CAS: 75847-73-3; Enalapril

上下游产品

2-oxo-4-phenylbutanoic acid ethyl ester L-alanyl-L-proline -L-alanyl-L-proline BenzylesterN-(1S)-1-(Ethoxycarbonyl)-3-phenylpropyl-L-alanyl-L-proline Benzylester -L-alanyl>-L-proline tert butyl esterN--L-alanyl-L-proline tert butyl esterenalaprilate Amprace (S)-2-((3S,8aS)-3-Methyl-1,4-dioxo-hexahydro-pyrrolo[1,2-a]pyrazin-2-yl)-4-phenyl-butyric acid ethyl ester enalaprilic acid

N-<(1S)-1-(Ethoxycarbonyl)-3-Phenylpropyl>-L-Alanyl-L-Proline Benzylester置于palladium On Activated Charcoal 氢气体系中,用 乙醇 作为反应溶剂,化学反应 2.0H,反应生成 依那普利
参考文献:Studies On Angiotensin Converting Enzyme Inhibitors. V. The Diastereoselective Synthesis Of 2-Oxoimidazolidine Derivatives.
标题:Studies On Angiotensin Converting Enzyme Inhibitors. V. The Diastereoselective Synthesis Of 2-Oxoimidazolidine Derivatives.
摘要:建立了一种具有二面体选择性的imidapril(1)合成方法,该药物正在进行临床研究,作为一种基于其血管紧张素转化酶(ace)抑制活性的抗高血压药物.将(2S)-2-Amino-4-Phenylbutyric Acid Ester(12)与3-((2R)-2-甲基或甲苯磺酰氧丙酰)-2-氧代咪唑烷衍生物(11)通过sn2方式进行n-烷基化,选择性地反应生成叔丁基(4S)-3-[(2S)-2-[n-[(1S)-1-乙氧基碳酰基)-3-苯基丙基]氨基]丙酰]-1-甲基-2-氧代咪唑烷-4-羧酸酯(13),该化合物是1的前体.作为替代,合成了苄基(2S)-2-[n-(1S)-1-(乙氧基碳酰基)-3-苯基丙基]氨基]丙酸酯(15),这是13的关键构件.该程序也应用于enalapril的合成.
DOI:10.1248/cpb.39.1374

专利信息

专利号:US-9353057-B2
优先权日:2003-12-30
标 题:Synthesis of acyloxyalkyl carbamate prodrugs and intermediates thereof
发明人：GALLOP MARK A; DAI XUEDONG; SCHEUERMAN RANDALL A; RAILLARD STEPHEN P; MANTHATI SURESH K; YAO FENMEI; PHAN THU; LUDWIKOW MARIA; PENG GE; BHAT SEEMA
权利人:XENOPORT INC
摘要:Methods for synthesis of 1-(acyloxy)-alkyl carbamates, particularly, the synthesis of 1-(acyloxy)-alkyl carbamate prodrugs of primary or secondary amine-containing drugs are described. Also described are methods for synthesis of 1-(acyloxy)-alkyl N-hydroxysuccinimidyl carbonates which are useful intermediates in the synthesis of 1-(acyloxy)-alkyl carbamates are also described.

专利号:US-7169589-B2
优先权日:2000-07-28
标题 :Silicatein-mediated synthesis of amorphous silicates and siloxanes and use thereof
发明人：MUELLER WERNER E G; SCHROEDER HEINZ C; LORENZ BERND; KRASKO ANATOLI
权利人:MUELLER WERNER E G; SCHROEDER HEINZ C; LORENZ BERND; KRASKO ANATOLI
摘要:Silicatein is an enzyme of silicate-forming organisms used for the synthesis of their silicate scaffold. The present invention relates to the use of highly-expressed and highly active recombinant silicatein, silicatein isolated from natural sources after gene induction as well as silicatein-fusion proteins for the synthesis of amorphous silicon dioxide (silicic acids and silicates), siloxanes as well as modification of these compounds and their technical use.

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人：JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

专利号:US-10005720-B2
优先权日:2013-04-05
标题:Compounds useful for the treatment of metabolic disorders and synthesis of the same
发明人：SEXTON JONATHAN Z; BRENMAN JAY E; MUSSO DAVID L
权利人:NORTH CAROLINA CENTRAL UNIV; UNIV NORTH CAROLINA CHAPEL HILL
摘要:The present invention provides compounds of Formula (I): wherein variables X, Y, Z and R1 are as described herein. Some of the compounds described herein are glutamate dehydrogenase activators. The invention is also directed to pharmaceutical compositions comprising these compounds, uses of these compounds and compositions in the treatment of metabolic disorders as well as synthesis of the compounds.

专利号:US-7094920-B2
优先权日:2001-05-21
标 题 :Stereoselective synthesis of 2-hydroxy-4-phenylbutyric acid esters
发明人：TIKARE RAVEENDRA KHANDURAO
权利人:FERMENTA BIOTECH LTD
摘要:A process is described for the stereospecific preparation of an ester of formula (I): wherein * signifies the (R) stereoisomer; R 1 is selected from C 1-6 alkyl, preferably ethyl; and R 2 is hydrogen, a protecting group or a leaving group which process comprises reaction of a nitrile of formula (II): wherein * signifies the (R) stereoisonomer; and Ph is the phenyl group C 6 H 5 with a solution of an inorganic acid in an alcohol and optional conversion of the compound of formula (I) wherein R 2 is H so prepared to any other desired compound of formula (I) by standard methods in the art. The compounds of formula (I) are chiral esters, useful as intermediates in the synthesis of the family of acetylcholine esterase (ACE) inhibitors known as “prilsâ€?, such as lisinopril, cilazapril, enalapril, benazepril, ramipril, delapril, enalaprilat, imidapril, spirapril, trandolapril and others.n n*n nPh-CH 2 —CH 2 —CH(OR 2 )—COOR 1   (I)n n*n nPh-CH 2 —CH 2 —CH(H)—CN  (II)