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    Aziridinyl quinone antitumor agents
    4.
    发明授权
    Aziridinyl quinone antitumor agents 失效
    氮丙啶醌抗肿瘤药

    公开(公告)号：US4233215A

    公开(公告)日：1980-11-11

    申请号：US954218

    申请日：1978-10-24

    申请人： John S. Driscoll ,  A. Hameed Khan ,  Feng-Te Chou

    发明人： John S. Driscoll ,  A. Hameed Khan ,  Feng-Te Chou

    IPC分类号： C07D203/14 ,  C07D295/12

    CPC分类号： C07D203/14

    摘要： The use of aziridinyl quinones as antitumor agents against transplanted tumors in mice is disclosed. A compound which has been found to be particularly effective is the compound 2,5-diaziridinyl-3,6-bis (carboethoxyamino)-1,4-benzoquinone. Treatment is described in connection with several transplanted mouse tumor test systems including various forms of leukemia, for example, as well as B16 melanoma, Lewis lung carcinoma, and the ependymoblastoma brain tumor system.

    摘要翻译： 公开了使用氮丙啶醌作为抗小鼠移植肿瘤的抗肿瘤剂。 已经发现特别有效的化合物是化合物2,5-二氮丙啶基-3,6-双（乙氧羰氨基）-1,4-苯醌。 关于包括各种形式的白血病的几种移植的小鼠肿瘤测试系统，例如以及B16黑素瘤，Lewis肺癌和室管膜母细胞瘤脑肿瘤系统描述了治疗。

    Diastereoselective process leading to a key intermediate for the preparation of fluorinated reverse transcriptase inhibitors
    7.
    发明授权
    Diastereoselective process leading to a key intermediate for the preparation of fluorinated reverse transcriptase inhibitors 失效
    导致氟化逆转录酶抑制剂制备的关键中间体的非对映选择性过程

    公开(公告)号：US5498719A

    公开(公告)日：1996-03-12

    申请号：US189095

    申请日：1994-01-31

    申请人： Victor E. Marquez ,  John S. Driscoll ,  Magbool A. Siddiqui

    发明人： Victor E. Marquez ,  John S. Driscoll ,  Magbool A. Siddiqui

    IPC分类号： C07D317/26 ,  C07D317/30 ,  C07D413/06

    CPC分类号： C07D413/06 ,  C07D317/26 ,  C07D317/30

    摘要： The present invention provides a novel synthetic route to a key precursor, i.e., an (S,S)-.alpha.-fluoro-2,2-dimethyl-1,3-dioxolane-4-propanoic acid ester useful in the preparation of FddA and FddC. The instant diastereoselective process utilizes a novel intermediate which contains a chiral auxiliary. The chiral auxiliary can be any chiral auxiliary moiety such as for example an auxiliary containing a substituted oxazolidinone group. The intermediate containing the chiral auxiliary is fluorinated utilizing a fluorination method applied for the first time in the synthesis of fluorinated sugars to give a fluorinated intermediate which after removal of the chiral group provides the desired key intermediate. In summary, in the instant process, a fluorine is introduced diastereoselectively into an intermediate via the reaction of a chiral enolate with an electrophilic fluorinating agent and the intermediate which is fluorinated is derived from mannitol.

    摘要翻译： 本发明提供了一种关键前体的新型合成途径，即用于制备FddA的（S，S）-α-氟-2,2-二甲基-1,3-二氧戊环-4-丙酸酯 FddC。 即时非对映选择性方法利用含有手性助剂的新型中间体。 手性助剂可以是任何手性辅助部分，例如含有取代的恶唑烷酮基团的助剂。 包含手性助剂的中间体在氟化糖的合成中首次使用氟化方法进行氟化，得到氟化中间体，其在除去手性基团后提供所需的关键中间体。 总之，在本发明的方法中，通过手性烯醇化物与亲电氟化剂的反应将氟非对映选择性引入中间体，并且氟化的中间体衍生自甘露醇。