CAS: 79815-20-6; (S)-Indoline-2-Carboxylic Acid

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2-溴溴苄置于palladium On Activated Charcoal,Cinchonidinium Bromide Derived Chiral 盐酸,Cesium Hydroxide,偶氮二异丁腈,氢气,三正丁基氢锡体系中,用 四氢呋喃,甲醇,苯 作为反应溶剂,85.0 °C,689.49 Kpa 条件下,反应 76.0H,反应生成 (S)-吲哚啉-2-羧酸
参考文献:自由基介导的芳基胺化及其在对映选择性二氢吲哚 α-氨基酸合成的收敛 [3 + 2] 策略中的应用
标题:自由基介导的芳基胺化及其在对映选择性二氢吲哚 α-氨基酸合成的收敛 [3 + 2] 策略中的应用
摘要:描述了偶氮甲碱氮上芳基加成的范围.芳基,三氟甲基烷基和 α,β-不饱和酮亚胺通过芳基自由基与偶氮甲亚胺氮的 5-外环化参与区域选择性芳基-氮键形成.碳-氮相对于碳-碳键形成的选择性通常很高 (>95:5),并且仅与锡烷 (0-10%) 的直接芳基自由基还原竞争.α-酮亚胺是一类很有前途的新型碳自由基受体,没有观测到竞争性芳基自由基还原.反应条件为 Ph 中性,因此是可用于芳环胺化的最温和的方法之一.检测的酮亚胺没有受到锡烷竞争性还原的影响,与使用重氮和叠氮官能团作为碳自由基的氮源相比具有优势.自由基介导的芳基胺化反应采用 O'Donnell 相转移催化的甘氨酰亚胺对映选择性烷基化策略进行测序,以提供具有高 Ee 的二氢吲哚α-氨基酸的任一对映体.这些新的受限苯丙氨酸衍生物现在可以很容易地用于各种应用的评估.
DOI:10.1021/ja0284308

专利信息

专利号:US-7323575-B2
优先权日:2003-04-09
标题:Process for the synthesis of (2S)-indoline-2-carboxylic acid
发明人：SOUVIE JEAN-CLAUDE; LECOUVE JEAN-PIERRE
权利人:SERVIER LAB
摘要:Process for the synthesis of (2S)-indoline-2-carboxylic acid of formula (I): n nApplication in the synthesis of perindopril and its pharmaceutically acceptable salts.

专利号:US-12240808-B2
优先权日:2021-05-28
标 题 :Process for the synthesis of calebin-a and its intermediates
发明人：MAJEED MUHAMMED; NAGABHUSHANAM KALYANAM; MUTHUKAMAN NAGARAJAN; NAIDU PENTAKOTA PARADESI
权利人:MAJEED MUHAMMED; NAGABHUSHANAM KALYANAM; MUTHUKAMAN NAGARAJAN; NAIDU PENTAKOTA PARADESI
摘要:The invention discloses novel intermediates in the synthesis of Calebin A represented by formula 3. The invention also covers processes for the synthesis of Calebin-A and its analogs using compounds of formula 3.

专利号:US-7060842-B2
优先权日:2001-07-24
标题 :Method for synthesis of (2S, 3aS, 7aS)-1-{(S)-alanyl}-octahydro-1H -indole-2-carboxylic acid derivatives and use for synthesis of perindopril
发明人：MEZEI TIBOR; PORCS-MAKKAY MARTA; SIMIG GYULA
权利人:SERVIER LAB
摘要:Process for the industrial synthesis of the compounds of formula (I): n nwherein R 1 represents a hydrogen atom or an alkyl or benzyl group, and R 2 represents a group that protects the amino function.

专利号:US-4914214-A
优先权日:1987-09-17
标 题:Process for the industrial synthesis of perindopril
发明人：VINCENT MICHEL; BALIARDA JEAN; MARCHAND BERNARD; REMOND GEORGES
权利人:ADIR
摘要:Process for the industrial synthesis of perindopril, in which (2S,3aS,7aS)-2-carboxyperhydroindole is condensed with N-[(S)-1-carbethoxybutyl]-(S)-alanine after protection of the carboxyl group, the product resulting from the condensation being then subjected to deprotection of the carboxyl carried by the heterocyclic ring. n The (2S,3aS,7aS)-2-carboxyperhydroindole and N-[(S)-1-carbethoxybutyl]-(S)-alanine are themselves obtained in excellent conditions from 2-carboxyindole and from L-alanine respectively, both available on an industrial scale.

专利号:US-7157484-B2
优先权日:2003-02-28
标 题 :Method for synthesissing (2s, 3as, 7as)-perhydroindole-2-carboxylic acid and the esters thereof and the use thereof for perindopril synthesis
发明人：DUBUFFET THIERRY; LANGLOIS PASCAL
权利人:SERVIER LAB
摘要:Process for the synthesis of compounds of formula (I): n nwherein R represents hydrogen or a protecting group.n n Application in the synthesis of perindopril and pharmaceutically acceptable salts thereof.

专利号:WO-2024224414-A1
优先权日:2023-04-25
标题:Process for preparation of (2s, 3as,7as)-octahydro-1h-indole-2-carboxylic acid
发明人：DESAI PARIMAL HASMUKHLAL; SALVI NARENDRA JAGANNATH; PATRAVALE BHARATKUMAR SURENDRA; KULKARNI MAHESH RAMRAO
权利人:AARTI PHARMALABS LTD
摘要:The present invention relates to a process for preparation of compound of formula (A). The process for stereo-specific synthesis of (2S,3aS,7aS)-Octahydro-1H-indole-2-carboxylic acid of formula (A) includes hydrogenation of compound of formula (I) in the aqueous medium in presence of a metal catalyst and an alkali to form compound of formula (A). Further, the present invention also includes the process of synthesis of compound of formula (I) by resolving indoline-2-carboxylic acid of formula (II). The process of the present invention provides higher chiral purity and higher yield of compound of formula (A) without substantial amounts of undesired by-products. The process of the present invention is cost effective due to recyclability and reuse of catalyst and resolving agent (R)-(+)-α-methylbenzylamine with higher efficiency.