CAS: 76547-98-3; (S)-1-((S)-6-Amino-2-(((S)-1-Carboxy-3-Phenylpropyl)Amino)Hexanoyl)Pyrrolidine-2-Carboxylic Acid

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CAS号77726-95-5 N2-[(1S)-1-Carb... | CAS号16652-71-4 L-脯氨酸苄酯盐酸盐 | CAS号85955-58-4 (2S)-1-[(2S)-6-... | CAS号103300-91-0 N2-[1-(S)-乙氧羰基-... | CAS号32489-85-3 L-Lys(B°C)-L-Pr... | CAS号19522-26-0 3-benzoyl-2-pro... | CAS号17812-07-6 trans-3-苯甲酰丙烯酸 | CAS号104-53-0 3-苯丙醛 | CAS号120379-81-9 5-phenylethyl-i...

N2-[1-(S)-乙氧羰基-3-苯丙基]-N6-三氟乙酰基-L-赖氨酸-L-脯氨酸置于水,Sodium Hydroxide体系中,用92%的收率获得产物赖诺普利
参考文献:一种高纯度赖诺普利的制备工艺
标题:一种高纯度赖诺普利的制备工艺
摘要:本发明提供了一种高纯度赖诺普利的合成方法,采用l‑脯氨酸弱碱性复合铵盐来代替现有技术中的l‑脯氨酸强碱复合盐(如四甲基氢氧化铵,氢氧化钠),与赖诺普利氢化物(II)在dcc和n‑羟基琥珀酰亚胺(Nhs)存在下缩合,后水解得到赖诺普利.该制备方法从源头上控制了特定杂质n6‑(3‑羧基丙酰基)赖诺普利(I)的反应生成,使得得到的赖诺普利及其二水合物符合药品标准,适用于工业化大生产.

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-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-6166217-A
优先权日:1998-02-09
标题 :Process for the production of alkoxycarbonyldipeptides intermediates in the synthesis of the lisinopril
发明人：CANNATA VINCENZO; MERLI VALERIANO; SAGUATTI STEFANO
权利人:ALLIED SIGNAL INC
摘要:Process for the production of alkoxycarbonyldipeptides intermediates in the synthesis of the lisinopril which comprises protecting both amino functions of the L-lysine with an alkoxycarbonyl group, subsequently making the N-carboxyanhydride of the N6-[alkoxycarbonyl]-L-lysine by treatment with thionyl chloride and making the desired alkoxycarbonyldipeptide by reaction with L-proline in alkaline medium.

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)

专利号:US-8431712-B2
优先权日:2004-02-09
标 题 :Methods for the synthesis of pyridoxamine
发明人：KHALIFAH RAJA G; KEILITZ ROLAND; KOELLNER CHRISTOPH; DEGENHARDT THORSTEN; BRAND STEPHEN ROBERT
权利人:KHALIFAH RAJA G; KEILITZ ROLAND; KOELLNER CHRISTOPH; DEGENHARDT THORSTEN; BRAND STEPHEN ROBERT; NEPHROGENEX INC
摘要:The invention provides non-oxidative methods for the large scale manufacture of pyridoxamine (I) (4-aminomethyl-3-hydroxy-5-hydroxymethyl-2-methylpyridine): n nand salts thereof.n nThe invention also provides intermediate compounds for the synthesis of pyridoxamine, as well as compositions and methods for the treatment and/or prevention of conditions associated with the formation of post-Amadori advanced glycation end-products.