专利号:US-2008287649-A1 优先权日:2006-12-29 标 题 :Methods for the synthesis of cyclic peptides 发明人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R 权利人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R 摘要:Methods for the synthesis of cyclic peptides are provided, as well as novel dipeptide compounds. The methods include the solid phase synthesis of a dipeptide, which is the coupled to a second peptide in a solid phase reaction. The peptide is then cyclized following the coupling reaction. The methods and dipeptides are particularly useful for the synthesis of MC-4 receptor agonist peptides.
专利号:EP-1960423-B1 优先权日:2004-12-30 标 题:Synthesis of peptide t-20 using peptide intermediate fragments 发明人:HAN YEUN-KWEI; JOHNSTON DAVID A; KHATRI HIRALAL N 权利人:HOFFMANN LA ROCHE 摘要:Methods for the solid phase synthesis of T-20 peptides and peptide intermediates, in particular methods involving synthesizing T-20 peptide intermediates at low loading factors to produce products having excellent purity and yield.
专利号:US-7544665-B2 优先权日:2004-12-30 标题 :Synthesis using peptide intermediate fragments 发明人:KHATRI HIRALAL N; HAN YEUN-KWEI; JOHNSTON DAVID A; HODGES L MARK 权利人:ROCHE COLORADO CORP 摘要:Methods for the solid phase synthesis of T-1249 peptides and peptide intermediates, in particular methods involving synthesizing T-1249 peptide intermediates at low loading factors to produce products having excellent purity and yield.
专利号:US-8227571-B2 优先权日:2007-12-11 标题 :Insulinotropic peptide synthesis using solid and solution phase combination techniques 发明人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R 权利人:CHEN LIN; HAN YEUN-KWEI; ROBERTS CHRISTOPHER R; ROCHE PALO ALTO LLC 摘要:The present invention relates to the preparation of insulinotropic peptides that are synthesized using a solid and solution phase (“hybridâ€?) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to add additional amino acid material to the third fragment which is then coupled to the second fragment and then the first fragment in solution. Alternatively, a different second fragment is coupled to the first fragment in the solid phase. Then, solution phase chemistry is then used to add additional amino acid material to a different third fragment. Subsequently, this different third fragment is coupled to the coupled first and different second fragment in the solution phase. The use of a pseudoproline in one of the fragments eases solid phase synthesis of that fragment and also eases subsequent solution phase coupling of this fragment to the other fragments. The present invention is very useful for forming insulinotropic peptides such as GLP-1(7-36) and its natural and non-natural counteparts.
专利号:US-7820858-B2 优先权日:2006-03-25 标 题 :Concise β2-amino acid synthesis via organocatalytic aminomethylation 发明人:CHI YONGGUI; GELLMAN SAMUEL H; POMERANTZ WILLIAM C; HORNE WILLIAM S; GUO LI; ENGLISH EMILY P 权利人:WISCONSIN ALUMNI RES FOUND 摘要:The present invention provides a method for the synthesis of β 2 -amino acids. The method also provides methods yielding α-substituted β-amino aldehydes and β-substituted γ-amino alcohols. The present method according to this invention allows for increased yield and easier purification using minimal chromatography or crystallization. The methods described herein are based on an aldehyde aminomethylation which involves a Mannich reaction between an aldehyde and a formaldehyde-derived N,O-acetal (iminium precursor) and a catalyst, such as, for example, L-proline or a pyrrolidine. The invention allows for large scale, commercial preparation of β 2 -amino acids.
专利号:US-8378066-B2 优先权日:2007-10-27 标 题 :Insulinotropic peptide synthesis using solid and solution phase combination techniques 发明人:KING BARRY THOMAS; BURY PAUL ADAM; GABEL RICHARD A; CRIDER JOHN EDWARD; CARR II ROBERT THAD; DEHOFF BRADLEY S 权利人:CORDEN PHARMA COLORADO INC; KING BARRY THOMAS; BURY PAUL ADAM; GABEL RICHARD A; CRIDER JOHN EDWARD; CARR II ROBERT THAD; DEHOFF BRADLEY S 摘要:The present invention relates to the preparation of insulinotropic peptides that are synthesized using a solid and solution phase (“hybridâ€?) approach. Generally, the approach includes synthesizing three different peptide intermediate fragments using solid phase chemistry. Solution phase chemistry is then used to add additional amino acid material to one of the fragments. The fragments are then coupled together in the solution phase. The use of a pseudoproline in one of the fragments eases solid phase synthesis of that fragment and also eases subsequent solution phase coupling of this fragment to other fragments. The present invention is very useful for forming insulinotropic peptides such as Exenatide(1-39) and its natural and non-natural counterparts.
参考标题:A Linker For The Solid-Phase Synthesis Of Hydroxamic Acids And Identification Of Hdac6 Inhibitors 作者:Claus G. Bang,Jakob F. Jensen,Emil O'Hanlon Cohrt,Lasse B. Olsen,Saba G. Siyum,Kim T. Mortensen,Tine Skovgaard,Jens Berthelsen,Liang Yang,Michael Givskov,Katrine Qvortrup,Thomas E. Nielsen |发布日期:2017.10.9 摘要:Readily Available And Nonintegral Hydroxylamine Linkers For The Routine Solid-Phase Synthesis Of Hydroxamic Acids. The Developed Protocols Enable The Efficient Synthesis And Release Of A Wide Range Of Hydroxamic Acids From Various Resins, Relying On High Control And Flexibility With Respect To Reagents And Synthetic Processes. A Trityl-Based Hydroxylamine Linker Was Used To Synthesize A Library Of Peptide