专利号:US-2006264608-A1 优先权日:2001-08-03 标题 :Bi-directional synthesis of oligoguanidine transport agents 发明人:WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C 权利人:WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C 摘要:Synthesis routes that can be adapted to large scale synthesis of oligoguanidine compounds such as oligoarginine compounds are described which use a perguanidinylation step to convert a group of ω-amino groups to the corresponding guanidinyl groups. These compounds find utility as transport agents. Modified oligoguanidine compounds are also described.
专利号:US-8829157-B2 优先权日:2004-06-14 标 题:Process for the synthesis of cyclic heptapeptide 发明人:SAKSENA DIVYA LAL; MURALIDHARAN CHANDRAKESAN; LOBO LESTER; PAWAR DIGAMBER SHRIPATI; MOHE NIKHIL UMESH; TARUR RADHAKISHNAN VENKATASUBRAMANIAN 权利人:SAKSENA DIVYA LAL; MURALIDHARAN CHANDRAKESAN; LOBO LESTER; PAWAR DIGAMBER SHRIPATI; MOHE NIKHIL UMESH; TARUR RADHAKISHNAN VENKATASUBRAMANIAN; USV LTD 摘要:The present invention relates to an improved process for the large scale synthesis of cyclic heptapeptide using Fmoc solid phase synthesis technique. The described process assembles the peptide on a solid support resin by coupling to one another by peptide bonds to obtain a peptide wherein the coupling of cysteine to the resin employs a combination of solvents to reduce cysteine racemization. The process described relates to the use of C1-C4 alcohols as total substitute to organic nitriles thus making the process cost effective, non-toxic and eco-friendly.
专利号:US-7317129-B2 优先权日:2002-06-07 标 题:Chemical synthesis of reagents for peptide coupling 发明人:RAINES RONALD T; KIESSLING LAURA L; NILSSON BRADLEY L; HE YI; SOELLNER MATTHEW B; HINKLIN RONALD J 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The present invention provides improved methods for synthesis of phosphinothiol reagents, as well as novel protected reagents, for use in formation of amide bonds, and particularly, for peptide ligation. The invention provides phosphine-borane complexes useful as reagents in the formation of amide bonds, particularly for the formation of an amide bond between any two of an amino acid, a peptide, or a protein.
专利号:WO-2023039068-A1 优先权日:2021-09-08 标题:Compositions and methods for synthesis of peptide nucleic acid intermediates 发明人:COULL JAMES M; GILDEA BRIAN D 权利人:NEUBASE THERAPEUTICS INC 摘要:The present disclosure provides intermediates for the synthesis of peptide nucleic acid (PNA) backbones and monomers, such as cyclic intermediates, and methods of making the same.
专利号:US-7067698-B2 优先权日:2001-08-03 标 题 :Bi-directional synthesis of oligoguanidine transport agents 发明人:WENDER PAUL A; VANDEUSEN CHRISTOPHER L; PATTABIRAMAN KANAKA; PELKEY ERIN T; JESSOP THEODORE C 权利人:UNIV LELAND STANFORD JUNIOR 摘要:Synthesis routes that can be adapted to large scale synthesis of oligoguanidine compounds such as oligoarginine compounds are described which use a perguanidinylation step to convert a group of ω-amino groups to the corresponding guanidinyl groups. These compounds find utility as transport agents. Modified oligoguanidine compounds are also described.
专利号:US-9938509-B2 优先权日:2010-12-08 标 题 :Biocatalysts and methods for the synthesis of armodafinil 发明人:ANG EE LUI; ALVIZO OSCAR; BEHROUZIAN BEHNAZ; CLAY MICHAEL D; COLLIER STEVEN J; EBERHARD ELLEN D; FAN FU; SONG SHIWEI; SMITH DEREK J; WIDEGREN MAGNUS; WILSON ROBERT; XU JUNYE; ZHU JUN 权利人:CODEXIS INC 摘要:The present invention relates to non-naturally occurring polypeptides useful for preparing armodafinil, polynucleotides encoding the polypeptides, and methods of using the polypeptides. The non-naturally occurring polypeptides of the present invention are effective in carrying out biocatalytic conversion of the (i) 2-(benzhydrylsulfinyl)acetamide to (−)-2-[(R)-(diphenylmethyl)sulfinyl]acetamide (armodafinil), or (ii) benzhydryl-thioacetic acid to (R)-2-(benzhydrylsulfinyl)acetic acid, which is a pivotal intermediate in the synthesis of armodafinil, in enantiomeric excess.
1: Zinellu A, Paliogiannis P, Carru C, Mangoni AA. Homoarginine and all-cause mortality: A systematic review and meta-analysis. Eur J Clin Invest. 2018 May 28:e12960. doi: 10.1111/eci.12960. [Epub ahead of print] Review. doi: 10.1021/jacs.8b01933. Epub 2018 Jun 4. 3: Baldassarri F, Schwedhelm E, Atzler D, Böger RH, Cordts K, Haller B, Pressler A, Müller S, Suchy C, Wachter R, Düngen HD, Hasenfuss G, Pieske B, Halle M, Edelmann F, Duvinage A. Relationship between exercise intervention and NO pathway in patients with heart failure with preserved ejection fraction. Biomarkers. 2018 Apr
合成参考文献
摘要:Faber, K.; Glueck, S. M., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 437. 摘要:Faber, K.; Glueck, S. M., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 1, 438. 参考文献:10.1007/s00424-002-0787-z 摘要:Levillain O, Marescau B, Possemiers I, De Deyn P. Dehydration modifies guanidino compound concentrations in the different zones of the rat kidney. Pflügers Archiv - European Journal of Physiology. 2002 May;444(1-2):143–52. doi: 10.1007/s00424-002-0787-z. 参考文献:10.1007/978-1-60327-058-8_31 摘要:Mouradov D, King G, Ross IL, Forwood JK, Hume DA, Sinz A, Martin JL, Kobe B, Huber T. Protein structure determination using a combination of cross-linking, mass spectrometry, and molecular modeling. Methods Mol Biol. 2008;426():459–74. doi: 10.1007/978-1-60327-058-8_31.