Processes for the preparation of regadenoson and a new crystalline form thereof
    15.
    发明授权
    Processes for the preparation of regadenoson and a new crystalline form thereof 有权
    制备regadenoson的方法及其新的结晶形式

    公开(公告)号:US08859522B2

    公开(公告)日:2014-10-14

    申请号:US14112173

    申请日:2012-04-26

    IPC分类号: C07H19/16 C07H1/00 C07H19/167

    CPC分类号: C07H19/16 C07H1/00 C07H19/167

    摘要: This disclosure relates to an improved process for the preparation of regadenoson, pharmaceutically acceptable salts thereof, and hydrates thereof, and for the preparation of intermediates useful in the synthesis of regadenoson. The disclosure also relates to a new crystalline form of regadenoson. Processes for the preparation of the crystalline form, compositions containing the crystalline form, and methods of use thereof are also described.

    摘要翻译: 本公开涉及一种改进的制备regadenoson,其药学上可接受的盐及其水合物以及制备可用于合成regadenoson的中间体的方法。 本公开还涉及regadenoson的新结晶形式。 还描述了制备结晶形式的方法,含有结晶形式的组合物及其使用方法。

    Fungicidal compositions and methods of making thereof
    18.
    发明授权
    Fungicidal compositions and methods of making thereof 有权
    杀真菌组合物及其制备方法

    公开(公告)号:US6140511A

    公开(公告)日:2000-10-31

    申请号:US326225

    申请日:1999-06-04

    摘要: The fungicidal compound 4,5-dimethyl-N-2-propenyl-2-(trimethylsilyl)-3-thiophenecarboxamide (Formula (I) shown superior and unexpected control of the growth of the soil-borne fungus Gaeumannomyces graminis (Gg). The present invention provides a novel compound for synthesizing the compound of Formula (I) which uses the compound 4-hydroxy-4,5-dimethyl-2-trimethylsilanyl-dihydrothiophene-3-carboxylic acid allylamide (Formula (II)) as well as novel compounds of synthesizing the allylamide. In addition, Formula (II) itself has unexpectedly been found to provide control of Gg. Therefore, the compounds having Formula (III): ##STR1## or an agronomic salts and compositions thereof are expected to provide such control as well; wherein:Q is --NH, S, or O;W is O, or S;X is --OH, --OAc, --OR, where R is lower alkyl;Y is S, O, or --NH;Z is --Si(R).sub.3, --C(R).sub.3, where R is lower alkyl;R.sub.1 is a lower alkyl, allyl, or propargyl;R.sub.2 is a lower alkyl or aryl; andR.sub.3 and R.sub.4 are independently chosen from hydrogen, a lower alkyl and aryl;optionally, R.sub.2 and R.sub.3 together form a 5- or 6-membered ring.

    摘要翻译: 杀真菌化合物4,5-二甲基-N-2-丙烯基-2-(三甲基甲硅烷基)-3-噻吩甲酰胺(式(I))显示出对土壤真菌Gaeumannomyces graminis(Gg)的生长的优异和意想不到的控制。 本发明提供用于合成使用化合物4-羟基-4,5-二甲基-2-三甲基硅烷基 - 二氢噻吩-3-甲酸烯丙基酰胺(式(II))的式(I)化合物的新化合物以及新颖的 此外,意外地发现式(II)本身提供了对Gg的控制。因此,具有式(III)的化合物或其农艺盐及其组合物也预期也提供这样的控制; 其中:Q是-NH,S或O; W是O或S; X是-OH,-OAc,-OR,其中R是低级烷基; Y是S,O或-NH; Z是-Si (R)3,-C(R)3,其中R是低级烷基; R 1是低级烷基,烯丙基或炔丙基; R 2是低级烷基或芳基; R 3和R 4独立地选自氢,低 烷基和芳基; 任选地,R 2和R 3一起形成5-或6-元环。