专利号:US-2008032964-A1 优先权日:2006-04-10 标题:Process for the synthesis of azetidinone 发明人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 权利人:KANSAL VINOD K; AHMAD SUHAIL; MARIAPPAN SHANMUGAVEL; TYAGI BHUPENDRA; PERLMAN NURIT; LE PAIH JACQUES; ZANOTTI-GEROSA ANTONIO 摘要:Provided are intermediates useful for the synthesis of hydroxyl-alkyl substituted azetidinones, processes of their preparation, and processes for the synthesis of certain hydroxyl-alkyl substituted azetidinones. Also provided are processes for the synthesis of 1-(4-fluorophenyl)-3(R)-[3-(4-fluorophenyl)-3(S)-hydroxypropyl]-4(S)-(4-hydroxyphenyl)-2-azetidinone, or ezetimibe.
专利号:US-5679864-A 优先权日:1995-11-03 标题:Process for the synthesis of curcumin-related compounds 发明人:KRACKOV MARK HARRY; BELLIS HAROLD EDWARD 权利人:GENE PRINT INC 摘要:The invention is directed to a process for the synthesis of curcumin and curcumin-related compounds by reacting the enol form of a 2,4-diketone with a monocarbocyclic aldehyde in the presence of an organic amine catalyst. The reactants are dissolved in a highly polar, aprotic organic solvent. The curcumin-related product is recovered in crystalline form by precipitation from the reaction mass and solvent recrystallization.
专利号:US-8212071-B2 优先权日:2005-09-19 标题:Asymmetric synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid 发明人:KANSAL VINOD KUMAR; CHAURASIA BRIJNATH P; RAO V GOVARDHAN; TIWARI ANAND PRAKASH 权利人:KANSAL VINOD KUMAR; CHAURASIA BRIJNATH P; RAO V GOVARDHAN; TIWARI ANAND PRAKASH; TEVA PHARMA 摘要:The invention encompasses processes for the synthesis of (S)-(+)-3-(aminomethyl)-5-methylhexanoic acid, (S)-Pregabalin, and intermediates of (S)-Pregabalin.
专利号:US-11717498-B2 优先权日:2013-12-31 标题 :Methods of treatment using amphetamine controlled release, prodrug, and abuse deterrent dosage forms 发明人:POPP KARL; MECKLER HAROLD 权利人:Chemapotheca LLC; PHARMAPOTHECA A INC 摘要:The invention also relates to pharmaceutical compositions comprising highly pure amphetamine and amphetamine-class compounds resulting from the synthesis of chiral and racemic amphetamine derivatives by stereospecific, regioselective cuprate addition reaction with aziridine phosphoramidate compounds, and to methods of manufacturing, delivering, and using the amphetamine compounds resulting from the synthesis of chiral and racemic amphetamine derivatives by stereospecific, regioselective cuprate addition reaction with aziridine phosphoramidate compounds.
专利号:US-2008015197-A1 优先权日:2006-06-26 标题 :Process for the preparatrion of zopiclone 发明人:MAINFELD ALEX; MENDELOVICI MARIOARA 权利人:MAINFELD ALEX; MENDELOVICI MARIOARA 摘要:Provided is a process for the preparation of zopiclone, an intermediate in the synthesis of eszopiclone.
专利号:US-2010010212-A1 优先权日:2005-09-08 标题 :Processes for the preparation of (3R,4S)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-((S)-3-(4-fluorophenyl)-3-hydroxypropyl)-2-azetidinone, an intermediate for the synthesis of ezetimibe 发明人:KANSAL VINOD KUMAR; AHMAD SUHAIL; TYAGI BHUPENDRA; GUPTA NITIN 权利人:KANSAL VINOD KUMAR; AHMAD SUHAIL; TYAGI BHUPENDRA; GUPTA NITIN 摘要:The invention encompasses (3R,4S)-4-((4-benzyloxy)phenyl)-1-(4-fluorophenyl)-3-(3-(4-fluorophenyl)-3-oxopropyl)-2-azetidinone (Compound 2a) having an enantiomeric purity of at least about 97.5%. The invention also encompasses Compound 2a having a chemical purity of at least about 97%. The invention further encompasses processes for preparing Compound 2a from Compound 1 having the following formula: n n n n n n n n n n The invention also encompasses processes for preparing a compound having the following formula: n n n n n n n n n n from a compound having the following formula: n n n n n n n n n n wherein R is selected from the group consisting of: H or a hydroxyl protecting group. The invention also encompasses processes for preparing Compound 2a, preferably to form Compound 2a-Form 01. Also included are processes for preparing ezetimibe from Compound 2a-Form 01 or Compound 2a prepared according to the invention, compositions containing such ezetimibe, and methods for reducing cholesterol using such compositions
[参考文献]: Gke Polat Yemi, Et Al. Thermal Tolerance And Survival Of Cronobacter Sakazakii In Powdered Infant Formula Supplemented With Vanillin, Ethyl Vanillin, And Vanillic Acid. J Food Sci. 2012 Sep;77(9):M523-7. [参考文献]: Hyun-Joo Jung, Et Al. Assessment Of The Anti-Angiogenic, Anti-Inflammatory And Antinociceptive Properties Of Ethyl Vanillin. Arch Pharm Res. 2010 Feb;33(2):309-16. [参考文献]: Jean-Pierre Rospars, Et Al. Competitive And Noncompetitive Odorant Interactions In The Early Neural Coding Of Odorant Mixtures. J Neurosci. 2008 Mar 5;28(10):2659-66. [参考文献]: Jih-Jung Chen, Et Al. Dihydroagarofuranoid Sesquiterpenes, A Lignan Derivative, A Benzenoid, And Antitubercular Constituents From The Stem Of Microtropis Japonica. J Nat Prod. 2008 Jun;71(6):1016-21. [参考文献]: Laila Ali, Et Al. Rapid Method For The Determination Of Coumarin, Vanillin, And Ethyl Vanillin In Vanilla Extract By Reversed-Phase Liquid Chromatography With Ultraviolet Detection. J Aoac Int. 2008 Mar-Apr;91(2):383-6.
合成参考文献
摘要:National Technical Information Service., OTS0534355 摘要:NITE; Chemical Risk Information Platform (CHRIP). Biodegradation and Bioconcentration. Tokyo, Japan: Natl Inst Tech Eval. Available from, as of June 11, 2015: 摘要:21 CFR 582.60 (USFDA); U.S. National Archives and Records Administration's Electronic Code of Federal Regulations. Available from, as of April 20, 2015: 摘要:Lyman WJ et al; Handbook of Chemical Property Estimation Methods. Washington, DC: Amer Chem Soc pp. 7-4, 7-5, 8-12 (1990) 摘要:40 CFR 716.120 (USEPA); U.S. National Archives and Records Administration's Electronic Code of Federal Regulations. Available from, as of April 20, 2015: https://www.ecfr.gov