专利号:US-6825378-B2 优先权日:2003-03-28 标 题 :Process for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid 发明人:KUMAR PRADEEP; FERNANDES RODNEY AGUSTINHO; GUPTA PRITI 权利人:COUNCIL SCIENT IND RES 摘要:The present invention provides a process for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid of formula (1). The present invention more particularly relates to a process using cyclohexylphenyl ketone for the synthesis of enantiomerically pure cyclohexylphenyl glycolic acid of formula (1).
专利号:US-2023174567-A1 优先权日:2020-05-22 标题:Synthesis of fluorinated nucleotides 发明人:ARMIGER TRAVIS; BELYK KEVIN M; BENKOVICS TAMAS; CHUNG CHEOL K; JI CHEN YINING; JOHNSON HEATHER CLAIRE; KLAPARS ARTIS; LIU ZHIJIAN; LIU ZHUQING; MOORE JEFFREY C; NEEL ANDREW J; PENG FENG; RUMMELT STEPHAN M; SALEHI MARZUARANI NASTARAN; SHERRY BENJAMIN D; SONG ZHIGUO JAKE; TURNBULL BEN WILLIAM HULME; WANG LU; XU FENG 权利人:MERCK SHARP & DOHME LLC 摘要:The present invention relates to efficient processes useful in the preparation of fluorinated nucleosides, such as (2S,3R,4S,5R)-5-(2-amino-6-oxo-1,6-dihydro-9H-purin-9-yl)-3-fluoro-4-hydroxy-2-(mercaptomethyl)tetrahydrofuran-3-yl dihydrogen phosphate, also known as 3′-fluoro-thio-guanosine monophosphate or 3′-F-thio-GMP. Such fluorinated nucleosides may be useful as a biologically active compound and or as an intermediate for the synthesis of more complex biologically active compounds. The present invention also encompasses intermediates useful in the disclosed synthetic processes and the methods of their preparation. (I)
专利号:US-2006154325-A1 优先权日:2005-01-10 标题 :Synthesis of epoxide based inhibitors of cysteine proteases 发明人:BOGYO MATTHEW; VERHELST STEVEN H 权利人:BOGYO MATTHEW; VERHELST STEVEN H 摘要:Epoxide based cysteine protease inhibitors containing peptide derivatives and methods for synthesizing them in sold phase are disclosed. Preferably, an epoxy succinyl “warheadâ€? (for binding to the enzyme) is prepared, having two amino acid residues or residue-like structures on either side. Natural and non-natural amino acids may be used. The present process may be carried out entirely on a solid support, with the proviso that a dipeptide like group is prepared prior to coupling to one side of the supported complex. The method lends itself to more efficient inhibitor synthesis, and may be employed with mixtures of peptide compounds, and various modifications of epoxides to create diverse libraries of inhibitors.
专利号:US-6906046-B2 优先权日:2000-12-22 标题 :Pharmaceutical uses and synthesis of benzobicyclooctanes 发明人:JACKSON RANDY W; DARWISH IHAB; BAUGHMAN TED A; HOWBERT J JEFFRY 权利人:CELLTECH R & D INC 摘要:Benzobicyclooctane compounds, their use in inhibiting cellular events involving TNF-α and IL-8, and in the treatment of inflammation events in general; a combinatorial library of diverse bicyclooctanes and process for their synthesis as a library and as individual compounds.
专利号:US-5801047-A 优先权日:1992-11-25 标题:Method for making stable extracellular tyrosinase and synthesis of polyphenolic polymers therefrom 发明人:DELLA-CIOPPA GUY RICHARD; GARGER JR STEPHEN JOHN; HOLTZ RICHARD BARRY; MCCULLOCH MICHAEL JAY; SVERLOW GENADIE GLEB 权利人:BIOSOURCE TECH INC 摘要:A process for the in vitro production of chemically modified polyphenolic polymer (PPP). First, stable, highly active extracellular tyrosinase is produced from genetically transformed microorganism such as Streptomyces antibioticus. The tyrosinase is then incubated with a reaction substrate such as 1-tyrosine, hydrolyzed protein, or an oligopeptide in combination with 1-tyrosine. The ratio of the oligopeptide/tyrosine combination as well as variation in the concentration of tyrosinase can be used to modify the color, the molecular size, and the spectral absorbance properties of the PPP produced. Alternatively, or additionally, oxidants such as hydrogen peroxide or hypochlorite can be used to modify the color of the PPP, regardless of the method used to produce the PPP, and the PPP can subsequently be fractionated using molecular weight cut-off ultrafiltration. Organic solvents can also be used in the method of making PPP to produce PPPs having variable but reproducible physical properties.
专利号:US-6140529-A 优先权日:1998-10-22 标 题 :Synthesis of optically active cyclohexylphenylglycolate esters 发明人:BAKALE ROGER P; LOPEZ JORGE L; MCCONVILLE FRANCIS X; VANDENBOSSCHE CHARLES P; SENANAYAKE CHRIS HUGH 权利人:SEPRACOR INC 摘要:A process for the preparation of optically active cyclohexylphenylglycolate esters is described. The process utilizes carboxylic acid activation to couple (R)- or (S)-cyclohexylphenylglycolic acid (CHPGA) with 4-N,N-diethylamino butynol or other propargyl alcohol derivatives. The preparation of the hydrochloride salt is also described. In addition, a resolution process employing tyrosine methyl ester enantiomers for preparing a single enantiomer of CHPGA from racemic CHPGA is disclosed.
摘要:Kubik, S., Science of Synthesis Knowledge Updates, (2013) 3, 295. 摘要:R.W. Hay and L.J. Porter. J. Chem. Soc., B 1967, 1261. 摘要:Kleemann A., Kutscher B., Reichert D., Bossart M., Pharmaceutical Substances, Thieme [Online], Stuttgart, (2025). 摘要:Graham, J. S.; Stanway-Gordon, H. A.; Waring, M. J., Science of Synthesis: DNA-Encoded Libraries, (2024) nan, 431. 参考文献:10.1007/s00726-011-0931-1 摘要:Abdolmaleki A, Mallakpour S, Borandeh S, Sabzalian MR. Fabrication of biodegradable poly(ester-amide)s based on tyrosine natural amino acid. Amino Acids. 2012 May;42(5):1997–2007. doi: 10.1007/s00726-011-0931-1.