公开(公告)号：US07145000B2

公开(公告)日：2006-12-05

申请号：US10487480

申请日：2002-08-21

申请人： Joseph Antonius Maria Eisenbarth ,  Stefan Johannes Martin ,  Ulrike Wagner-Utermann ,  Michael Eisenhut

发明人： Joseph Antonius Maria Eisenbarth ,  Stefan Johannes Martin ,  Ulrike Wagner-Utermann ,  Michael Eisenhut

IPC分类号： C07H19/00 ,  C07H19/048 ,  C07H19/06

CPC分类号： C07D498/18 ,  C07H19/06 ,  Y02P20/55

摘要： What is described are compounds wherein R represents Br, I or R1—SO3, where R1 is an unsubstituted or substituted C1–C5-alkyl group, or an unsubstituted or substituted phenyl group; X is O or NR″, where R″ is a usual protective group for N; and R′ represents hydrogen, a halogen, such as F, Cl, and Br, a substituted or unsubstituted C1–C7-alkyl group, such as methyl and ethyl, a substituted or unsubstituted C2–C7-alkenyl group, or a substituted or unsubstituted C2–C7-alkynyl group.

摘要翻译： 描述的是其中R表示Br，I或R 1 -SO 3的化合物，其中R 1是未取代或取代的C

公开(公告)号：US06891033B2

公开(公告)日：2005-05-10

申请号：US10470817

申请日：2002-01-28

申请人： Stefan Johannes Martin ,  Joseph Antonius Maria Eisenbarth ,  Ulrike Wagner-Utermann ,  Michael Eisenhut ,  Walter Mier

发明人： Stefan Johannes Martin ,  Joseph Antonius Maria Eisenbarth ,  Ulrike Wagner-Utermann ,  Michael Eisenhut ,  Walter Mier

IPC分类号： C07H19/06 ,  A61K31/7072

CPC分类号： C07H19/06

摘要： The application relates to compounds that are suitable as labelable precursors for synthesis of 3′-[18F]fluoro-3′-deoxythymidine and that have formula (1), in which R denotes triphenylmethyl, triphenylmethyl substituted in the phenyl group, trialkylmethyl, triphenylsilyl, triphenylsilyl substituted in the phenyl group, or trialkylsilyl, R′ denotes R1—SO2, where R1 is an unsubstituted or substituted C1 to C5 alkyl or an unsubstituted or substituted phenyl, and R″ denotes C2 to C10 alkyloxycarbonyl, with the exception of 3-N-Boc-1-(3-O-nosyl-5-O-trityl-2-deoxy-β-D-lyxofuranosy The application also relates to a method for preparation of these compounds and to the use of the same for synthesis of 3′-[18F]fluoro-3′-deoxythymidine.

摘要翻译： 本申请涉及适用于合成3' - [16 F]氟-3'-脱氧胸苷的可标记前体的化合物，其具有式（1），其中R表示三苯基甲基，三苯基甲基取代的 在苯基中，三烷基甲基，三苯基甲硅烷基，苯基取代的三苯基甲硅烷基或三烷基甲硅烷基，R'表示R 1 -SO 2 - ，其中R 1， SUP>是未取代或取代的C 1至C 5烷基或未取代或取代的苯基，R“表示C 2至C 除了3-N-Boc-1-（3-O-壬基-5-O-三苯甲基-2-脱氧-β-D-吡喃葡萄糖醛酸之外），除了3-N-Boc- 1-烷氧基羰基外，本申请还涉及 制备这些化合物的方法及其用于合成3' - [[18 F]氟-3'-脱氧胸苷的方法。