Synthesis of C-14-labelled satigrel

被引:0
作者
Tanaka, S [1 ]
Yamagishi, Y [1 ]
Kusano, K [1 ]
Yoshimura, T [1 ]
机构
[1] EISAI & CO LTD,TSUKUBA RES LABS,TSUKUBA,IBARAKI 30026,JAPAN
关键词
anti-platelet aggregation agent; C-14-labelled satigrel; 4-cyano-5-(4'-methoxy[ring-U-C-14]phenyl)-5-(4''-methoxyphenyl)-4-pentenoic acid; synthesis;
D O I
暂无
中图分类号
Q5 [生物化学];
学科分类号
071010 ; 081704 ;
摘要
C-14-Labelled satigrel, or 4-cyano-5-(4'-methoxy [ring-U-C-14] phenyl)-5-(4 ''-methoxyphenyl)-4-pentenoic acid was synthesized for drug metabolism and pharmacokinetic studies using 4, 4'-dimethoxy [ring-U-C-14] benzophenone as the starting material. The radiochemical yield was 10.0%. The specific radioactivity and radiochemical purity, as determined by radio-HPLC analysis, were 10.3 MBq(277.2 mu Ci)/mg and 98.8%, respectively.
引用
收藏
页码:435 / 440
页数:6
相关论文
共 50 条
[41]   Synthesis of [2H4]oxymetazoline and [14C]oxymetazoline [J].
Brugger, Michelle L. ;
Borges, Scott ;
Ren, Sumei ;
McNamara, Paul .
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2010, 53 (13-14) :793-800
[42]   Synthesis and antibacterial activity of pleuromutilin derivatives with novel C(14) side chain [J].
Fu, Li Qiang ;
Ling, Chen Yu ;
Guo, Xing Sheng ;
He, Hui Li ;
Yang, Yu She .
CHINESE CHEMICAL LETTERS, 2012, 23 (01) :9-12
[43]   Total synthesis of [15N]-labelled C6-substituted purines from [15N]-formamide-easy preparation of isotopically labelled cytokinins and derivatives [J].
Bucek, Jan ;
Zatloukal, Marek ;
Havlicek, Libor ;
Plihalova, Lucie ;
Pospisil, Tomas ;
Novak, Ondrej ;
Dolezal, Karel ;
Strnad, Miroslav .
ROYAL SOCIETY OPEN SCIENCE, 2018, 5 (11)
[44]   C-13-AND D-LABELLED 3-PHENYLPROPIONIC ACIDS; SYNTHESIS AND CHARACTERIZATION BY NMR AND MS SPECTRA [J].
Rosca, Sorin Ioan ;
Stan, Raluca ;
Ungureanu, Eleonora-Mihaela ;
Stanciu, Gabriela ;
Rosca, Sanziana .
UNIVERSITY POLITEHNICA OF BUCHAREST SCIENTIFIC BULLETIN SERIES B-CHEMISTRY AND MATERIALS SCIENCE, 2008, 70 (04) :77-84
[45]   An efficient Perkin synthesis of 13C-labelled cinnamic acids from acetic acid as the source of the rare isotope [J].
Lenz, Dominik ;
Koeppe, Benjamin ;
Tolstoy, Peter M. ;
Limbach, Hans-Heinrich .
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2019, 62 (07) :298-300
[46]   Synthesis of 3H-, 13C3-, and 14C-labeled Sch 727965 [J].
Lavey, C. Flader ;
Hesk, D. ;
Koharski, D. ;
Truong, V. ;
McNamara, P. .
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 2011, 54 (04) :196-201
[47]   Proprietary Synthesis of the C27-C35 Fragment of Eribulin and Its Elaboration toward the C14-C35 Subunit [J].
Kim, U. Bin ;
Samala, Srinivas ;
Jung, Jaehun ;
Song, Juyoung ;
Lee, Kee-Young ;
Oh, Chang-Young ;
Shin, Hyunik .
ORGANIC PROCESS RESEARCH & DEVELOPMENT, 2024, 28 (07) :2832-2843
[48]   SYNTHESIS OF 2 C-14-LABELED CATECHOL-O-METHYLTRANSFERASE INHIBITORS [J].
KARLSSON, C ;
HONKANEN, E .
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 1991, 29 (02) :237-239
[49]   A GENERAL-APPROACH TO THE SYNTHESIS OF C-14-LABELED PHOTOACTIVE ACRYLIC ACIDS [J].
MOHAMMAD, T ;
MORRISON, H .
JOURNAL OF LABELLED COMPOUNDS & RADIOPHARMACEUTICALS, 1991, 29 (09) :1019-1026
[50]   Synthesis of optically active 14α- and 14β-cheilanthanic esters [J].
Ungur, Nicon ;
Kulcitki, Veaceslav ;
Gavagnin, Margherita ;
Castelluccio, Francesco ;
Cimino, Guido .
SYNTHESIS-STUTTGART, 2006, (14) :2385-2391