专利号:US-6639059-B1 优先权日:1999-03-24 标 题 :Synthesis of [2.2.1]bicyclo nucleosides 发明人:KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M 权利人:EXIQON AS 摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs.
专利号:US-6734291-B2 优先权日:1999-03-24 标题:Synthesis of [2.2.1]bicyclo nucleosides 发明人:KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M 权利人:EXIQON AS 摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs
专利号:EP-1953140-A1 优先权日:2007-01-24 标 题 :Process for the preparation of ezetimibe and derivatives thereof 发明人:STIMAC ANTON; MOHAR BARBARA; STEPHAN MICHEL; BEVC MOJCA; ZUPET ROK; GARTNER ANDREJ; KROSELJ VESNA; SMRKOLJ MATEJ 权利人:KRKA 摘要:The present invention relates to the method of preparing of ezetimibe and in particular to novel intermediates for its synthesis and an improved process for preparing such intermediates. Said intermediates may be obtained in high yields and purity in a fast and cost efficient manner. The present invention relates to a novel crystalline form of ezetimibe as well.
专利号:US-2003092905-A1 优先权日:1999-03-24 标 题:Synthesis of [2.2.1]bicyclo nucleosides
专利号:EP-1326851-B1 优先权日:2000-10-13 标 题 :Substituted dipeptides as growth hormone secretagogues 发明人:DODGE JEFFREY ALAN; EVERS BRITTA; JUNGHEIM LOUIS NICKOLAUS; MUEHL BRIAN STEPHEN; RUEHTER GERD; THRASHER KENNETH JEFF 权利人:LILLY CO ELI 摘要:This invention relates to novel compounds which are useful in the modulation of endogenous growth hormone levels in a mammal. The invention further relates to novel intermediates for usein the synthesis of said compounds, as well as novel processes employed in these syntheses. Also included are methods of treating a mammal which include the administration of said compounds.
专利号:US-5202444-A 优先权日:1990-11-27 标题:Optically isomeric inositol and process for making optically active compound 发明人:OZAKI SHOICHIRO; AKIYAMA TAKAHIKO; KAGEYAMA KUNIO; MACHIDA MORIHISA 权利人:YOKOHAMA RUBBER CO LTD 摘要:Optically active diols and hydroxycarboxylic acids and their esters are produced by deriving 1L-1,2:5,6-di-O-cyclohexylidene-chiro-inositol from 1L-chiro-inositol as an asymmetric source, followed by introduction of a selected class of sterically hindering and asymmetrically reactive groups into the first-mentioned compound and by subsequent reduction of the resulting compound. Seven specific inositols are also derivable from synthesis of those ultimate compounds.
[参考文献]: B J Phillips, Et Al. The Effects Of 4Cmb, 4Hmb And Bc On Sce, Chromosome Aberration And Point Mutation In Cultured Chinese Hamster Ovary Cells. Mutat Res. 1982 Jan-Feb;100(1-4):263-9. [参考文献]: C F Arlett, Et Al. The Use Of Cultured Mammalian Cells The Ukems Collaborative Genotoxicity Trial (1981). Mutat Res. 1982 Jan-Feb;100(1-4):271-6. [参考文献]: D Scott, Et Al. Ukems Collaborative Genotoxicity Trial. Cytogenetic Tests Of 4Cmb, Bc And 4Hmb: Summary And Appraisal. Mutat Res. 1982 Jan-Feb;100(1-4):313-31. [参考文献]: J C Topham, Et Al. Ukems Genotoxicity Trial 1981. In Vivo Assay Systems. Mutat Res. 1982 Jan-Feb;100(1-4):381-7. [参考文献]: K Scott, Et Al. Assay Of 4Cmb, 4Hmb And Bc By The Micronucleus Tests--Subcutaneous Administration. Mutat Res. 1982 Jan-Feb;100(1-4):365-71.
合成参考文献
摘要:Margaretha, P., Science of Synthesis Knowledge Updates, (2014) 2, 414. 摘要:Ho, C.-Y.; Raja, D., Science of Synthesis: Knowledge Updates, (2023) 1, 55.