Synthesis of isotope-labeled HSP90 inhibitor: [(CD3)-C-13] and [C-14]-TAK-459

Plesescu Mihaela; Elliott Eric L.; Li Yuexian; Prakash Shimoga R.

首页> 外文期刊>Journal of Labelled Compounds and Radiopharmaceuticals >Synthesis of isotope-labeled HSP90 inhibitor: [(CD3)-C-13] and [C-14]-TAK-459

【24h】

Synthesis of isotope-labeled HSP90 inhibitor: [(CD3)-C-13] and [C-14]-TAK-459

机译：同位素标记的HSP90抑制剂的合成：[（CD3）-C-13]和[C-14] -TAK-459

获取原文

获取原文并翻译 | 示例

掌桥外文数据库（机构版） >>

开具论文收录证明 >>

文献代查 >>

页面导航

摘要
著录项
相似文献
相关主题

摘要

[(CD3)-C-13]-TAK-459 (1A), an HSP90 inhibitor, was synthesized from [(CD3)-C-13]-sodium methoxide in three steps in an overall yield of 29%. The key intermediate [(CD3)-C-13]-2-methoxy-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)pyridine was synthesized in two steps from 2,6-dibromopyridine and stable isotope-labeled sodium methoxide. [C-14]-TAK-459 (1B) was synthesized from [C-14(U)]-guanidine hydrochloride in five steps in an overall radiochemical yield of 5.4%. The key intermediate, [C-14]-(R)-2-amino-7-(2-bromo-4-fluorophenyl)-4-methyl-7,8-dihydropyrido[4,3-d] pyrimidin-5(6H)-one, was prepared by microwave-assisted condensation.

机译：由[（CD3）-C-13]-甲醇钠分三步合成HSP90抑制剂[（CD3）-C-13] -TAK-459（1A），总产率为29％。从2的两个步骤合成了关键中间体[（CD3）-C-13] -2-甲氧基-6-（4,4,5,5-四甲基-1,3,2-二氧杂硼烷-2-基）吡啶，6-二溴吡啶和稳定同位素标记的甲醇钠。由[C-14（U）]-盐酸胍分五个步骤合成[C-14] -TAK-459（1B），总放射化学产率为5.4％。关键中间体[C-14]-（R）-2-氨基-7-（2-溴-4-氟苯基）-4-甲基-7,8-二氢吡啶并[4,3-d]嘧啶-5（通过微波辅助缩合制备6H）-1。

著录项

来源
《Journal of Labelled Compounds and Radiopharmaceuticals》 |2014年第9期|共5页
作者
Plesescu Mihaela; Elliott Eric L.; Li Yuexian; Prakash Shimoga R.;
展开▼
作者单位

展开▼
收录信息
原文格式 PDF
正文语种 eng
中图分类药学;
关键词
(CD3)-C-13-TAK-459; C-14-TAK-459; microwave chemistry; HSP90 inhibitor;

机译：[（CD3）-C-13] -TAK-459;[C-14] -TAK-459;微波化学;HSP90抑制剂;

相似文献

外文文献
中文文献
专利

1. Synthesis of isotope-labeled HSP90 inhibitor: [(CD3)-C-13] and [C-14]-TAK-459 [J] . Plesescu Mihaela, Elliott Eric L., Li Yuexian, Journal of Labelled Compounds and Radiopharmaceuticals . 2014,第9期

机译：同位素标记的HSP90抑制剂的合成：[（CD3）-C-13]和[C-14] -TAK-459
2. Synthesis of [H-3], [C-13(3), N-15], and [C-14]SCH 900567: an inhibitor of TNF-alpha (tumor necrosis factor alpha) converting enzyme (TACE) [J] . Ren Sumei, Hesk David, McNamara Paul, Journal of Labelled Compounds and Radiopharmaceuticals . 2014,第11期

机译：[H-3]，[C-13（3），N-15]和[C-14] SCH 900567的合成：TNF-α（肿瘤坏死因子α）转化酶（TACE）的抑制剂
3. Synthesis of C-14 and C-13, H-2-labeled IKK inhibitor:[~(14)C] and [~(13)C_4,D_3]-N-(6-chloro-7-methoxy-9H-pyrido[3,4-b]indol-8-yl)-2-methyl-3-pyridinecarboxamide [J] . Yuexian Li, Mihaela Plesescu, Shimoga R. Prakash Journal of Labelled Compounds and Radiopharmaceuticals . 2006,第9期

机译：H-14标记的IKK抑制剂C-14和C-13的合成：[〜（14）C]和[〜（13）C_4，D_3] -N-（6-氯-7-甲氧基-9H-吡啶基[3,4-b]吲哚-8-基）-2-甲基-3-吡啶甲酰胺
4. SYNTHESIS OF TWO C-14 LABELED CYCLOOXYGENASE-II INHIBITORS VIA A PUMMERER DEGRADATION-RESYNTHESIS STRATEGY [C] . Charles S. Elmore, Dennis C. Dean, Tina M. Marks, International Symposium on the Synthesis and Applications of Isotopes and Isotopically Labelled Compounds . 2004

机译：通过Pammerer降解 - 重新合成策略合成两种C-14标记的环氧基酶-II抑制剂
5. The role of NQO1 in the metabolism of benzoquinone ansamycin Hsp90 inhibitors and development of novel Hsp90 inhibitors as anticancer agents. [D] . Guo, Wenchang. 2007

机译：NQO1在苯醌安沙霉素Hsp90抑制剂的代谢中的作用以及新型Hsp90抑制剂作为抗癌剂的开发。
6. Cell-based assay of MGAT2-driven diacylglycerol synthesis for profiling inhibitors: use of a stable isotope-labeled substrate and high-resolution LC/MS [O] . Joelle M. Onorato, Ching-Hsuen Chu, Zhengping Ma, 2015

机译：MGAT2驱动的二酰基甘油合成用于谱抑制剂的基于细胞的测定：使用稳定的同位素标记的底物和高分辨率LC / MS
7. Compound-specific C-13 and C-14 measurements improve the understanding of soil organic matter dynamics [O] . Mendez-Millan M., Tu T. T. Nguyen, Balesdent J., 2014

机译：特定于化合物的C-13和C-14测量值可增进对土壤有机质动力学的了解

Synthesis of isotope-labeled HSP90 inhibitor: [(CD3)-C-13] and [C-14]-TAK-459

摘要

著录项

相似文献

相关主题

期刊订阅