专利号:US-11945838-B2 优先权日:2018-12-20 标 题:Method for synthesis of protein amphiphiles 发明人:BRITTO Sandanaraj Selvaraj; REDDY Mullapudi Mohan 权利人:INDIAN INSTITUTE OF SCIENCE EDUCATION AND RES 摘要:The present invention discloses a novel cost effective method for synthesis of protein/peptide amphiphiles irrespective of functional and structural classification of proteins useful in designing a vaccine candidate from antigenic protein. The protein modification of the present invention is universal and hence any protein/peptide can be converted into amphiphilic proteins/peptides.
专利号:US-7589170-B1 优先权日:1998-09-25 标题 :Synthesis of cyclic peptides 发明人:SMYTHE MARK LESLIE; MEUTERMANS WIM DENIS FRANS; BOURNE GREGORY THOMAS; MCGEARY ROSS PETER 权利人:UNIV QUEENSLAND 摘要:This invention relates to methods for preparing cyclic peptides and peptidomimetic compounds in solution and bound to solid supports, and to cyclic peptide or peptidomimetic libraries for use in drug screening programs. In particular, the invention relates to a generic strategy for synthesis of cyclic peptides or peptidomimetics that enables the efficient synthesis under mild conditions of a wide variety of desired compounds. Two approaches were evaluated for their improvements in solution and solid phase synthesis of small cyclic peptides: positioning reversible N-amide substituents in the sequence; and applying native ligation chemistry in an intramolecular sense. Systematic investigation of the effects of preorganising peptides prior to cyclisation by using peptide cyclisation auxiliaries, and developing new linkers and peptide cyclisation auxiliaries to aid cyclic peptide synthesis gives surprising improvements in both yields and purity of products compared to the prior art methods. The combination of these technologies provides a powerful generic approach for the solution and solid phase synthesis of small cyclic peptides. The ring contraction and N-amide substitution technology of the invention provide improved methods for the synthesis of cyclic peptides and peptidomimetics. When used in conjunction with linker strategies, this combination provides solid-phase avenues to cyclic peptides and peptidomimetics.
专利号:US-8350031-B2 优先权日:2008-06-02 标 题:Processes for the synthesis of levocetirizine and intermediates for use therein 发明人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 权利人:CIPLA LTD; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 摘要:The present invention provides a compound of formula (IV) n nwherein R is Cl, Br, NO 2 , OH or OR′, and R′ is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (−)-1-[(4-chlorophenyl)-phenylmethyl]piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).
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:WO-2023012709-A1 优先权日:2021-08-05 标 题 :An improved process for fmoc synthesis of semaglutide 发明人:LOBO LESTER JOHN; CHANDRAKESAN MURALIDHARAN; DOSHI CHETAN; CHANADAK SHAILESH LALCHAND; YADAV NANDLAL GOPAL; MOHE NIKHIL UMESH; VISHWANATHAN KODANDARAMAN 权利人:USV PRIVATE LTD 摘要:The present invention relates to an improved process for the synthesis of glucagon-like-peptide-1 (GLP-1) and its analogs by using combination of solid and solution phase synthesis of Fmoc protected amino acids in a sequential manner, optionally incorporating Boc protected dipeptide for unnatural amino acid in the Sequence of GLP-1, cleaving GLP-1 sequence from the resin followed by purification; attaching side-chain to the desired amino acid in the solution phase to synthesize desired GLP-1 analog, purifying it to Semaglutide. Temperature gradient is applied during initial coupling of amino acids to facilitate completion of difficult coupling reactions.
专利号:US-2004018598-A1 优先权日:2000-05-30 标题 :Bio-intermediates for use in the chemical synthesis of polyketides 发明人:SANTI DANIEL; ASHLEY GARY; MYLES DAVID C 摘要:The present invention relates to compounds made by a subset of modules from one or more polyketide synthase (“PKSâ€?) genes that are used as starting material in the chemical synthesis of novel molecules, particularly naturally occurring polyketides or derivatives thereof. The biologically derived intermediates (“bio-intermediatesâ€?) generally represent particularly difficult compounds to synthesize using traditional chemical approaches due to one or more stereocenters. In one aspect of the invention, an intermediate in the synthesis of epothilone is provided that feeds into the synthetic protocol of Danishefsky and co-workers. In another aspect of the invention, intermediates in the synthesis of discodermolide are provided that feed into the synthetic protocol of Smith and co-workers. By taking advantage of the inherent stereochemical specificity of biological processes, the syntheses of key intermediates and thus the overall syntheses of compounds like epothilone and discodermolide are greaty simplified.
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合成参考文献
参考文献:10.1107/s1600536811017351 摘要:Chen M, Lai X, Zhou C, Yang X. (S)-Benzyl 3-(4-hy-droxy-phen-yl)-2-(trityl-amino)-propano-ate. Acta Crystallogr Sect E Struct Rep Online. 2011 Jun 01;67(Pt 6):o1412.