专利号:WO-2024201393-A1 优先权日:2023-03-29 标 题:Methods for the synthesis of nucleoside analogues and nucleosides analogues derived therefrom 发明人:BRITTON ROBERT; Muir Garrett; ANKETELL MATTHEW JAMES; HUXLEY COHAN; BAIKABI SUPING 权利人:UNIV FRASER SIMON 摘要:The present invention relates to methods for the synthesis of nucleoside analogues. More specifically, the present invention relates to methods for the synthesis of C4' substituted nucleoside analogues via the reaction of a soft nucleophile with a halohydrin ketone.
专利号:US-6624294-B2 优先权日:1999-01-08 标 题:Regioselective synthesis of 2′-O-modified nucleosides 发明人:KAWASAKI ANDREW M; FRASER ALLISTER S; MANOHARAN MUTHIAH; COOK P DAN; PRAKASH THAZHA P 权利人:ISIS PHARMACEUTICALS INC 摘要:Methods for the regioselective alkylation at the 2'-hydroxy position over the 3'-hydroxy position of nucleosides and nucleoside analogs, forming 2'-O-ester modified compounds, are disclosed. Reduction and derivatization of the 2'-O-ester provides 2'-O-modified nucleosides and nucleoside analogs useful for the synthesis of oligomeric compounds having improved hybridization affinity and nuclease resistance.
专利号:US-9388147-B2 优先权日:2009-11-13 标题 :Selective sphingosine 1 phosphate receptor modulators and methods of chiral synthesis 发明人:MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA; TIMONY GREGG ALAN; BROOKS JENNIFER L; PEACH ROBERT; SCOTT FIONA LORRAINE; HANSON MICHAEL ALLEN 权利人:RECEPTOS INC; CELGENE INTERNAT II SÃ?RL 摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
专利号:WO-2005103035-A1 优先权日:2004-04-23 标题:Modified fischer indole synthesis of eletriptan 发明人:ASHCROFT CHRISTOPHER PAUL 权利人:PFIZER LTD; ASHCROFT CHRISTOPHER PAUL; PFIZER 摘要:The present invention relates to a new process for the preparation of eletriptan (I), or its enantiomer comprising a modified Fischer indole synthesis, namely the reaction of a compound of formula (II), wherein R1 is a suitable hydrazine protecting group, with a compound of formula (III) wherein R2 is an aldehyde group (-CHO) or the functional equivalent thereof.
专利号:US-9394264-B2 优先权日:2009-11-13 标 题:Sphingosine 1 phosphate receptor modulators and methods of chiral synthesis 发明人:MARTINBOROUGH ESTHER; BOEHM MARCUS F; YEAGER ADAM RICHARD; TAMIYA JUNKO; HUANG LIMING; BRAHMACHARY ENUGURTHI; MOORJANI MANISHA 权利人:RECEPTOS INC 摘要:Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.
专利号:US-3790555-A 优先权日:1972-01-20 标 题:Octapeptide derivative of gonadotropinreleasing hormone 发明人:FLOURET G; COLE J 权利人:ABBOTT LAB 摘要:THE SYNTHESIS OF THE OCTAPEPTIDE TRP-SER-TYR-GLY-LEUARG-PRO-GLY-AMIDE CARRYING EASILY REMOVABLE PROTECTIVE GROUPS ON THE SER, TYR, ARG AND TRP MOIETIES IS DESCRIBED. THE NEW SYNTHESIS USES AS THE STARTING MATERIAL TWO TETRAPEPTIDE FRAGMENTS CARRYING EASILY REMOVABLE PROTECTIVE GROUPS. ONE OF THESE FRAGMENTS, TRP-SER-TYR-GLY-OH WITH SUITABLE PROTECTIVE GROUPS, ALSO IS A PART OF THE PRESENT INVENTION. AFTER COUPLING OF THE TWO FRAGMENTS, THE PROTECTIVE GROUP ON THE AMINO-N OF THE TRYPTOPHANE MOIETY IS REMOVED TO OBTAIN AN OCTAPEPTIDE CARRYING EASILY REMOVABLE PROTECTIVE GROUPS WHICH CAN BE RETAINED VHILE BULIDING UP THE MOLECULE TO THE DECAPEPTIDE CHAIN WHICH IS THE GONADOTROPIN-RELEASING HORMONE, AFTER REMOVAL OF THESE PROTECTIVE GROUPS.
摘要:Kantchev, E. A. B.; Organ, M. G., Science of Synthesis, (2009) 48, 18. 摘要:Zaidlewicz, M.; Krzemiński, M. P.; Dzieleńdziak, A., Science of Synthesis, (2009) 48, 359. 摘要:Kostikov, R.; Baird, M. S., Science of Synthesis, (2009) 48, 616. 摘要:Bruffaerts, J.; Vasseur, A., Science of Synthesis Knowledge Updates, (2016) 2, 160. 摘要:Bruffaerts, J.; Vasseur, A., Science of Synthesis Knowledge Updates, (2016) 2, 162.