CAS: 87679-37-6; (2S,3Ar,7As)-1-[(2S)-2-[[(2S)-1-Ethoxy-1-Oxo-4-Phenylbutan-2-Yl]Amino]Propanoyl]-2,3,3A,4,5,6,7,7A-Octahydroindole-2-Carboxylic Acid

上下游产品

CAS号82717-90-6 八氢吲哚-2-羧酸苄酯 | CAS号82717-96-2 N-[1-(S)-乙氧羰基-3... | CAS号98677-37-3 替诺拉普利苄基酯 | CAS号145641-35-6 (2S,3aR,7aS)-八氢... | CAS号114192-42-6 N-[(S)-1-carbet... | CAS号82717-97-3 °Ctahydroindole... | CAS号84793-24-8 N-[1-(S)-乙氧羰基-3... | CAS号145438-94-4 L-(2S,3aR,7aS)-... | CAS号881637-74-7 (2S,3aR,7aS)-pe... | CAS号80828-13-3 八氢-1H-吲哚-2-羧酸 | CAS号82717-96-2 N-[1-(S)-乙氧羰基-3...

Tert-Butyl (2S,3Ar,7As)-1-(((S)-1-Ethoxy-1-Oxo-4-Phenylbutan-2-yl)-L-Alanyl)octahydro-1H-Indole-2-Carboxylate置于三氟乙酸体系中,用 二氯甲烷 作为反应溶剂,化学反应 0.5H,以97%的收率获得产物群多普利
参考文献:Ace抑制剂群多普利的立体选择性合成
标题:Ace抑制剂群多普利的立体选择性合成
摘要:实现了对映纯八氢吲哚结构单元的概念新颖和立体选择性合成,并将其转化为 Ace 抑制剂群多普利.关键步骤包括受保护的 L-焦谷氨酸衍生物的 α-烯丙基化,高度非对映选择性的 Hosomi-Sakurai 反应和 Ru 催化的 4,5-二烯丙基化脯氨酸的闭环复分解.这样,群多普利的合成以 25% 的总产率(12 步)有效实现.
DOI:10.1055/s-0037-1612306

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-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-7973173-B2
优先权日:2005-07-05
标 题:Process for the synthesis of an ACE inhibitor
发明人：KANKAN RAJENDRA NARAYANRAO; RAO DHARMARAJ RAMACHANDRA; PHULL MANJINDER SINGH; SAWANT ASHWINI; BIRARI DILIP RAMDAS
权利人:CIPLA LTD
摘要:A process for the synthesis of trandolapril which comprises condensing N—[I—(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine N-carboxyanhydride with trans octahydro-1H-indole-2-carboxylic acid in a first organic solvent comprising a water immiscible inert organic solvent and in the presence of a base, and isolating trandolapril from a second organic solvent. N-[1-(S)-ethoxycarbonyl-3-phenylpropyl]-L-alanine N-carboxyanhydride may also be condensed with (2S,3aR,7aS) octahydro-1H-indole-2-carboxylic acid in a first organic solvent and in the presence of a base, and trandolapril isolated. There is also provided a process for the resolution of racemic trans octahydro-1H-indole-2-carboxylc acid.

专利号:EP-1724260-B1
优先权日:2005-05-06
标题:Process for the synthesis of (2S, 3aR, 7aS)octahydroindole-2-carboxylic acid and its conversion to trandolapril
发明人：AKHTAR HAIDER; RAMESH BABU POTLURI; VENKATA SUBHRAMANIAN HARIHARAK; HARI PRASSAD KODALI
权利人:SOCHINAZ SA
摘要:The present invention describes a novel method for the synthesis of (2S,3aR,7aS)-octahydroindole-2-carboxylic acid of formula III nusing a new intermediate of formula II nand conversion of the product of formula-III to trandolapril of formula I

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.