5-氯-1-苯并噻吩-2-羧酸置于喹啉,铜体系中,化学反应 0.5H,以18%的收率获得5-氯苯并噻吩 参考文献:新的5-取代的苯并[ B ]噻吩衍生物的合成 标题:新的5-取代的苯并[ B ]噻吩衍生物的合成 摘要:我们小组以前的工作涉及1-(芳基)-3-[4-(芳基)哌嗪-1-基]丙烷衍生物的合成,以寻找具有双重作用方式的新型高效抗抑郁药:5-羟色胺再摄取抑制和5-Ht 1A受体的亲和力[1-4].从这些研究中我们得出结论,3-[4-(芳基)哌嗪-1-基]-1-(苯并[ B ]噻吩-3-基)丙烷衍生物导致了最佳结果.该研究项目的继续,需要制备一些新的3-酰基-5-取代的苯并[ B ]噻吩,其在5位上具有广泛的取代基,范围从硝基到羟基衍生物.为了获得这些衍生物,我们尽可能地将相应的5-取代的苯并[ B ]噻吩酰化. Doi:10.1002/jhet.5570380502
专利号:WO-9427985-A1 优先权日:1993-05-28 标题 :Process for the preparation of substituted 3-halomethyl-benzothiophenes, benzofurans and -indoles and intermediates thereof 发明人:PRIDGEN LENDON NORWOOD 权利人:SMITHKLINE BEECHAM CORP; PRIDGEN LENDON NORWOOD 摘要:This invention relates to novel intermediates and processes for preparing useful intermediates of formula (I) which are useful in the synthesis of pharmaceutically active agents.
专利号:US-2005192265-A1 优先权日:2003-03-20 标 题:Cycloalkyl, lactam, lactone and related compounds, pharmaceutical compositions comprising same, and methods for inhibiting beta-amyloid peptide release and/or its synthesis by use of such compounds 发明人:THOMPSON RICHARD C; WILKIE STEPHEN; STACK DOUGLAS R; VANMETER ELDON E; SHI QING; BRITTON THOMAS C; AUDIA JAMES E; REEL JON K; MABRY THOMAS E; DRESSMAN BRUCE A; CWI CYNTHIA L; HENRY STEVEN S; MCDANIEL STACEY L; STUCKY RUSSELL D; PORTER WARREN J 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions that include a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:WO-9967219-A1 优先权日:1998-06-22 标 题:Compounds for inhibiting beta-amyloid peptide release and/or its synthesis 发明人:AUDIA JAMES E; PORTER WARREN J; THOMPSON RICHARD C; WILKIE STEPHEN C; STACK DOUGLAS R; SHI QING 权利人:ELAN PHARM INC; LILLY CO ELI; AUDIA JAMES E; PORTER WARREN J; THOMPSON RICHARD C; WILKIE STEPHEN C; STACK DOUGLAS R; SHI QING 摘要:Compounds of formula (I), wherein W is a cyclic group of the type (2); (3); Y is represented by the formula (II); these compounds inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:WO-9966934-A1 优先权日:1998-06-22 标 题 :CYCLIC AMINO ACID COMPOUNDS, PHARMACEUTICAL COMPOSITIONS COMPRISING SAME, AND METHODS FOR INHIBITING β-AMYLOID PEPTIDE RELEASE AND/OR ITS SYNTHESIS BY USE OF SUCH COMPOUNDS 发明人:AUDIA JAMES E; DRESSMAN BRUCE A; SHI QING 权利人:ELAN PHARM INC; LILLY CO ELI; AUDIA JAMES E; DRESSMAN BRUCE A; SHI QING 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6774125-B2 优先权日:1998-06-22 标 题:Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:AUDIA JAMES E; THOMPSON RICHARD C; WILKIE STEPHEN C; BRITTON THOMAS C; PORTER WARREN J; HUFFMAN GEORGE W; LATIMER LEE H 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
专利号:US-6509331-B1 优先权日:1998-06-22 标题:Deoxyamino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds 发明人:AUDIA JAMES E; THOMPSON RICHARD C; WILKIE STEPHEN C; BRITTON THOMAS C; PORTER WARREN J; HUFFMAN GEORGE W; LATIMER LEE H 权利人:ELAN PHARM INC; LILLY CO ELI 摘要:Disclosed are compounds which inhibit beta-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits beta-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.
摘要:Yoshikai, N.; Rayner, C. M.; Graham, M. A., Science of Synthesis Knowledge Updates, (2020) 2, 94. 摘要:Huang, J.; Ma, D., Science of Synthesis: Special Topics, (2022) 1, 12.