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    Alkaloid esters
    1.
    发明授权
    Alkaloid esters 失效
    生物碱类

    公开(公告)号：US4035370A

    公开(公告)日：1977-07-12

    申请号：US645244

    申请日：1975-12-29

    申请人： Csaba Lorincz ,  Egon Karpati ,  Laszlo Szporny ,  Kalman Szasz ,  Lajos Kisfaludy

    发明人： Csaba Lorincz ,  Egon Karpati ,  Laszlo Szporny ,  Kalman Szasz ,  Lajos Kisfaludy

    IPC分类号： C07D461/00 ,  C07D459/00

    CPC分类号： C07D461/00 ,  Y10S514/929

    摘要： Vasodilatory eburnamine-type alkaloid esters of the formula (I) ##STR1## and salts and quaternary derivatives thereof, wherein X.about.Y REPRESENTS A =CH=CH- or ##STR2## R represents a C.sub.1-6 alkoxycarbonyl group optionally substituted with a hydroxy group or with a halogen atom, further an alkenyloxycarbonyl, aryloxycarbonyl, aralkoxycarbonyl group or an acylated primary alcohol group, especially apovincaninic acid ethyl ester, have been prepared by various methods of esterification.

    摘要翻译： 式（I）的血管扩张性本burn胺型生物碱及其盐和季衍生物，其中X代表Y代表A = CH = CH-或R表示任选取代的C 1-6烷氧基羰基 具有羟基或卤素原子，还通过各种酯化方法制备了链烯氧基羰基，芳氧基羰基，芳烷氧基羰基或酰化伯醇基，特别是亚氨基二乙酸乙酯。

    Process for the isolation of alkaloid components from the plant Vinca Rosea L.
    9.
    发明授权
    Process for the isolation of alkaloid components from the plant Vinca Rosea L. 失效
    从植物中分离生物碱成分的方法长春花

    公开(公告)号：US4172077A

    公开(公告)日：1979-10-23

    申请号：US908584

    申请日：1978-05-22

    申请人： Karola Jovanovics ,  Gyorgy Fekete ,  Eszter Dezseri ,  Lajos Dancsi ,  Csaba Lorincz ,  Bela Szarvady ,  Gyorgy Dobo ,  Csaba Szantay ,  Lajos Szabo

    发明人： Karola Jovanovics ,  Gyorgy Fekete ,  Eszter Dezseri ,  Lajos Dancsi ,  Csaba Lorincz ,  Bela Szarvady ,  Gyorgy Dobo ,  Csaba Szantay ,  Lajos Szabo

    IPC分类号： C07D471/18 ,  C07D471/20 ,  C07D471/22 ,  C07D519/04 ,  C07D215/00 ,  C07G5/00

    CPC分类号： C07D519/04

    摘要： Tumor inhibiting alkaloids are recovered from Vinca Rosea L. by a method which comprises extracting the dried leaves with a solvent selected from the group consisting of an alkanol having 1 to 5 carbon atoms, a mixture of an alkanol having 1 to 5 carbon atoms and a dilute, aqueous solution, benzene and benzene homologs; subsequently purifying the alkaloid extract obtained by a phase-change method between immiscible solvents, precipitating the main amount of dimeric alkaloids in form of their sulphuric acid addition salts, isolating leurosine, vincistine, vinblastine, desacetoxy-vinblastine, N-desmethyl-vinblastine and desacetyl-vinblastine from the salt mixture obtained, and then completing the separation and isolation of the remaining alkaloids by separation and isolation by adjusting the pH-value of the mother liquor, after precipitation and removal of the salt mixture, to 5.5 to 10, extracting the solution with a water-immiscible organic solvent and separating vindoline, catharantine, 3',4' -anhydrovinblastine and leurosine from the extract by chromatography, extracting vindoline in the pH-range of 2.5 to 3.5 and catharantine 3',4'-anhydrovinblastine and leurosine in the pH-range of 5 to 6 with benzene or a benzene homologue, from the mother liquor obtained when isolating the salt mixture, and separating a mixture of leurosine and 3',4'-anhydrovinblastine by crystallization, epoxidizing this mixture with an oxygen source, or separating the mixture into its components by chromatography, and subsequently epoxidizing the 3',4'-anhydrovinblastine component to leurosine, and isolating catharantine remaining from the mother liquor obtained when separating the crystalline mixture, or separating the extract containing catharantine, 3',4'-anhydrovinblastine and leurosine into its components by chromatography.

    摘要翻译： 通过包括用选自具有1至5个碳原子的链烷醇，具有1至5个碳原子的链烷醇和1至5个碳原子的链烷醇的溶剂萃取干燥叶子的方法从长春花（Vinca Rosea L.）回收肿瘤抑制生物碱 稀释水溶液，苯和苯同系物; 随后将不相溶溶剂之间的相变法获得的生物碱提取物纯化，以其硫酸加成盐的形式沉淀出主要量的二聚生物碱，分离出白蛋白，长春新碱，长春花碱，去乙酰氧基 - 长春花碱，N-去甲基长春花碱和去乙酰基 从所得的盐混合物中分离并分离残留的生物碱，然后通过调节沉淀和除去盐混合物后的pH值，分离和分离，得到5.5〜10 溶液与水不混溶的有机溶剂混合，并通过色谱法从提取物中分离出vindoline，catharantine，3'，4'-脱氢长春花碱和leurosine，在2.5至3.5的pH范围内提取vindoline，并检测3'，4'-脱氢长春花碱和 柠檬酸在5〜6的pH范围内用苯或苯同系物，从分离盐混合物时得到的母液，和sepa 通过结晶评估白蛋白和3'，4'-脱氢长春花碱的混合物，用氧源将该混合物环氧化，或通过色谱法将该混合物分离成其组分，随后将3'，4'-脱氢长春花碱组分环氧化成亮氨酸，以及 隔离离开结晶混合物时获得的母液中残留的检疫物，或通过色谱法将含有检疫胺，3'，4'-脱氢长春花碱和酪氨酸的提取物分离成其组分。