CAS: 60929-23-9; Indeloxazine

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CAS号60929-60-4 4-morpholin-2-y... | CAS号104908-23-8 6-(((1H-inden-7... | CAS号81542-44-1 1-((1H-inden-7-...

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    📜1-Amino-3-(3H-Inden-4-Yloxy)Propan-2-Ol置于lithium Aluminium Tetrahydride,Sodium Methylate,三乙胺体系中,用 四氢呋喃,甲醇,二氯甲烷 作为反应溶剂,化学反应生成 茚洛秦
    参考文献:Syntheses Of (.+-.)-2-((Inden-7-Yloxy)Methyl)Morpholine Hydrochloride (Ym-08054,Indeloxazine Hydrochloride) And Its Derivatives With Potential Cerebral-Activating And Antidepressive Properties.
    标题:Syntheses Of (.+-.)-2-((Inden-7-Yloxy)Methyl)Morpholine Hydrochloride (Ym-08054,Indeloxazine Hydrochloride) And Its Derivatives With Potential Cerebral-Activating And Antidepressive Properties.
    摘要:研究了(+/-)-2-[(茚-7-基氧基)甲基]吗啉盐酸盐(7.hcl,Ym-08054,盐酸吲哚嗪)的合成及其光学拆分为左旋和右旋异构体.采用优先结晶法从7.hcl及其互变异构体(+/-)-2-[(茚-4-基氧基)-甲基]吗啉盐酸盐(6.hcl)的平衡混合物中优先结晶,建立了7.hcl的实用合成方法.,在催化量的碱的存在下,在meoh中.研究发现,7.hcl 及其左旋异构体 ((-)-7.hcl) 不仅具有很强的抗抑郁活性,而且具有强大的脑激活特性.还简要讨论了相关化合物的合成和药理活性.
    DOI:10.1248/cpb.33.3766

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    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-7576211-B2
    优先权日:2004-09-30
    标题 :Synthesis of thienopyridinone compounds and related intermediates
    发明人:DHANOA DALE S; BECKER OREN; NOIMAN SILVIA; CHEN DONGLI; MARANTZ YAEL; SHACHAM SHARON; HEIFETZ ALEXANDER; INBAL BOAZ; BAR-HAIM SHAY; MOHANTY PRADYUMNA; LOBERA MERCEDES; WU LAURENCE
    权利人:EPIX DELAWARE INC
    摘要:The invention relates to 5-HT receptor agonists and partial agonists. Novel thienopyridinone compounds represented by Formula I, and synthesis and uses thereof for treating diseases mediated directly or indirectly by 5-HT receptors, are disclosed. Such conditions include Alzheimer's disease, cognition disorders, irritable bowel syndrome, nausea, emesis, vomiting, prokinesia, gastroesophageal reflux disease, nonulcer dyspepsia, depression, anxiety, urinary incontinence, migraine, arrhythmia, atrial fibrillation, ischemic stroke, gastritis, gastric emptying disorders, feeding disorders, gastrointestinal disorders, constipation, erectile dysfunction, and respiratory depression. Methods of preparation and novel intermediates and pharmaceutical salts thereof are also included.

    专利号:US-2004152897-A1
    优先权日:2002-09-13
    标 题 :Synthesis of indolizines
    发明人:SUN LIJUN; KOYA KEIZO; XIA ZHI-QIANG; PRZEWLOKA TERESA; ZHANG SHIJIE; ONO MITSUNORI
    权利人:SYNTA PHARMACEUTICALS CORP
    摘要:Disclosed are methods of preparing substituted indolizines represented by the following formula: n n n comprising reacting a substrate represented by the following formula: n n n with either the cyclization reagent of the following formula: n n n or, a reagent prepared by reacting the compound represented the formula below with an alkylating agent: n n n The variables in the above formulas are defined herein.

    专利号:US-2015158809-A9
    优先权日:2013-02-26
    标 题 :Method of making 1-(acyloxy)-alkyl carbamate compounds
    发明人:WANG HUAN; LIU PENG; DAI QUNYING; YIN HAO; RAILLARD STEPHEN P
    权利人:XENOPORT INC
    摘要:Methods of preparing carbamate prodrugs of amine-containing drugs are provided. Carbonates useful in the synthesis of the carbamate prodrugs are also provided.

    专利号:US-2008214827-A1
    优先权日:2004-02-03
    标 题:Synthesis of Cyanoimino-Benzoimidazoles
    发明人:GOEHRING R RICHARD; WHITEHEAD JOHN; SHAO BIN
    权利人:EURO CELTIQUE SA
    摘要:Disclosed in certain embodiments is a process for synthesizing a compound of formula (V) and salts thereof.

    专利号:US-6696438-B2
    优先权日:1998-06-22
    标题:Cyclic amino acid compounds, pharmaceutical compositions comprising same, and methods for inhibiting β-amyloid peptide release and/or its synthesis by use of such compounds
    发明人:AUDIA JAMES E; DRESSMAN BRUCE A; SHI QING
    权利人:ELAN PHARM INC; LILLY CO ELI
    摘要:Disclosed are compounds which inhibit β-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits β-amyloid peptide release and/or its synthesis as well as methods for treating Alzheimer's disease both prophylactically and therapeutically with such pharmaceutical compositions.

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    主要参考文献

    1. Shimizu-Sasamata M, Yamamoto M, Harada M. Cerebral activating properties of indeloxazine HCl and its optical isomers. Pharmacol Biochem Behav. 1993 Jun;45(2):335-41. doi: 10.1016/0091-3057(93)90248-r. 28(12):1291-7. doi: 10.1016/0028-3908(89)90001-4.

    合成参考文献


    参考文献:10.1254/fpj.99.123
    摘要:Hokonohara T, Shinoda Y, Hori N. [Effects of oxiracetam on the decrease in population spikes in hypoxic and low glucose media]. Nihon Yakurigaku Zasshi. 1992 Mar;99(3):123–33. doi: 10.1254/fpj.99.123.
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