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首页> 外文期刊>Acta crystallographica. Section C, Structural chemistry. >N N , N N , N N ‐Trimethyl‐5‐[(2,3,5,6‐tetrafluorophenoxy)carbonyl]pyridin‐2‐aminium trifluoromethanesulfonate a precursor for the synthesis of 2,3,5,6‐tetrafluorophenyl 6‐[ 18 18 F]‐fluoronicotinate
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N N , N N , N N ‐Trimethyl‐5‐[(2,3,5,6‐tetrafluorophenoxy)carbonyl]pyridin‐2‐aminium trifluoromethanesulfonate a precursor for the synthesis of 2,3,5,6‐tetrafluorophenyl 6‐[ 18 18 F]‐fluoronicotinate

机译：NN，NN，NN-甲基-5 - [（2,3,5,6-四氟氧基氧基）羰基]吡啶-2-氨基三氟甲磺酸盐合成2,3,5,6-四氟苯基6- [18]的前体 f] -fluoronotinate.

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The synthesis, recrystallization, and X‐ray deterimination of N , N , N ‐trimethyl‐5‐[(2,3,5,6‐tetrafluorophenoxy)carbonyl]pyridin‐2‐aminium trifluoromethanesulfonate (PyTFP‐precursor), C 15 H 13 F 4 N 2 O 2 + ·CF 3 SO 3 ? , is described. This triflate salt precursor is required for the synthesis of 2,3,5,6‐tetrafluorophenyl 6‐[ 18 F]‐fluoronicotinate ([ 18 F]FPyTFP), a prosthetic group used to radiolabel peptides for positron emission tomography (PET), as peptides are increasingly being used as PET‐imaging probes in nuclear medicine. Radiolabeling of peptides is typically done using a `prosthetic group', a small synthon to which the radioisotope is attached in the first step, followed by attachment to the peptide in the second step. During the synthesis of the PyTFP‐precursor, displacement of a Cl atom with trimethylamine gas and anion replacement with a triflate counter‐ion is critical, as incomplete replacement would hinder radioisotopic incorporation of nucleophilic fluorine‐18 and result in diminished radiochemical yields. The structural determination of the PyTFP‐precursor by X‐ray crystallography helped confirm the anion exchange of chloride with triflate.
机译：N，N，N-三甲基-5 - [（2,3,5,6-四氟氧基氧基）羰基]吡啶-2-氨基三氟甲磺酸盐（PyTFP-前体），C 15 H的合成，重结晶和X射线脱酯滴乳。 13 F 4 N 2 O 2 +·CF 3 SO 3？ ，描述。该Triflate盐前体是合成2,3,5,6-四氟苯基6- [18 f] -fluoronotinate（[18 f] fpytfp），用于用于正电子发射断层扫描（PET）的radiolabel肽的假体组，由于肽越来越多地被用作核医学中的宠物成像探针。通常使用“假体基”进行肽的放射性标记，其中放射性同位素在第一步中附着放射性同位素的小合成酮，然后在第二步骤中附着于肽。在合成PyTFP-前体的合成期间，用三甲胺气体的Cl原子与Triflate反离子的阴离子置换是至关重要的，因为不完全替代将妨碍核细胞氟-18的放射性同位素掺入并导致放射化学产率降低。 X射线晶体学通过X射线晶体学的PyTFP-前体的结构测定有助于确认氯化物的阴离子交换与三氟甲酸酯。

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