydroxyphenyl)pentane [( 18F]fluoronor-hexestrol), a positron-emitting estrogen that shows highly-selective, receptor-mediated uptake by target tissues in vivo.
(2R*, 3S*)-1-[18F]fluoro-2,3-bis(4-hydroxyphenyl)pentane [( 18F]fluoronor-hexestrol), a positron-emitting estrogen that shows highly-selective, receptor-mediated uptake by target tissues in vivo.
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(2R*, 3S*)-1-[18F]氟-2,3-双(4-羟基苯基)戊烷[( 18F]氟正己雌醇)，一种正电子发射雌激素，具有高度选择性、受体介导的摄取
DOI：
10.1016/0024-3205(83)90678-1
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发表时间：
1983
期刊：
影响因子：
6.1
通讯作者：
Welch,MJ
中科院分区：
文献类型：
--
作者：
Landvatter,SW;Kiesewetter,DO;Kilbourn,MR;Katzenellenbogen,JA;Welch,MJ
采用氟离子置换法制备了正电子发射的非甾体雌激素(2 R∗,3 S∗)-1-[18 F]氟- 2,3 -双（4-羟基苯基）戊烷（[18 F]-氟己烯醇），在适当保护前体的不稳定的三氟甲烷磺酸（三氟酸盐）衍生物上，然后用氢化铝锂去除三氟酸盐芳基基团，并用高效液相色谱法纯化。在未成熟的雌性大鼠中，由于与雌激素受体结合，这种化合物被子宫选择性地吸收并保留较长时间。因此，该化合物和相关的18f标记的雌激素似乎是雌激素受体阳性人类乳腺肿瘤成像的有希望的药物。
The positron-emitting, non-steroidal estrogen (2 R∗, 3 S∗)-1-[18 F] fluoro-2, 3-bis (4-hydroxyphenyl) pentane ([18 F]-fluoronor-hexestrol), has been prepared by fluoride ion displacement on a labile trifluoromethanesulfonate (triflate) derivative of a suitably protected precursor, followed by removal of the aryl triflate groups with lithium aluminum hydride and purification by HPLC. In immature female rats, this compound is taken up selectively by the uterus and is retained for prolonged periods, due to its binding to the estrogen receptor. This compound and related 18 F-labeled estrogens thus appear to be promising agents for imaging estrogen receptor-positive breast tumors in humans.