Synthesis of cyclopropylacetylene
    3.
    发明授权
    Synthesis of cyclopropylacetylene 失效
    环丙基乙炔的合成

    公开(公告)号:US6028237A

    公开(公告)日:2000-02-22

    申请号:US990471

    申请日:1997-12-15

    摘要: The present invention relates generally to novel methods for the synthesis of cyclopropylacetylene which is a reagent in the asymmetric synthesis of (S)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-1,4-dihydro-2H-3,1-benzoxazin-2-one which is a useful human immunodeficiency virus (HIV) reverse transcriptase inhibitor.

    摘要翻译: 本发明一般涉及用于合成环己基乙炔的新方法,该环乙炔是不对称合成(S)-6-氯-4-环丙基乙炔基-4-三氟甲基-1,4-二氢-2H- 苯并恶嗪-2-酮,其是有用的人类免疫缺陷病毒(HIV)逆转录酶抑制剂。

    Crystalline (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-3,4-dihydro-2(1H)-quinazolinone
    4.
    发明授权
    Crystalline (-)-6-chloro-4-cyclopropylethynyl-4-trifluoromethyl-3,4-dihydro-2(1H)-quinazolinone 失效
    ( - ) - 6-氯-4-环丙基乙炔基-4-三氟甲基-3,4-二氢-2(1H) - 喹唑啉酮

    公开(公告)号:US06225317B1

    公开(公告)日:2001-05-01

    申请号:US09442605

    申请日:1999-11-18

    IPC分类号: C07D23472

    CPC分类号: C07D239/80 C07D239/78

    摘要: The potent reverse transcriptase inhibitor (−)-6-Chloro-4-cyclopropylethynyl-4-trifluoromethyl-3,4-dihydro-2(1H)-quinazolinone is produced in solvate and crystalline form. These forms are designated Forms 1 and 2, and are characterized by x-ray powder diffraction and differential scanning calorimetry. Pharmaceutical compositions and methods are useful for the treatment of the human immunodeficiency virus (HIV).

    摘要翻译: 以溶剂化物和结晶形式产生有效的逆转录酶抑制剂( - )-6-氯-4-环丙基乙炔基-4-三氟甲基-3,4-二氢-2(1H) - 喹唑啉酮。 这些形式指定为形式1和2,其特征在于X-射线粉末衍射和差示扫描量热法。 药物组合物和方法可用于治疗人类免疫缺陷病毒(HIV)。