专利号:US-9388131-B2 优先权日:2011-04-27 标题:Automated synthesis of small molecules using chiral, non-racemic boronates 发明人:BURKE MARTIN D; LI JUNQI; GILLIS ERIC P 权利人:UNIV ILLINOIS 摘要:Provided are methods for making and using chiral, non-racemic protected organoboronic acids, including pinene-derived iminodiacetic acid (PIDA) boronates, to direct and enable stereoselective synthesis of organic molecules. Also provided are methods for purifying PIDA boronates from solution. Also provided are methods for deprotection of boronic acids from their PIDA ligands. The purification and deprotection methods may be used in conjunction with methods for coupling or otherwise reacting boronic acids. Iterative cycles of deprotection, coupling, and purification can be performed to synthesize chiral, non-racemic compounds. The methods are suitable for use in an automated chemical synthesis process. Also provided is an automated small molecule synthesizer apparatus for performing automated stereoselective synthesis of chiral, non-racemic small molecules using iterative cycles of deprotection, coupling, and purification.
专利号:US-7344863-B2 优先权日:1998-03-13 标题:Methods for producing polypeptides through enhanced synthesis of encoding nucleic acid molecules 发明人:LI WU-BO; JESSEE JOEL A; SCHUSTER DAVID; XIA JIULIN; GEBEYEHU GULILAT 权利人:INVITROGEN CORP 摘要:The present invention is directed to compositions and methods for enhancing synthesis of nucleic acid molecules, particularly GC-rich nucleic acid molecules. Specifically, the invention provides compositions comprising one or more nitrogen-containing organic compounds having a formula selected from the group consisting of formula I and formula II (or salts or derivatives thereof), preferably 4-methylmorpholine N-oxide or betaine (carboxymethyltrimethylammonium), and further comprising one or more compounds selected from the group consisting of proline and an N-alkylimidazole compound, and more preferably proline, 1-methylimidazole or 4-methylimidazole. The invention further relates to methods for enhanced, high-fidelity synthesis of nucleic acid molecules, including via amplification (particularly PCR), reverse transcription, and sequencing methods. The invention also relates to nucleic acid molecules synthesized by these methods, to fragments or derivatives thereof, and to vectors and host cells comprising such nucleic acid molecules, fragments, or derivatives. The invention also relates to kits for synthesizing, amplifying, reverse transcribing or sequencing nucleic acid molecules comprising one or more of the compositions of the invention.
专利号:WO-03031376-A1 优先权日:2001-10-12 标 题 :Solid phase synthesis of substituted 1,5-benzodiazepine-2-one and 1,5-benzothiazepine-2-one 发明人:MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 权利人:AVENTIS PHARMA INC; MORTON GEORGE C; SALVINO JOSEPH M; LABAUDINIERE RICHARD F; HERPIN TIMOTHY F 摘要:A solid phase synthetic method for making substituted 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one. The method is useful for synthesis of large numbers of compounds through automated parallel synthesis or combinatorial library generation and is thus important to rapid discovery or new therapeutic agents containing the base structure of 1,5-benzodiazepine-2-one or 1,5-benzothiazepine-2-one.
专利号:US-2010069644-A1 优先权日:2008-09-15 标题:Method of regio-selective synthesis of tri-substituted-1, 2, 3-triazoles 发明人:SHI XIAODONG 权利人:SHI XIAODONG 摘要:The embodiments provide for region-selective synthesis of tri-substituted 1,2,3-traizoles. A first embodiment provides for the selective N-2 alkylation of a 4,5-disubstituted 1,2,3-triazole. A second embodiment provides for the selective acetylation of a 4,5-disubstituted 1,2,3-triazole. A third embodiment provides for the selective arylation of a 4,5-disubstituted 1,2,3-triazole.
专利号:US-8735586-B2 优先权日:2007-06-26 标 题 :Regioselective copper catalyzed synthesis of benzimidazoles and azabenzimidazoles 发明人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR 权利人:ALONSO JORGE; LINDENSCHMIDT ANDREAS; NAZARÉ MARC; URMANN MATTHIAS; HALLAND NIS; RKYEK OMAR; SANOFI SA 摘要:The present invention relates to a process for the regioselective synthesis of compounds of the formula I, n nwherein R0; R1; R2; R3; R4; R5; A1; A2; A3; A4, Q and J have the meanings indicated in the claims. The present invention provides a direct copper catalyzed regioselective process to a wide variety of unsymmetrical, multifunctional N-substituted benzimidazoles or azabenzimidazoles of formula I starting from 2-halo-nitroarenes and N-substituted amides.
专利号:US-10464958-B2 优先权日:2012-07-17 标题 :Method for the synthesis of alpha-aminoalkylenephosphonic acid 发明人:NOTTE PATRICK; COGELS SAMUEL; BURCK SEBASTIAN 权利人:MONSANTO TECHNOLOGY LLC 摘要:The present invention is related to a new method for the synthesis of alpha-aminoalkylenephosphonic acid or its phosphonate esters comprising the steps of forming a reaction mixture by mixing a P—O—P anhydride moiety comprising compound, having one P-atom at the oxidation state (+III) and the other P-atom at the oxidation state (+III) or (+V), an aminoalkanecarboxylic acid and an acid catalyst, wherein said reaction mixture comprises an equivalent ratio of alpha-aminoalkylene carboxylic acid to P—O—P anhydride moieties of at least 0.2, and recovering the resulting alpha-aminoalkylene phosphonic acid compound or an ester thereof from the reaction mixture.
1: Dhanjal DS, Bhardwaj S, Chopra C, Singh R, Patocka J, Plucar B, Nepovimova E, Valis M, Kuca K. Millennium Nutrient N,N-Dimethylglycine (DMG) and its Effectiveness in Autism Spectrum Disorders. Curr Med Chem. 2022;29(15):2632-2651. doi: 10.2174/0929867328666211125091811. 308(9):527-8. doi: 10.1056/NEJM198303033080918. 26(7-8):935-7. 46(7):946-954. doi: 10.1248/bpb.b23-00098. Epub 2023 May 13. 24(7):6696. doi: 10.3390/ijms24076696. 6: Yao H, Hu Y, Tong H, Shi S. Dimethylglycine Alleviates Metabolic Dysfunction- Associated Fatty Liver Disease by Improving the Circulating Estrogen Level via Gut Staphylococcus. J Agric Food Chem. 2023 Dec 22. doi: 10.1021/acs.jafc.3c07075. Epub ahead of print. 243(2):396-407. doi: 10.1016/0003-9861(85)90516-8.
合成参考文献
摘要:TSAI,RS ET AL. (1991) 参考文献:10.1016/j.bbrc.2014.05.064 摘要:Luka Z, Pakhomova S, Loukachevitch LV, Newcomer ME, Wagner C. Folate in demethylation: The crystal structure of the rat dimethylglycine dehydrogenase complexed with tetrahydrofolate. Biochemical and Biophysical Research Communications. 2014 Jul;449(4):392–8. doi: 10.1016/j.bbrc.2014.05.064. 参考文献:10.1128/aem.00377-18 摘要:Shao YH, Guo LZ, Zhang YQ, Yu H, Zhao BS, Pang HQ, Lu WD. Glycine Betaine Monooxygenase, an Unusual Rieske-Type Oxygenase System, Catalyzes the Oxidative N-Demethylation of Glycine Betaine in Chromohalobacter salexigens DSM 3043. Appl Environ Microbiol. 2018 Jul 01;84(13).