专利号:WO-2024185734-A1 优先权日:2023-03-03 标 题:Polyphosphorylated nucleoside, phosphate-activated nucleotide used for synthesis of polyphosphorylated nucleoside and method for synthesis of same, and method for synthesis of polyphosphorylated nucleoside using phosphate-activated nucleotide 发明人:KATAOKA MASANORI; FUKUI CHIHARU; TSUJI YOHEI; FUJIMURA Kazuma 权利人:NATIAS INC 摘要:The present invention provides: a polyphosphorylated nucleoside which has a structure represented by formula (I) and can be efficiently produced by a short process and a simple operation with use of a less expensive material; a phosphate-activated nucleotide which is used for the synthesis of the polyphosphorylated nucleoside and a method for the synthesis of this phosphate-activated nucleotide; and a method for the synthesis of a polyphosphorylated nucleoside using a phosphate-activated nucleotide. In the formula, B represents a protected or unprotected, natural or artificial nucleoside base; R 1 , R 2 , R 4 and R 5 each represent H or an alkyl group or the like, and R 1 , R 2 , R 4 and R 5 may be the same as or different from each other; X and Y each represents H, OH, OCH 3 or the like; h represents an integer of 1 to 3; p, n, m and q each represent 0 or an integer, and p, n, m and q are in no particular order; and (p + n + m + q) is an integer of 0 to 5,000.
专利号:US-10961273-B2 优先权日:2016-08-16 标 题 :N-carboxyanhydride-based-scale synthesis of elamipretide 发明人:DUNCAN SCOTT M; OUDENES JAN; ANDERSEN MARC W 权利人:STEALTH BIOTHERAPEUTICS CORP 摘要:Disclosed are methods of making elamipretide (MTP-131), a peptide compound with therapeutic potential for treating various mitochondrial myopathies. The synthesis of the peptide can be achieved via the use of N-carboxyanhydride-modified amino acid residues, which increases the efficiency of the synthetic process and the purity of the peptide product generated.
专利号:US-2024218014-A1 优先权日:2022-11-21 标 题:Synthesis of a cyclic peptide 发明人:BAUR PIUS BRUNO; CLEATOR EDWARD; DENIAU GILDAS; EISELE FRANK; FLÖGEL OLIVER; HUSTE ANJA; KEHL MARCEL ROMAN; LÖWENECK MARKUS; SILVA ROLANDO RAVELO; VORBERG RAFFAEL 权利人:JANSSEN PHARMACEUTICA NV 摘要:Processes for performing peptide synthesis, particularly for cyclic peptide synthesis are generally described. Reaction intermediates of the peptide synthesis are also described.
专利号:US-11851651-B2 优先权日:2017-06-19 标 题 :Automated methods for scalable, parallelized enzymatic biopolymer synthesis and modification using microfluidic devices 发明人:BANAL JAMES; BERLEANT JOSEPH DON; SHEPHERD TYSON; BATHE MARK 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:Methods for the automated template-free synthesis of user-defined sequence controlled biopolymers using microfluidic devices are described. The methods facilitate simultaneous synthesis of up to thousands of uniquely addressed biopolymers from the controlled movement and combination of regents as fluid droplets using microfluidic and EWOD-based systems. In some forms, biopolymers including nucleic acids, peptides, carbohydrates, and lipids are synthesized from step-wise assembly of building blocks based on a user-defined sequence of droplet movements. In some forms, the methods synthesize uniquely addressed nucleic acids of up to 1,000 nucleotides in length. Methods for adding, removing and changing barcodes on biopolymers are also provided. Biopolymers synthesized according to the methods, and libraries and databases thereof are also described. Modified biopolymers, including chemically modified nucleotides and biopolymers conjugated to other molecules are described.
专利号:WO-2013177713-A1 优先权日:2012-05-31 标题 :Process for preparation of an antifolate agent 发明人:GIUST WALTER; BURTON RYAN; GORIN BORIS; CLAYTON JOSHUA 权利人:ALPHORA RES INC 摘要:The specification relates to a process for preparation of an antifolate compound of formula 7, such as Pralatrexate. Also, disclosed are intermediates and processes for preparation of intermediates useful in the preparation of the antifolate compound. The substituents Y, Z, R, R 1 and R 2 are as described herein. The processes and intermediates can provide an alternate route to the synthesis of the antifolate compound. Further, the processes can help to avoid distillation or evaporation of high boiling point solvents, chromatographic purification and use of hazardous combination of solvents; and can also provide a product having high purity, all of which are desirable for synthesis on a large scale.
专利号:US-10344069-B2 优先权日:2014-10-31 标 题:Process for the preparation of liraglutide 发明人:VADLAMANI SURESH KUMAR; DAGADU PATIL NILESH; SHAFEE MOHAMMED ABDUL; PATIL SANJAY DEVIDAS; AGASALADINNI NAGANA GOUD 权利人:AURO PEPTIDES LTD; VADLAMANI SURESH KUMAR; DAGADU PATIL NILESH; SHAFEE MOHAMMED ABDUL; PATIL SANJAY DEVIDAS; AGASALADINNI NAGANA GOUD 摘要:The present invention relates to a process for the preparation of Liraglutide, which comprises: a) synthesis of suitable fragments (protected) by solid phase peptide synthesis; b) coupling of the suitable fragments on solid support; c) concurrently cleaving the protected peptide from the solid support and de-protecting the peptide; d) purification of Liraglutide (crude) on reverse phase HPLC; e) isolating pure Liraglutide.
[参考文献]: Thipapun Plyduang, Et Al. Carboxymethylcellulose-Tetrahydrocurcumin Conjugates For Colon-Specific Delivery Of A Novel Anti-Cancer Agent, 4-Amino Tetrahydrocurcumin. Eur J Pharm Biopharm. 2014 Oct;88(2):351-60.
合成参考文献
参考文献:10.1055/s-0037-1611773 摘要:Hollanders K, Maes B, Ballet S. A New Wave of Amide Bond Formations for Peptide Synthesis. Synthesis. 2019 Apr 24;51(11):2261–77. doi: 10.1055/s-0037-1611773. 参考文献:10.1038/s44160-023-00343-1 摘要:Roth P, Meyer R, Harley I, Landfester K, Lieberwirth I, Wagner M, Ng DYW, Weil T. Supramolecular assembly guided by photolytic redox cycling. Nat. Synth. 2023 Jun 08;2(10):980–8. doi: 10.1038/s44160-023-00343-1.