专利号:US-8350031-B2 优先权日:2008-06-02 标 题:Processes for the synthesis of levocetirizine and intermediates for use therein 发明人:RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 权利人:CIPLA LTD; RAO DHARMARAJ RAMACHANDRA; KANKAN RAJENDRA NARAYANRAO; GHAGARE MARUTI; CHIKHALIKAR SANDIP VASANT 摘要:The present invention provides a compound of formula (IV) n nwherein R is Cl, Br, NO 2 , OH or OR′, and R′ is alkyl, and its use in the synthesis of levocetirizine, including its use in the synthesis of (−)-1-[(4-chlorophenyl)-phenylmethyl]piperazine, an intermediate useful in the synthesis of levocetirizine. The present invention also provides compounds (II) and (III) which are useful in the synthesis of compound (IV).
专利号:WO-2013121018-A1 优先权日:2012-02-17 标题 :Synthesis of cyanocarboxylic acid alkyl esters 发明人:FRANZKE CONSTANZE; OTT LOTHAR; GRUETZNER THOMAS; LITZMANN OLIVER; REPKE JENS-UWE; HAMMANN MARKUS; LORENZ HILKE-MARIE; MEEMKEN FABIAN CARL INGOLD 权利人:LONZA AG 摘要:Provided is a process for obtaining a compound of formula (I): N≡C-CH 2 -A-C(O)-OR, wherein Hal is halogen selected from F, Cl, Br or I, A denotes a bond or a divalent spacer selected from alkylene and arylene groups, and R is a C 1-4 alkyl group, by reacting a compound of formula (II): Hal-CH 2 -A-C(O)-OR, wherein Hal is a halogen atom selected from F, Cl, Br and I, and wherein A and R are as defined above, with hydrogen cyanide in the presence of a first base, wherein the molar ratio between hydrogen cyanide and said first base is from 1:0.3 to 1:0.95 and the molar ratio between hydrogen cyanide to the compound of formula (II) is at least 1:1.
专利号:US-11298390-B2 优先权日:2017-09-18 标题:Total flavonoids extract of Gynura formosana Kitam., preparation method therefor and use thereof for treating hyperuricemia 发明人:YUAN HUIJUN; YIN TINGTING; HONG FEI; YU JUAN; ZENG JINXIANG; WANG SHICONG 权利人:ZHANGZHOU PIEN TZE HUANG PHARM 摘要:Disclosed is a total flavonoids extract of Gynura formosana Kitam., containing 80%-85% of rutin by weight percent content. The results of pharmacological experiments show that the extract can lower the activity of xanthine oxidase in the liver of a hyperuricemia model mouse and reduce the synthesis of uric acid to a certain degree and has a certain uric acid-lowering effect, and can be used as a potential drug for treating hyperuricemia or gout. The method for preparing the total flavonoids extract of Gynura formosana Kitam. comprises: after an extraction step, selecting a complex enzyme composed of enzymes with a specific composition and a specific ratio for enzymolosis, and further carrying out the step of extracting and concentrating with macroporous resin and isolating and purifying with macroporous resin, so that the HPLC purity of rutin in the resulting total flavonoids extract of Gynura formosana Kitam. reaches 80%-85%.
专利号:US-9296709-B2 优先权日:2012-07-03 标 题 :Manufacture of 2-(5-bromo-4-(4-cyclopropylnaphthalen-1-yl)-4H-1,2,4-triazol-3-ylthio)acetic acid 发明人:GUNIC ESMIR; GALVIN GABRIEL 权利人:ARDEA BIOSCIENCES INC 摘要:Described herein are certain processes for the synthesis of compounds of Formula (I):
专利号:WO-2009057133-A2 优先权日:2007-07-24 标题 :A process for the synthesis of 2-[2-[4-[(4-chlorophenyl)phenyl methyl]-1-piperazinyl] ethoxy acetic acid
专利号:US-2011184174-A1 优先权日:2008-06-02 标题 :Processes for the Synthesis of Levocetirizine and Intermediates for Use Therein
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