Clinical efficacy of Sep-Pak(R) assisted one pot automated synthesis of pharmaceutical grade [18F]FLT using 5′-O-(benzoyl)-2,3′-anhydrothymidine precursor

被引：1

作者：

Mitra, Arpit ^{[1
]}

Chakraborty, Avik ^{[2
]}

Upadhye, Trupti ^{[2
]}

Verma, Priyanka ^{[2
]}

Rajesh, C. ^{[2
]}

Lad, Sangita ^{[2
]}

Pawar, Yogita ^{[2
]}

Basu, Sandip ^{[2
]}

Banerjee, Sharmila ^{[1
,2
]}

机构：

[1] Board Radiat & Isotope Technol, Med Cyclotron Facil, Radiat Med Ctr, Mumbai, Maharashtra, India

[2] Bhabha Atom Res Ctr, Radiat Med Ctr, TMH Annex, Mumbai 400012, Maharashtra, India

来源：

JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY | 2021年 / 327卷 / 01期

关键词：

5 '-O-(Benzoyl)-2,3 ' anhydrothymidine; Radiofluorination; F-18]FLT; Radiochemical; PET/CT; Stavudine; RADIOSYNTHESIS; PET;

D O I：

10.1007/s10967-020-07531-9

中图分类号：

O65 [分析化学];

学科分类号：

070302 ; 081704 ;

摘要：

An automated production of pharmaceutical grade 3 '-deoxy-3 '-[F-18]fluorothymidine ([F-18]FLT) with solid phase extraction (SPE) purification using 5 '-O-(Benzoyl)-2,3 ' anhydrothymidine precursor (Benzoyl-Anhydro) poses a major challenge. Herein, an automated, one-pot, two-step, radiochemical synthesis of [F-18]FLT using benzoyl-anhydro precursor and subsequent optimization of SPE purification (using readily available SepPak (R) cartridges) while maintaining radiochemical purity, chemical purity and residual solvent levels within the specified limits has been reported. The current method yields pharmaceutical grade [F-18]FLT suitable for inclusion as a generic product in different pharmacopeia. The desired clinical results add support to indigenously produced Sep-Pak(R) purified [F-18]FLT as a pharmaceutical grade diagnostic radiopharmaceutical.

引用

页码：585 / 596

页数：12

共 11 条

[1] Clinical efficacy of Sep-Pak® assisted one pot automated synthesis of pharmaceutical grade [18F]FLT using 5′-O-(benzoyl)-2,3′-anhydrothymidine precursor
Arpit Mitra
Avik Chakraborty
Trupti Upadhye
Priyanka Verma
C. Rajesh
Sangita Lad
Yogita Pawar
Sandip Basu
Sharmila Banerjee
Journal of Radioanalytical and Nuclear Chemistry, 2021, 327 : 585 - 596
[2] Automated Synthesis of Pharmaceutical Grade [18F]FLT using 5′-O-(Benzoyl)-2,3′-anhydrothymidine Precursor
Mitra, Arpit
Rajesh, Chinagandham
Lad, Sangita
Upadhye, Trupti
Banerjee, Sharmila
Rajan, Ramakrishna
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2017, 60 : S616 - S616
[3] Sep-Pak® Assisted Automated One-pot Synthesis of [18F]FLT using 3-N-BOC-DMTr Protected Nosyl Thymidine Precursor
Mitra, A.
Rajesh, C.
Upadhye, T.
Pawar, Y.
Murhekar, V. V.
Rajan, R. M. G.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2014, 41 : S347 - S347
[4] Synthesis and labeling of 5′-O-(4,4′-dimethoxytrityl)-2,3′-anhydrothymidine for [18F]FLT preparation
Blocher, A
Kuntzsch, M
Wei, R
Machulla, HJ
JOURNAL OF RADIOANALYTICAL AND NUCLEAR CHEMISTRY, 2002, 251 (01) : 55 - 58
[5] Automated radiochemical synthesis of pharmaceutical grade [18F]FLT using 3-N-Boc-5′-O-dimethoxytrityl-3′-O-nosyl-thymidine precursor and its Sep-Pak® purification employing selective elution from reversed phase
Mitra, Arpit
Chakraborty, Avik
Upadhye, Trupti
Tawate, Megha
Lad, Sangita
Sahu, Sudeep
Rajesh, Chinagandham
Bagul, Swati
Pawar, Yogita
Ray, Mukti Kant
Banerjee, Sharmila
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2022, 65 (08): : 206 - 222
[6] Fully Automated Radiosynthesis of 3′-deoxy-3′-[18F]Fluoro Thymidine ([18F]FLT) With Anhydro Precursor (DMTThy) and Sep-Pak® Cartridge Purification and Analysis of Chemical and Radiochemical Purity
Nandy, S. K.
Chakraborty, A.
Pawar, Y.
Moghe, S. H.
Rajan, M. G. R.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2014, 41 : S346 - S346
[7] Synthesis and labeling of 5'-O-(4,4'-dimethoxytrityl)-2,3'-anhydr othymidine for [18F]FLT preparation
A. Blocher
M. Kuntzsch
R. Wei
H.-J. Machulla
Journal of Radioanalytical and Nuclear Chemistry, 2002, 251 : 55 - 58
[8] An improved automated one-pot synthesis of O-(2-[18F]fluoroethyl)-L-tyrosine ([18F]FET) based on a purification by cartridges
Bogni, A.
Laera, L.
Cucchi, C.
Iwata, R.
Seregni, E.
Pascali, C.
NUCLEAR MEDICINE AND BIOLOGY, 2019, 72-73 : 11 - 19
[9] Simplified and Automated Synthesis of O-(2-[18F]Fluoroethyl)-L-tyrosine ([18F]FET) Using a Single Pot, Two-stage Procedure and Solid-Phase Extraction Purification
Nandy, S. K.
Chakraborty, A.
Pawar, Y.
Moghe, S. H.
Rajan, M. G. R.
EUROPEAN JOURNAL OF NUCLEAR MEDICINE AND MOLECULAR IMAGING, 2014, 41 : S421 - S421
[10] Synthesis of 3′-deoxy-3′-[18F]fluoro-thymidine with 2,3′-anhydro-5′-O-(4,4′-dimethoxytrityl)thymidine
Wodarski, C
Eisenbarth, J
Weber, K
Henze, M
Haberkorn, U
Eisenhut, M
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2000, 43 (12): : 1211 - 1218

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