公开(公告)号：US07132563B1

公开(公告)日：2006-11-07

申请号：US11162286

申请日：2005-09-06

申请人： Jenn Tzong Chen ,  Wuu Jyh Lin ,  Ai Ren Lo ,  Ming Hsin Lee ,  Hsin Er Wang ,  Shih Yan Wu ,  Mao Hsiung Chang

发明人： Jenn Tzong Chen ,  Wuu Jyh Lin ,  Ai Ren Lo ,  Ming Hsin Lee ,  Hsin Er Wang ,  Shih Yan Wu ,  Mao Hsiung Chang

IPC分类号： C07C229/36

CPC分类号： C07C227/20 ,  C07C269/06 ,  Y02P20/55 ,  C07C229/36 ,  C07C271/22

摘要： This is a novel method for production of no-carrier-added O-(2-[18F]fluoroethyl)-L-Tyrosine, which has been proved a suitable PET (position emission tomography) probe for tumor diagnosis imaging, and the preparation of the title compound starts from precursors with the chemical structures as in Formula 1, wherein R1 is a protective group for the carboxyl functional group, R2 is a protective group for the amino group, and R3 acts as a leaving group, R1 represents an arylalkyl group, R2 represents a carboxyl group, and R3 represents a p-tosyloxy, methane sulfonyloxy or trifluoromethane sulfonyloxy or bromine, and the final purification of the product is using a separation column, which is very convenient for automated synthesis, and the invention uses the precursor with the chemical structures as in Formula 1.

摘要翻译： 这是一种生产无载体添加的O-（2- [叔丁基]氟乙基）-L-酪氨酸的新方法，已被证明是合适的PET（位置发射断层摄影）探针， 肿瘤诊断成像和标题化合物的制备从具有式1化学结构的前体开始，其中R 1是羧基官能团的保护基，R 2， SUP>是氨基的保护基，R 3 3作为离去基团，R 1表示芳基烷基，R 2， 表示羧基，R 3表示对甲苯磺酰氧基，甲磺酰氧基或三氟甲磺酰氧基或溴，产物的最终纯化是使用分离柱，这对于自动合成非常方便， 本发明使用具有式1化学结构的前体。

公开(公告)号：US07138540B1

公开(公告)日：2006-11-21

申请号：US11162287

申请日：2005-09-06

申请人： Jenn Tzong Chen ,  Wuu Jyh Lin ,  Ai Ren Lo ,  Ming Hsin Lee ,  Hsin Er Wang ,  Shih Yan Wu

发明人： Jenn Tzong Chen ,  Wuu Jyh Lin ,  Ai Ren Lo ,  Ming Hsin Lee ,  Hsin Er Wang ,  Shih Yan Wu

IPC分类号： C07C229/36

CPC分类号： C07C227/20 ,  C07C269/06 ,  Y02P20/55 ,  C07C229/36 ,  C07C271/22

摘要： This is a new precursor and new method for the synthesis of no-carrier-added O-(2-[18F]fluoroethyl)-L-Tyrosine which has been proved a suitable PET (position emission tomography) probe for tumor diagnosis imaging, the preparation of the title compound starts from precursors with the chemical structures as in Formula 1, wherein R1 is a protective group for the carboxyl functional group, R2 is a protective group for the amino group, and R3 acts as a leaving group. R1 represents an arylalkyl group, R2 represents a carboxyl group, and R3 represents a p-tosyloxy, methane sulfonyloxy or trifluoromethane sulfonyloxy or bromine, the invention includes a method for the syntheses of new precursors with the chemical structures as in Formula 1.

摘要翻译： 这是合成无载体添加的O-（2 - [[18 F] F]氟乙基）-L-酪氨酸的新的前体和新方法，已被证明是合适的PET（位置发射断层扫描 ）探针用于肿瘤诊断成像，标题化合物的制备从具有式1化学结构的前体开始，其中R 1是羧基官能团的保护基，R 2 作为氨基的保护基，R 3 3作为离去基团。 R 1表示芳基烷基，R 2表示羧基，R 3表示对甲苯磺酰氧基，甲磺酰氧基或三氟甲磺酰氧基或 溴，本发明包括用于合成具有式1化学结构的新前体的方法。