CAS: 4093-35-0; 4-Amino-5-Bromo-N-(2-(Diethylamino)Ethyl)-2-Methoxybenzamide

该化合物是一种属于代用苯丙胺的化学化合物,主要因其抗乳性特性而得到承认,有助于治疗恶心和呕吐,特别是正在接受化疗或外科手术的病人.该化合物作为多巴胺受体对立体,有助于调节胃肠功能和减少恶心的情绪.Bromopride通常以口服或注射方式进行,其药理效应归因于其在中...

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CAS号201230-82-2 carbon monoxide | CAS号1285695-16-0 2-bromo-4-iodo-... | CAS号100-36-7 N,N-二乙基乙二胺 | CAS号5344-78-5 4-溴-3-硝基苯甲醚 | CAS号59557-92-5 2-溴-5-甲氧基苯胺 | CAS号96-96-8 冰染重氮组分 1

合成工艺路线路线简述

    4-溴-3-硝基苯甲醚置于盐酸,Tetramethylammonium Dichloroiodate(I),铁粉,三乙胺,三苯基膦,Bis(Dibenzylideneacetone)-Palladium(0)体系中,用 1,4-二氧六环,乙醇,水,乙酸乙酯 作为反应溶剂,化学反应 99.0H,反应生成 溴灭吐灵
    参考文献:化学计量和亚化学计量 12Co 和 13Co 的异位反应生成及其在钯催化氨基羰基化中的有效掺入
    标题:化学计量和亚化学计量 12Co 和 13Co 的异位反应生成及其在钯催化氨基羰基化中的有效掺入
    摘要:使用简单的密封两室系统实现了异位反应生成一氧化碳 (Co) 及其在钯催化的羰基化反应中的有效结合的新技术.co 的异位反应生成是通过钯催化的叔酰氯脱羰使用源自 Pd(Dba)(2) 和 P(Tbu)(3) 的催化剂产生的.使用新戊酰氯作为 Co 前体的初步研究为仅使用 1.5 当量的 Co 对 2-吡啶基甲苯磺酸酯衍生物进行氨基羰基化提供了另一种方法. 酰氯 Co 前体的进一步设计导致开发了一种新的固体,稳定,并且易于处理用于化学转化的 Co 源.这种 Co 前体的合成也为后期安装同位素碳标记的酰氯以随后释放气态 [(13)C]Co 提供了切入点.结合旨在应用 Co 作为限制剂的研究,该方法提供了高效的钯催化氨基羰基化,Co 结合率高达 96%.异位反应生成的 Co 和双室系统在几种药物化合物的合成中进行了测试,所有这些化合物都被标记为 [(13)C] 羰基对应物,基于限制 Co 的产率从非常好到极好.
    DOI:10.1021/ja200818W

    海关参考信息

    专利信息


    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-4381301-A
    优先权日:1980-05-07
    标题 :Substituted tricyclic thieno compounds, their synthesis, their use, their compositions and their medicaments
    发明人:RAINER GEORG
    权利人:BYK GULDEN LOMBERG CHEM FAB
    摘要:Substituted thienobenzodiazepinones of the general formula I (I) [wherein R1 denotes a hydrogen atom (-H) or an alkyl radical with 1 to 4 carbon atoms; R2 represents a halogen atom (halo) or has one of the meanings of R1; R3 denotes a halogen atom (halo) or the group -N(R4)R5; R4 denotes an alkyl radical with 1 to 4 carbon atoms or an alkenyl radical with 3 to 5 carbon atoms; R5 has one of the meanings of R4 or represents the group -(CH2)m-N(R6)R7; or R4 and R5, together with the nitrogen atom to which both are bonded, denote a morpholino group, a pyrrolidino group, a piperidino group, a hexahydroazepin-1-yl group, a piperazin-1-yl group (which is optionally substituted in the 4-position by a methyl, ethyl or benzyl group), a 2,4-dimethylpiperazin-1-yl group, or a hexahydro-1H-1,4-diazepin-1-yl group (which is substituted in the 4-position by a methyl or ethyl group); R6 denotes an alkyl group with 1 to 4 carbon atoms; R7 denotes an alkyl group with 1 to 4 carbon atoms; A denotes a straight-chain or branched alkylene group with 1 to 5 carbon atoms; and m denotes 2 or 3] and their acid-addition salts are new compounds. They either have a protective action on the stomach and intestine and are suitable for treating illnesses based on disorders of the stomach or intestine, or they are intermediates for preparing products having protective action. Processes for the preparation of the new pharmacologically-active compounds and of the intermediate products are presented.

    专利号:EP-3103803-B1
    优先权日:2008-10-27
    标 题 :Intermediates for the synthesis of mtor kinase inhibitors

    专利号:CA-2555219-A1
    优先权日:2004-02-03
    标 题 :Synthesis of cyanoimino-benzoimidazoles

    专利号:US-11759496-B2
    优先权日:2016-05-10
    标题:Compounds and pharmaceutical use thereof in the treatment of cancer
    发明人:SUSIN SANTOS A; KAROYAN PHILIPPE; MERLE-BERAL HÉLÈNE
    权利人:KAROYAN PHILIPPE
    摘要:The present invention relates to a compound or a pharmaceutical salt thereof comprising a hexapeptide sequence of formula (I), its method of synthesis and its use in anticancer therapy. The invention also relates to a pharmaceutical composition for use in the treatment of cancer comprising at least one soluble peptide according to the invention or at least one acid nucleic according to the invention or at least one expression vector according to the invention, or at least one host cell according to the invention and a pharmaceutically acceptable carrier.

    专利号:US-2023271983-A1
    优先权日:2020-07-29
    标题 :Functionalized isonitriles and products, preparation and uses thereof
    发明人:SOTELO PÉREZ EDDY; AZUAJE GUERRERO JHONNY ALBERTO; MAJELLARO MARIA
    权利人:UNIV SANTIAGO COMPOSTELA
    摘要:The present invention relates to functionalized isonitrile compounds, formed by means of multicomponent environmentally friendly reactions, suitable for coupling to functional molecules such as biomolecules, APIs, chromophore and fluorophore molecules. The invention also relates to conjugates between said isonitrile compounds and functional molecules, which are useful in the synthesis of pharmaceutic drugs or tools, fluorescent molecules and labels, polymeric smart materials. The invention furthermore provides a kit for the in-vitro preparation of the functionalized isontrile compounds and conjugates. The invention also contemplates the medical use of said compounds and conjugates.
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    主要参考文献


    1: Huebner EA, Budel S, Jiang Z, Omura T, Ho TS, Barrett L, Merkel JS, Pereira LM, Andrews NA, Wang X, Singh B, Kapur K, Costigan M, Strittmatter SM, Woolf CJ. Diltiazem Promotes Regenerative Axon Growth. Mol Neurobiol. 2018 Sep 19. doi: 10.1007/s12035-018-1349-5. [Epub ahead of print] doi: 10.1016/j.jped.2017.06.004. Epub 2017 Aug 1. Epub 2014 Aug 15.
    4: Lima LS, Los Weinert P, Pezza L, Pezza HR. Sensitive flow-injection spectrophotometric analysis of bromopride. Spectrochim Acta A Mol Biomol Spectrosc. 2014 Dec 10;133:597-604. doi: 10.1016/j.saa.2014.06.027. Epub 2014 Jun 14. Epub 2013 Apr 23. English, Portuguese. doi: 10.1086/651667. Review. Spanish. Italian.

    合成参考文献


    参考文献:10.1107/s1600536811009536
    摘要:Khan IU, Khan MH, Arshad MN, Akkurt M. 2-(4-Chloro-benzamido)-acetic acid. Acta Crystallogr Sect E Struct Rep Online. 2011 Apr 01;67(Pt 4):o916.
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