CAS: 4880-92-6; Apovincamine

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CAS号42971-09-5 长春西汀

📜长春胺置于对甲苯磺酸体系中,用 甲苯 作为反应溶剂,化学反应 2.0H,以95%的收率获得产物阿扑长春胺
参考文献:通过重新设计长春胺的生物活性来防止吗啡寻求行为.
标题:通过重新设计长春胺的生物活性来防止吗啡寻求行为.
摘要:创新的发现策略对于解决美国持续存在的阿片类药物流行病至关重要.滥用处方药和非法阿片类药物(例如吗啡,海洛因)导致了成瘾和用药过量的严重问题.我们使用长春胺(一种吲哚生物碱)作为合成起点,对其复杂的稠合环系统进行显着的结构改变,从而合成了 80 种具有复杂分子结构的不同化合物.针对一组 168 个 Gpcr 药物靶点筛选了一系列精选的长春胺衍生化合物的激动和拮抗活性.尽管长春胺没有效果,但新型化合物 4 (V2A) 表现出对下丘脑分泌素(食欲素)受体 2 的拮抗活性.当进行动物研究时,4 (V2A) 显着预防急性吗啡条件性位置偏爱 (Cpp) 和应激诱导的恢复在阿片类药物奖励和复发的小鼠模型中,吗啡-Cpp 熄灭的情况.这些结果表明,长春胺的环变形为探索与阿片类药物成瘾相关的新化学空间提供了一种有前途的方法.
DOI:10.1021/acs.Jmedchem.9B01924

专利信息

专利号:US-4379935-A
优先权日:1980-08-04
标 题 :Process for the synthesis of vincamine and related indole alkaloids
发明人：PARACCHINI SILVANO; MORA PAOLO C
权利人:CORVI MORA PAOLO
摘要:A process is taught for the synthesis of vincamine and related indole alkaloids, according to which, through only two steps and through a novel synthesis intermediate, namely the glycidic ester, having the formula ##STR1## wherein R' represents --COOCH 3 or --COOCH 2 CH 3 , 1-ethyl-1,2,3,4,5,6,7,12b-octahydroindole[2,3-a]quinolizine-1-carboxaldehyde is reacted with a haloester in the presence of a base and the glycidic ester is converted to vincamine or apovincamine or like esters by reaction with a Lewis acid or a mineral acid, the reaction products being subsequently separated by chromatography.

专利号:US-4316029-A
优先权日:1979-06-22
标 题:Synthesis of vincaminic acid derivatives
发明人：ROSSEY GUY
权利人:SYNTHELABO
摘要:Vincaminic acid derivatives of formula (A) ##STR1## useful in treating cerebral insufficiency, are prepared by reacting 1-ethyl-2,3,4,6,7,12-hexahydroindolo[2,3-a]quinolizine with the 2,4-DNP hydrazone of ethyl or methyl bromopyruvate followed by (i) reduction of the Câ•?N bond and (ii) simultaneous cyclization with removal of the ketone-protecting group in either order.

专利号:US-11130764-B2
优先权日:2017-02-17
标题 :Analogs of vincamine and uses thereof
发明人：HUIGENS III ROBERT WILLIAM; NORWOOD IV VERRILL M; LUESCH HENDRIK
权利人:UNIV FLORIDA
摘要:The present disclosure provides compounds of any one of Formulae (I′), (I), (IA), (II′), (II), (IIA), (IIIA), (III″), (III′), (III), (IIIA), (IV), (V′), (V), (VI), (VII), (VIII′), (VIII), (IX′), (IX), and (X). The compounds described herein may be useful in treating and/or preventing a broad range of diseases (e.g., proliferative disease (e.g., cancers (e.g., non-small cell lung cancer, or glioma), inflammatory diseases, autoimmune diseases), CNS disorder (e.g., drug addiction), metabolic disorder (e.g., diabetes), or infectious disease (e.g., bacterial infection or parasitic infection (e.g., malaria))). Also provided in the present disclosure are pharmaceutical compositions, methods of synthesis of a compound described herein, kits, methods, and uses including or using a compound described herein.

专利号:CN-102485723-A
优先权日:2010-12-02
标题 :One-pot semi-synthesis of vinpocetine and its water-soluble salts

专利号:JP-S5758683-A
优先权日:1980-08-04
标 题:Synthesis of vincamine and related indole alkaloids

专利号:EP-0045918-A1
优先权日:1980-08-04
标 题:A process for the synthesis of vincamine and related indole alkaloids