专利号:US-2016200665-A1 优先权日:2013-08-21 标 题:Synthesis of biphenylalaninol via novel intermediates 发明人:ZIMMERMANN AXEL; HERMSEN PETRUS JOHANNES; HANBAUER MARTIN HELMUT FRIEDRICH 权利人:DPX HOLDINGS BV 摘要:The invention relates to a novel synthesis route towards R-biphenylalaninol and to the intermediates applied in this synthesis route. The process according to the invention and the intermediate compounds are useful in the synthesis of pharmaceutically active compounds.
专利号:US-5877278-A 优先权日:1992-09-24 标题:Synthesis of N-substituted oligomers 发明人:ZUCKERMANN RONALD N; GOFF DANE A; NG SIMON; SPEAR KERRY; SCOTT BARBARA O; SIGMUND AARON C; GOLDSMITH RICHARD A; MARLOWE CHARLES K; PEI YAZHONG; RICHTER LUTZ; SIMON REYNA 权利人:CHIRON CORP 摘要:A solid-phase method for the synthesis of N-substituted oligomers, such as poly (N-substituted glycines) (referred to herein as poly NSGs) is used to obtain oligomers, such as poly NSGs of potential therapeutic interest which poly NSGs can have a wide variety of side-chain substituents. Each N-substituted glycine monomer is assembled from two 'sub-monomers' directly on the solid support. Each cycle of monomer addition consists of two steps: (1) acylation of a secondary amine bound to the support with an acylating agent comprising a leaving group capable of nucleophilic displacement by -NH2, such as a haloacetic acid, and (2) introduction of the side-chain by nucleophilic displacement of the leaving group, such as halogen (as a solid support-bound alpha -haloacetamide) with a sufficient amount of a second sub-monomer comprising an -NH2 group, such as a primary amine, alkoxyamine, semicarbazide, acyl hydrazide, carbazate or the like. Repetition of the two step cycle of acylation and displacement gives the desired oligomers. The efficient synthesis of a wide variety of oligomeric NSGs using automated synthesis technology of the present method makes these oligomers attractive candidates for the generation and rapid screening of diverse peptidomimetic libraries. The oligomers of the invention, such as N-substituted glycines (i.e. poly NSGs) disclosed here provide a new class of peptide-like compounds not found in nature, but which are synthetically accessible and have been shown to possess significant biological activity and proteolytic stability. Combinatorial libraries of cyclic compounds are disclosed wherein the cyclic compounds are comprised of at least one ring structure derived from cyclization of a peptoid backbone. The diversity of product compounds is generated by the sequential addition of substituted submonomers. The combinatorial library includes 10 or more, preferably 100 or more, and more preferably 1,000 or more distinct and different compounds. The library includes each of the product compounds in retrievable and analyzable amounts and preferably includes at least one biologically active compound. Methods of synthesizing the combinatorial libraries and assay devices produced using the libraries are disclosed as is methodology for screening for and obtaining biologically active cyclic organic compounds.
专利号:US-9139515-B2 优先权日:2011-08-19 标 题:Synthesis of R-biphenylalaninol 发明人:HERMSEN PETRUS JOHANNES; ERMANN PETER HANS; RIEBEL PETER HANS; WOLBERG MICHAEL; DE VRIES ANDREAS HENDRIKUS MARIA 权利人:HERMSEN PETRUS JOHANNES; ERMANN PETER HANS; RIEBEL PETER HANS; WOLBERG MICHAEL; DE VRIES ANDREAS HENDRIKUS MARIA; DPX HOLDINGS BV 摘要:This invention relates to a novel process for the synthesis of R-biphenylalaninol and to intermediate compounds that are formed in the process according to the invention, i.e. novel intermediates useful in the synthesis of R-biphenylalaninol. The invention also relates to R-biphenylalaninol, The process according to the invention, the intermediates to of R-biphenylalaninol and of R-biphenylalaninol are all useful in the synthesis of pharmaceutically active compounds.
专利号:US-2024383940-A1 优先权日:2021-03-31 标题 :Synthesis of trinucleotide and tetranucleotide caps for mrna production 发明人:ENDO ATSUSHI 权利人:MODERNA TX INC 摘要:Provided herein are methods of making trinucleotides and tetranucleotides for use as 5′ mRNA caps. The methods utilize a novel “top-downâ€? strategy and provide for synthesis of oligonucleotides with higher yields and increased efficiency compared to traditional methods. A key step of the methods disclosed, herein can also be adapted to utilize a “one-potâ€? approach, resulting in an increase in the yield of the final oligonucleotide product.
专利号:US-2023278959-A1 优先权日:2020-05-04 标题:Synthesis of Optically Active Indoline Derivatives Via Ruthenium(II)-Catalyzed Enantioselective C-H Functionalization 发明人:CUI XIN; LI ZHONG-YUAN; CHAMINDA LAKMAL HETTI HANDI 权利人:UNIV MISSISSIPPI STATE 摘要:Provided herein are a method of Ru(II)-catalyzed enantioselective synthesis of a cyclic compound and cyclic compounds formed therefrom. The method includes providing a precursor compound having an unfunctionalized C—H bond and activating the unfunctionalized C—H bond by reacting the precursor compound in the presence of co-catalysts including a Ru(II) arene complex and a chiral transient directing group (CTDG).
专利号:US-10918627-B2 优先权日:2016-05-11 标 题:Convergent and enantioselective total synthesis of Communesin analogs 发明人:MOVASSAGHI MOHAMMAD; LATHROP STEPHEN PAUL; POMPEO MATTHEW W; CHANG WEN-TAU TIMOTHY 权利人:MASSACHUSETTS INST TECHNOLOGY 摘要:A highly convergent biomimetic synthesis of a complex polycyclic scaffold has been successfully implemented. From these efforts, compounds having a structure of Formula (I): n nor a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R 1 -R 8 and m, n, r, s, t, and u are as defined herein, is provided. Methods of making such compounds are also disclosed as are methods for the treatment of cancer, various infectious diseases, and abnormal cardiovascular function.
[参考文献]: Niwa T, Et Al. Organic Acids And The Uremic Syndrome: Protein Metabolite Hypothesis In The Progression Of Chronic Renal Failure. Semin Nephrol. 1996 May;16(3):167-82. [参考文献]: Cynthia Stretch, Et Al. Prediction Of Skeletal Muscle And Fat Mass In Patients With Advanced Cancer Using A Metabolomic Approach. J Nutr. 2012 Jan;142(1):14-21. [参考文献]: David S Wishart, Et Al. Hmdb: A Knowledgebase For The Human Metabolome. Nucleic Acids Res. 2009 Jan;37(Database Issue):D603-10. [参考文献]: Davide Bressanello, Et Al. Urinary Metabolic Fingerprinting Of Mice With Diet-Induced Metabolic Derangements By Parallel Dual Secondary Column-Dual Detection Two-Dimensional Comprehensive Gas Chromatography. J Chromatogr A. 2014 Sep 26:1361:265-76. [参考文献]: Donald F Stec, Et Al. Alterations Of Urinary Metabolite Profile In Model Diabetic Nephropathy. Biochem Biophys Res Commun. 2015 Jan 9;456(2):610-4.
合成参考文献
参考文献:10.1203/pdr.0b013e31822d7860 摘要:Thomas EL, Parkinson JR, Hyde MJ, Yap IK, Holmes E, Doré CJ, Bell JD, Modi N. Aberrant adiposity and ectopic lipid deposition characterize the adult phenotype of the preterm infant. Pediatr Res. 2011 Nov;70(5):507–12. doi: 10.1203/pdr.0b013e31822d7860. 参考文献:10.4061/2011/263768 摘要:Weese JS, Blondeau JM, Boothe D, Breitschwerdt EB, Guardabassi L, Hillier A, Lloyd DH, Papich MG, Rankin SC, Turnidge JD, Sykes JE. Antimicrobial Use Guidelines for Treatment of Urinary Tract Disease in Dogs and Cats: Antimicrobial Guidelines Working Group of the International Society for Companion Animal Infectious Diseases. Veterinary Medicine International. 2011;2011():1–9. doi: 10.4061/2011/263768.