专利号:US-2025289827-A1 优先权日:2022-12-02 标 题:Morphic forms of a mutant braf degrader and methods of manufacture thereof 发明人:YU ROBERT T; HE MINSHENG; SCHNADERBECK MATTHEW J; KREGER BRIDGET; POLLOCK ROY MACFARLANE; JIANG SIYI; LI MEIQI; CHEN BOLU; LU JIANNAN 权利人:C4 THERAPEUTICS INC 摘要:Advantageous isolated morphic forms of (3R)-3-[6-[2-cyano-3-[[ethyl(methyl)sulfamoyl]amino]-6-fluorophenoxy]-4-oxoquinazolin-3-yl]-8-[2-[1-[3-(2,4-dioxo-1,3-diazinan-1-yl)-5-fluoro-1-methylindazol-6-yl]-4-hydroxypiperidin-4-yl]acetyl]-1-oxa-8-azaspiro[4.5]decane (Compound 1), which is a mutant BRAF degrader, and methods to prepare Compound 1 morphic forms for therapeutic applications are provided in the invention. The invention also provides improved methods for the synthesis of Compound 1, new pharmaceutical compositions comprising Compound 1, and new uses of Compound 1.
专利号:US-7642356-B2 优先权日:2005-09-16 标 题 :Process for preparing beta-ketoester compounds 发明人:SHIN HYUN IK; CHOI BO SEUNG; LEE JAE HOON 权利人:LG LIFE SCIENCES LTD 摘要:The present invention relates to a process for preparing a beta-keto ester compound of formula (1), which is an intermediate for the synthesis of quinolone antibiotics. Particularly, the present invention is characterized by the reaction of an organo nitrile compound with a salt of mono-alkyl malonate in the presence of metal salt, and so the reaction is easy to control due to its endothermic nature, and is devoid of lachrymatory reagents with excellent reproducibility. Subsequent in situ hydrolysis in the presence of aqueous acid solution provided the compound of formula (1).
专利号:US-6987199-B2 优先权日:2001-10-15 标题 :Process for preparing beta-ketoester compound 发明人:SHIN HYUN-LK; CHOI BO-SEUNG; CHOI SANG-CHUL 权利人:LG LIFE SCIENCES LTD 摘要:The present invention relates to a new process for preparing beta-ketoester compound of the following formula (1), which is a useful intermediate for the synthesis of such quinoline antibiotics as Ciprofloxacin, Levofloxacin, Gemifloxacin, Trovafloxacin, etc. The quinoline antibiotics obtained from the above compound of formula (1) show potent antibacterial activity, and so are advantageously used as a therapeutic agent for bacterial infections of humans or animals.
专利号:US-6090805-A 优先权日:1997-06-18 标 题 :Tocolytic oxytocin receptor antagonists 发明人:WILLIAMS PETER D; SPARKS MICHELLE A; BELL IAN; PERLOW DEBRA S; STAUFFER KENNETH; FREIDINGER ROGER M 权利人:MERCK & CO INC 摘要:This invention relates to certain novel benzoxazinone compounds and derivatives thereof, their synthesis, and their use as oxytocin receptor antagonists. One application of these compounds is in the treatment of preterm labor in mammals, especially humans. The ability of the compounds to relax uterine contractions in mammals also makes them useful for treating dysmenorrhea and stopping labor prior to cesarean delivery.
专利号:CN-117466729-A 优先权日:2023-12-28 标题:A kind of synthesis method of 2,4,5-trifluorophenylacetic acid
专利号:CN-117486706-A 优先权日:2024-01-02 标题:A kind of synthesis method of 2,4,5-trifluorophenylacetic acid
[参考文献]: V Mukherjee, Et Al. Quantum Chemical Determination Of Molecular Geometries And Interpretation Of Ftir And Raman Spectra For 2,4,5- And 3,4,5-Tri-Fluoro-Benzonitriles. Spectrochim Acta A Mol Biomol Spectrosc. 2008 Dec 15;71(4):1571-80.
合成参考文献
参考文献:10.1055/s-0033-1338535 摘要:Woydziak ZR, Fu L, Peterson BR. Efficient and Scalable Synthesis of 4-Carboxy-Pennsylvania Green Methyl Ester: A Hydrophobic Building Block for Fluorescent Molecular Probes. Synthesis (Stuttg). 2014 Jan 01;46(2):158–64.