专利号:US-10913747-B2 优先权日:2017-07-04 标题 :Efficient process for the preparation of sitagliptin through a very effective preparation of the intermediate 2,4,5-trifluorophenylacetic acid 发明人:DE LUCCHI OTTORINO; PADOVAN PIERLUIGI; BRASOLA ELENA 权利人:FIS FABBRICA ITALIANA SINTETICI SPA; F I S —FABBRICA ITALIANA SINTETICI S P A 摘要:Object of the present invention is an efficient process for the preparation of the active pharmaceutical ingredient Sitagliptine and the 2,4,5-trifluorophenylacetic acid (TFAA) and salt thereof, which is a key intermediate for the synthesis of Sitagliptine.
专利号:US-4111933-A 优先权日:1976-04-30 标题:Protection of functional groups during reaction and their subsequent restoration 发明人:ECKERT HEINER; UGI IVAR; KABBE HANS-JOACHIM 权利人:BAYER AG 摘要:In the process for preparing an organic compound of the formula n n A' -- X n n in which n X is an amino group, a hydroxyl group or a carboxyl group, and n A' is the remainder of the molecule, from an organic compound of the formula n n A -- X n n in which n A is the remainder of the molecule which can undergo reaction to form A', by converting A -- X into a compound of the formula n n A -- Z -- COOR n n in which n Z is --NH--, --O-- or a direct C--C bond, and n R is a radical of the formula ##STR1## IN WHICH Y is a direct C--C single bond, the --CHâ•?CH-- group or an arylene group, n R 1 to R 4 each independently is hydrogen, halogen or an alkyl, aryl, aralkyl, alkoxycarbonyl, alkylaminocarbonyl, arylaminocarbonyl or cycloalkylaminocarbonyl radical, or n R 1 + r 2 and R 3 + R 4 each independently completes a 5- or 6-membered carbocyclic ring, or n R 1 and R 3 conjointly with the grouping --C--Y--C-- forms a carbocyclic ring with 5 or 6 carbon atoms, and Hal is halogen, n Thereby to protect X, then converting A -- Z -- COOR into a compound of the formula n n A' -- Z -- COOR n n and then treating the compound A' -- Z -- COOR to restore the group X, the improvement which comprises effecting the treatment of the compound A' -- Z -- COOR with an alkali metal compound of a complex of monovalent cobalt. The process is applicable particularly to aminocarboxylic acids including intermediates from various stages of the synthesis of penicillins and cephalosporis.
专利号:US-3759898-A 优先权日:1971-09-14 标 题 :Synthesis of alpha-(carbo(5-indanyloxy)) benzylpenicillin 发明人:NAKANISHI S 权利人:PFIZER 摘要:THE PREPARATION OF A-(CARBO(5-INDANYLOXY))BENZYLPENICILLIN VIA THE ESTERIFICATION OF A-CARBOXYPENICILLIN WITH 5-INDANOL IN THE PRESENCE OF N, N''-DICYCLOHEXYLCARBODIIMIDE IN A REACTION-INERT SOLVENT AT A PH OF 2-8.
专利号:US-2004068141-A1 优先权日:2002-10-08 标 题 :Process for the synthesis of trifluorophenylacetic acids 发明人:ARMSTRONG JOSEPH D; DREHER SPENCER D; IKEMOTO NORIHIRO 摘要:The present invention addresses a process for the preparation of 2,4,5-trifluorophenylacetic acid using a Cu(I) salt as a catalyst.
专利号:US-2009111737-A1 优先权日:1999-05-24 标题:Novel antibacterial agents 发明人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 权利人:CHRISTENSEN BURTON G; MORAN EDMUND J; GRIFFIN JOHN H; JUDICE J KEVIN; MU YONGQI; PACE JOHN L; MAMMEN MATHAI; AGGEN JAMES 摘要:This invention relates to novel multibinding compounds (agents) that are antibacterial agents. The multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands in their monovalent (i.e., unlinked) state have the ability to bind to a an enzyme involved in cell wall biosynthesis and metabolism, a precursor used in the synthesis of the bacterial cell wall and/or the bacterial cell surface thereby interfere with the synthesis and/or metabolism of the cell wall. In particular the multibinding compounds of the invention comprise from 2-10 ligands covalently connected by a linker or linkers, wherein each of said ligands hasn a ligand domain capable of binding to penicillin binding proteins, a transpeptidase enzyme, a substrate of a transpeptidase enzyme, a beta-lactamase enzyme, pencillinase enzyme, cephalosporinase enzyme, a transglycoslase enzyme, or a transglycosylase enzyme substrate; Preferably, the ligands are selected from the beta lactam or glycopeptide class of antibacterial agents.
专利号:BR-112020010832-B1 优先权日:2017-12-05 标题 :CHEMICAL PROCESS FOR THE SYNTHESIS OF PYRAZOLIDINEDIONE HERBICIDAL COMPOUNDS
[参考文献]: V L Lapidus, Et Al. [参考文献]: Antibiotiki. 1981 May;26(5):357-60.
合成参考文献
摘要:Lewin, R.; Thompson, M. L.; Micklefield, J., Science of Synthesis: Biocatalysis in Organic Synthesis, (2015) 2, 148. 摘要:Zhang, J.; Liu, D.; Chen, Y., Science of Synthesis, (2021) , 326. 摘要:P. K. Glasoe and J. R. Hutchison, J. Phys. Chem. 68, 1562 (1964). 参考文献:10.2116/analsci.22.715 摘要:Tamaya K, Moriguchi S, Naito K, Takei S. Interpretation of solute retention of some monovalent inorganic anions in anion-exchange chromatography using a dicarboxylic Acid as an eluent. Anal Sci. 2006 May;22(5):715–9. doi: 10.2116/analsci.22.715. 参考文献:10.1107/s1600536810029764 摘要:Harrison JJ, Kingsford-Adaboh R, Gotoh K, Ishida H. Bis[(3-chloro-benz-yl)ammonium] 2-phenyl-propane-dioate dihydrate. Acta Crystallogr Sect E Struct Rep Online. 2010 Jul 31;66(Pt 8):o2168.