Chemical synthesis of azaindoles
    1.
    发明授权
    Chemical synthesis of azaindoles 失效
    氮杂吲哚的化学合成

    公开(公告)号:US5681959A

    公开(公告)日:1997-10-28

    申请号:US604133

    申请日:1996-02-20

    IPC分类号: C07D471/04

    CPC分类号: C07D471/04

    摘要: The present invention relates to a process for the preparation of azaindole derivatives of the formula ##STR1## wherein Q is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl, C.sub.1-6 alkoxy, hydroxy, aryl or arylC.sub.1-4 alkyl; one of X, Y and Z is --N.dbd. and the others are --CH.dbd.; R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.2-6 alkenyl or C.sub.1-6 alkyl substituted by a group selected from aryl or --NR.sup.2 R.sup.3 where R.sup.2 and R.sup.3 each independently represent C.sub.1-4 alkyl, or R.sup.2 and R.sup.3, together with the nitrogen atom to which they are attached, form a 4-7 membered saturated heterocyclic ring, optionally containing in the ring an oxygen or sulphur atom or a group NR.sup.4 where R.sup.4 is C.sub.1-4 alkyl, aryl or arylC.sub.1-4 alkyl; and R.sup.5 is a hydrogen atom or a group selected from C.sub.1-6 alkyl or aryl.

    摘要翻译: 本发明涉及制备式(III)的氮杂吲哚衍生物的方法,其中Q是氢,C 1-6烷基,C 2-6烯基,C 1-6烷氧基,羟基,芳基或芳基C 1-4烷基; X,Y和Z之一为-N =,其余为-CH =; R 1是氢,C 1-6烷基,C 2-6烯基或被选自芳基或-NR 2 R 3的基团取代的C 1-6烷基,其中R 2和R 3各自独立地代表C 1-4烷基,或R 2和R 3与它们所在的氮原子一起 形成4-7元饱和杂环,任选地在环中含有氧或硫原子或基团NR4,其中R4是C1-4烷基,芳基或芳基C1-4烷基; R5为氢原子或选自C1-6烷基或芳基的基团。

    Chemical synthesis of 1,4-oxazin-2-ones
    8.
    发明授权
    Chemical synthesis of 1,4-oxazin-2-ones 失效
    1,4-恶嗪-2-酮的化学合成

    公开(公告)号:US6046325A

    公开(公告)日:2000-04-04

    申请号:US391705

    申请日:1999-09-08

    IPC分类号: C07D265/32

    CPC分类号: C07D265/32

    摘要: The present invention relates to a process for the preparation of a compound of formula (I): ##STR1## wherein R.sup.1 is a C.sub.1-6 alkyl or arylC.sub.1-4 alkyl group; and R.sup.2 is a hydrogen atom, a halogen atom, or a group selected from C.sub.1-6 alkyl, CF.sub.3 or C.sub.1-6 alkoxy substituted by C.sub.1-4 alkoxy; which comprises reacting an anhydrous or hydrated glyoxal of formula (II) with a compound of formula (III): ##STR2## in the presence of an acid.

    摘要翻译: 本发明涉及制备式(I)化合物的方法:其中R 1是C 1-6烷基或芳基C 1-4烷基; R 2为氢原子,卤原子或选自被C 1-4烷氧基取代的C 1-6烷基,CF 3或C 1-6烷氧基的基团; 其包括使式(II)的无水或水合乙二醛与式(III)的化合物在酸的存在下反应。

    Chemical synthesis of a chiral oxazinone
    9.
    发明授权
    Chemical synthesis of a chiral oxazinone 失效
    手性恶嗪酮的化学合成

    公开(公告)号:US5668280A

    公开(公告)日:1997-09-16

    申请号:US652081

    申请日:1996-05-23

    IPC分类号: C07D265/32

    CPC分类号: C07D265/32

    摘要: The present invention provides a process for the preparation of substantially pure N-benzyl-3-(S)-(4-fluorophenyl)-1,4-oxazin-2-one which comprises:(i) contacting racemic N-benzyl-3-(4-fluorophenyl)-1,4-oxazin-2-one with (-)-3-bromocamphor-8-sulphonic acid (hereinafter referred to as (-)-3-BCS) in the presence of a racemising agent;(ii) collecting the resultant crystalline (-)-3-BCS salt of N-benzyl-3-(S)-(4-fluorophenyl)-1,4-oxazin-2-one; and(iii) liberating the free base of N-benzyl-3-(S)-(4-fluorophenyl)-1,4-oxazin-2-one by treatment of the (-)-3-BCS salt collected in step (ii) with aqueous base.

    摘要翻译: 本发明提供了制备基本上纯的N-苄基-3-(S) - (4-氟苯基)-1,4-恶嗪-2-酮的方法,其包括:(i)使外消旋N-苄基-3 - (4-氟苯基)-1,4-恶嗪-2-酮与( - ) - 3-溴樟脑磺酸(以下称为( - ) - 3-BCS)在消旋剂存在下反应; (ⅱ)收集N-苄基-3-(S) - (4-氟苯基)-1,4-恶嗪-2-酮的所得结晶( - ) - 3-BCS盐; 和(iii)通过处理步骤(1)中收集的( - ) - 3-BCS盐,释放N-苄基-3-(S) - (4-氟苯基)-1,4-恶嗪-2-酮的游离碱 ii)与碱水溶液。