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-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
专利号:US-8735391-B2 优先权日:2008-09-26 标 题 :Synthesis of functionalized octahydro-isoquinolin-1-one-8-carboxamides, octahydro-isoquinolin-1-one-8-carboxylic esters and analogs, and therapeutic methods 发明人:AUBE JEFFREY; ROTH BRYAN L; GHOSH PARTHA; FRANKOWSKI KEVIN J 权利人:AUBE JEFFREY; ROTH BRYAN L; GHOSH PARTHA; FRANKOWSKI KEVIN J; UNIV KANSAS 摘要:A functionalized polycyclic compound can have a structure of Formula 1 or salt, prodrug, analog, or derivative thereof, which compound can be prepared by providing a diene; reacting the diene with a dienophile under sufficient conditions for a combined Diels-Alder/acylation reaction so as to provide a polycyclic compound having a carboxylic acid; and coupling the carboxylic acid with an amine-containing compound or a hydroxyl-containing compound so as to form an amide or an ester and producing a compound having a structure of Formula 1. The compound can be used for modulating an opioid receptor, which can be conducted by administering to an opioid receptor a functionalized polycyclic compound as described herein in an effective amount to modulate the functionality of the opioid receptor. Such opioid modulation can provide a biological benefit to a subject.
1: Sun Y, Bressler J. Ethyl maltol disrupt iron homeostasis in SH-SY5Y neuroblastoma cell line. J Biochem Mol Toxicol. 2023 Dec;37(12):e23504. doi: 10.1002/jbt.23504. Epub 2023 Aug 22. 410:115354. doi: 10.1016/j.taap.2020.115354. Epub 2020 Nov 30. 31(Suppl 3):s238-s244. doi: 10.1136/tc-2022-057484. 4: Xing P, Che Z, Liu Y, He J, Wei R, Chen L, Zhang S, Huang X, Yang Y, Liu S, Chen G, Tian Y. Synthesis and Anti-Oomycete Preliminary Mechanism of Sulfonate Derivatives of Ethyl Maltol. Chem Biodivers. 2022 Jun;19(6):e202200255. doi: 10.1002/cbdv.202200255. Epub 2022 May 27.
合成参考文献
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