对氰基苯甲酸置于镍体系中,用 甲醇 作为反应溶剂,化学反应 16.0H,以to Afford 4-(Aminomethyl)Benzoic Acid (430 G,84%) As A White Solid的收率获得产物4-氨甲基苯甲酸 参考文献:Benzothiazole Formulations And Use Thereof 标题:Benzothiazole Formulations And Use Thereof 摘要:本发明涉及含有苯并噻唑衍生物的聚乙二醇甘油酯制药配方.特别地,本发明涉及苯并噻唑硬脂酰聚乙二醇制药配方,制备方法及其用途.
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-2024024493-A1 优先权日:2022-06-22 标 题 :Purification methods for large scale synthesis of cucurbit[7]uril-peg conjugates 发明人:WEBBER MATTHEW J 权利人:PORTAL INSULIN LLC 摘要:Methods of purification for the large scale synthesis of CB[ 7 ]-PEG may include at least one of diafiltration or tangential flow filtration, column chromatography, affinity “pull-downâ€? techniques, or selective precipitation methods. In one embodiment, the method includes providing a reaction mixture containing synthesized CB[ 7 ]-PEG, providing a membrane selected to be below the nominal molecular weight of CB[ 7 ]-PEG, and removing small molecular weight contaminant species from the reaction mixture using the membrane. In embodiments, regardless of which purification method is used, a copper catalyst component of the “clickâ€? chemistry reaction mixture may be removed using a commercially available metal-chelating resin.
专利号:US-2025090698-A1 优先权日:2018-11-27 标题 :Small molecule inhibitors for early diagnosis of prostate specific membrane antigen cancers and neurodegenerative diseases 发明人:CHELVAM VENKATESH; SENGUPTA SAGNIK; KRISHNAN MENA ASHA; PANDIT AMIT 权利人:INDIAN INSTITUTE OF TECH INDORE 摘要:Accordingly, embodiments herein disclose a conjugate D-E-F having binding affinity≤60 nM; wherein D comprises AAPT ligand or derivative thereof, E comprises a spacer comprising AA1, AA2, AA3 and/or AA4 and F is a chelating group. The conjugate also comprising AAPT ligand conjugated arene chelating linker for delivery of 99mTc radioisotope. Another embodiment also discloses a AAPT-PCa DOTA bioconjugate. An embodiment also discloses method of solid phase synthesis of AAPT-ligand. It also discloses a method of solid phase synthesis of AAPT-PCa DOTA bioconjugate for delivering of radioisotopes.
专利号:US-5880295-A 优先权日:1994-02-16 标 题 :Process for the preparation of diamine intermediates useful in the synthesis of HIV protease inhibitors 发明人:KALTENBACH III ROBERT FRANK 权利人:DU PONT PHARM CO 摘要:The present invention provides a process for the preparation of compounds of formula (V) below, and analogs thereof, which are useful as intermediates for the synthesis of HIV protease inhibitors, including cyclic ureas. ##STR1##
专利号:US-9206222-B2 优先权日:2009-06-29 标题:Solid phase peptide synthesis of peptide alcohols 发明人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN 权利人:CAUSSIL-AMBLARD MURIEL; MARTINEZ JEAN; TAILHADES JULIEN; CENTRE NAT RECH SCIENT 摘要:The present invention relates to the synthesis of depsipeptides on solid phase support. Said depsipeptides are then implicated in a solution phase O—N acyl shift enabling to obtain the corresponding peptide alcohols.
专利号:US-2023212788-A1 优先权日:2020-03-26 标 题:New method for automated on-demand biomolecular array synthesis 发明人:ZHANG YIXIN; LIN WEILIN 权利人:UNIV DRESDEN TECH 摘要:The invention provides an amphiphilic coating for the direct and rapid synthesis of an array of peptides and small molecular compounds on a planar surface of a solid support, comprising a hydrophilic chemical structure and a lipophilic group, wherein said peptides and small molecular compounds differ from spot to spot from each other in the chemical structure, characterized in that said amphiphilic coating possesses low wettability to polar aprotic solvents used in the array synthesis; said amphiphilic coating possessing low wettability is designed that it can be converted to a coating possessing high wettability by hydrolysis of the lipophilic group; and said amphiphilic coating comprises an amino group for the reaction with an electrophilic reagent. The invention further provides a solid support comprising said amphiphilic coating and a method for method for the direct and rapid synthesis of an array of peptides and small molecular compounds on a planar surface of a solid support, wherein said planar surface of a solid support comprises said amphiphilic coating. Said method includes the enhancing of the wettability of a glass surface to organic solvents to realize automated on-demand biomolecular array synthesis comprising both, peptides and small molecular compounds. The amphiphilic surface can be switched to a hydrophilic surface, resulting in high density arrays suitable for protein- and cell-based screening.
摘要:Osuna Gálvez, A.; Bode, J. W., Science of Synthesis Knowledge Updates, (2020) 1, 386. 摘要:Metternich, J. B.; Mudd, R. J.; Gilmour, R., Science of Synthesis: Photocatalysis in Organic Synthesis, (2017) 1, 394. 摘要:S72 | NTUPHTW | Pharmaceutically Active Substances from National Taiwan University | DOI:10.5281/zenodo.3955664 参考文献:10.1021/jo049840c 摘要:Loris A, Perosa A, Selva M, Tundo P. Selective N,N-Dibenzylation of Primary Aliphatic Amines with Dibenzyl Carbonate in the Presence of Phosphonium Salts. J. Org. Chem. 2004 May 01;69(11):3953–6. doi: 10.1021/jo049840c. 参考文献:10.1007/s12033-011-9402-x 摘要:Thiele A, Stangl GI, Schutkowski M. Deciphering enzyme function using peptide arrays. Mol Biotechnol. 2011 Nov;49(3):283–305. doi: 10.1007/s12033-011-9402-x.