CAS: 77521-29-0; 2-Amino-3-(5-Methyl-3-Oxo-2,3-Dihydroisoxazol-4-yl)Propanoic Acid

📜4-(Bromomethyl)-2-(Methoxymethyl)-5-Methylisoxazol-3(2H)-One置于氢溴酸,Sodium Hydride体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 12.0H,反应生成 (R,S)-α-氨基-3-羟基-5-甲基-4-异恶唑丙酸
参考文献:Equilibrium Control In Bromomethylation: An Expedient Route To 2-Amino-3-(3-Hydroxy-5-Methylisoxazol-4-yl)Propionic Acid (Ampa)
标题:Equilibrium Control In Bromomethylation: An Expedient Route To 2-Amino-3-(3-Hydroxy-5-Methylisoxazol-4-yl)Propionic Acid (Ampa)
摘要:通过三步法从 3-羟基-5-甲基异恶唑制备出了 2-氨基-3-(3-羟基-5-甲基异恶唑-4-基)丙酸(ampa),总产率为 42%.该研究显示了如何通过控制相关的平衡来优化溴甲基化反应,以及如何去除 N-保护甲氧基甲基.
DOI:10.1055/s-1993-25956

专利信息

专利号:US-5338851-A
优先权日:1993-03-31
标 题:Synthesis of cis-decahydroisoquinoline-3-carboxylic acids
发明人：HUFF BRET E; KHAU VIEN V; MARTINELLI MICHAEL J; PETERSON BARRY C
权利人:LILLY CO ELI
摘要:This invention provides a process for the synthesis of cis-decahydroisoquinoline-3-carboxylic acids and provides intermediates in the synthesis thereof.

专利号:US-5591867-A
优先权日:1992-12-04
标 题 :Synthesis of kainic acid
发明人：MONN JAMES A
权利人:LILLY CO ELI
摘要:This invention provides a process for preparing kainic acid and provides intermediates in the synthesis thereof.

专利号:US-6160133-A
优先权日:1994-08-31
标题:Synthesis of (S)-α-methyl-1,3-benzodioxole-5-ethanol and derivatives
发明人：VARIE DAVID L; VICENZI JEFFREY T; ZMIJEWSKI MILTON J
权利人:LILLY CO ELI
摘要:A process for stereoselectively forming N-substituted dihydro-2,3 benzodiazepines which are useful as AMPA receptor antagonists. The process includes an opening reduction step which sets the stereochemistry of the intermediates and the final compounds to the desired enantiomer. The reduction step may be carried out by an enzymatic reduction.

专利号:US-2004110228-A1
优先权日:2002-04-01
标 题:Combinatorial organic synthesis of unique biologically active compounds
发明人：MCALPINE SHELLI R; TAYLOR RACHEL E; BOLLA MEGAN L; SEGALL ANCA M
摘要:The invention provides a method for making a combinatorial library of cyclic compounds, such as Holliday junction-trapping compounds, comprising the steps of (a) obtaining a plurality of trimers according to the generic structure X 1- X 2- X 3 , wherein X 1 , X 2 and X 3 can be independently any naturally or nonnaturally occurring amino acids or peptidomimetics thereof; (b) optionally coupling a spacer S to the trimer at either end; (c) cyclizing two trimers or trimer-spacer conjugates in a head-to-tail orientation; thereby obtaining a combinatorial library of compounds, wherein the library does not include an unmodifed or naturally occurring Holliday Junction-trapping compounds. The invention additionally provides methods macrocyclic compounds that are synergimycin derivatives.

专利号:US-10111867-B2
优先权日:2015-02-17
标题:Process and intermediates for the preparation of perampanel
发明人：MAROM EHUD; RUBNOV SHAI
权利人:MAPI PHARMA LTD
摘要:The present invention describes a process for the synthesis of 3-(2-cyanophenyl)-5-(2-pyridyl)-1-phenyl-1,2-di-hydro-pyridin-2-one (Perampanel) represented by the structure of formula (1), and salts thereof, especially salts with pharmaceutically acceptable acids. The present invention further relates to certain intermediates formed and/or used in such process.

专利号:US-5470979-A
优先权日:1994-07-01
标 题:Asymmetric synthesis of bicyclic amino acid esters
发明人：TROVA MICHAEL P
权利人:AMERICAN CYANAMID CO
摘要:The invention is an improved process for producing an optically active compound of formula IV: ##STR1## wherein R 1 , R 2 and R 4 are herein described. The improved process to produce a compound of formula IV comprises: n a). reacting a diene with a chiral compound, containing a chiral auxiliary to obtain an olefinic compound; n b). removing the chiral auxiliary and reducing the olefin by hydrogenation to obtain a compound of formula IV.