Synthesis of 2,6-difluoro-N-(3-[11C]methoxy-1H-pyrazolo[3,4-b]pyridine-5-yl)-3-(propylsulfonamidio)benzamide as a new potential PET agent for imaging of B-Raf(V600E) in cancers.
Synthesis of 2,6-difluoro-N-(3-[11C]methoxy-1H-pyrazolo[3,4-b]pyridine-5-yl)-3-(propylsulfonamidio)benzamide as a new potential PET agent for imaging of B-Raf(V600E) in cancers.
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2,6-二氟-N-(3-[11C]甲氧基-1H-吡唑并[3,4-b]吡啶-5-基)-3-(丙基磺酰氨基)苯甲酰胺的合成作为一种新的潜在PET成像剂
DOI：
10.1016/j.bmcl.2012.12.027
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发表时间：
2013
影响因子：
2.7
通讯作者：
Q. Zheng
中科院分区：
文献类型：
--
作者：
Min Wang;Mingzhang Gao;K. Miller;Q. Zheng
由2,6-二氟苯甲酸和3-氨基-5-羟基吡唑经过9步合成了真实的标准品2,6-二氟-N-(3-甲氧基-1H-吡唑并[3,4-b]吡啶-5-基)-3-(丙基磺酰胺基)苯甲酰胺，总化学产率为1%。用 TMSCl/NaI 对参考标准进行直接去甲基化，得到用于放射性标记的前体 2,6-二氟-N-(3-羟基-1H-吡唑并[3,4-b]吡啶-5-基)-3-(丙基磺酰胺基)苯甲酰胺，产率 70%。目标示踪剂 2,6-二氟-N-(3-[11C]甲氧基-1H-吡唑并[3,4-b]吡啶-5-基)-3-(丙基磺酰氨基)苯甲酰胺是由前体与[11C]CH3OTf通过O-[11C]甲基化制备的，并通过 HPLC 结合 SPE 进行分离，衰减校正放射化学产率为 40-50%轰击结束时 (EOB) 比活度为 370–740GBq/μmol。
The authentic standard 2,6-difluoro-N-(3-methoxy-1H-pyrazolo[3,4-b]pyridine-5-yl)-3-(propylsulfonamidio)benzamide was synthesized from 2,6-difluorobenzoic acid and 3-amino-5-hydroxypyrazole in 9 steps with 1% overall chemical yield. Direct desmethylation of the reference standard with TMSCl/NaI gave the precursor 2,6-difluoro-N-(3-hydroxy-1H-pyrazolo[3,4-b]pyridine-5-yl)-3-(propylsulfonamidio)benzamide for radiolabeling in 70% yield. The target tracer 2,6-difluoro-N-(3-[11C]methoxy-1H-pyrazolo[3,4-b]pyridine-5-yl)-3-(propylsulfonamidio)benzamide was prepared from the precursor with [11C]CH3OTf through O-[11C]methylation and isolated by HPLC combined with SPE in 40–50% decay corrected radiochemical yields with 370–740GBq/μmol specific activity at end of bombardment (EOB).
影响因子：
11.2
作者：
Nucera C;Lawler J;Parangi S
通讯作者：
Parangi S
[11C]甲烷的便捷气相溴化和[11C]三氟甲磺酸甲酯的生产。
影响因子：
3.1
作者：
Mock,BH;Mulholland,GK;Vavrek,MT
通讯作者：
Vavrek,MT