Enantioselective alkylation of tricyclic compounds
    1.
    发明授权
    Enantioselective alkylation of tricyclic compounds 有权
    三环化合物的对映选择性烷基化

    公开(公告)号:US06288233B1

    公开(公告)日:2001-09-11

    申请号:US09667411

    申请日:2000-09-21

    IPC分类号: C07D22106

    摘要: Disclosed is a process for preparing a compound of the formula: wherein X1, X2, X3, X4, and X5 are independently selected from the group consisting of H, halo, alkyl, alkoxy, aryl, and aryloxy, and R is a protecting group, in which a compound having the formula wherein X1, X2, X3, X4, and X5 are as defined above, is treated with the following, in any sequence: (a) a non-nucleophilic strong base; (b) a chiral amino alcohol; and (c) a compound having the formula wherein L is a leaving group and R is as defined above. The compounds made by this process are useful intermediates for preparing compounds that are inhibitors of farnesyl protein transferase. Also disclosed is a compound having the formula:

    摘要翻译: 公开了一种制备下式化合物的方法:其中X 1,X 2,X 3,X 4和X 5独立地选自H,卤素,烷基,烷氧基,芳基和芳氧基,R是保护基 其中具有如下定义的具有如下定义的化合物:(a)非亲核性强碱;(b)手性氨基醇(其中R 1,R 2,R 3,X 4, ; 和(c)具有甲醛的化合物L是离去基团,R如上定义。 通过该方法制备的化合物是制备法呢基蛋白转移酶抑制剂的化合物的有用中间体。 还公开了具有下式的化合物:

    Synthesis of intermediates useful in preparing tricyclic compounds
    2.
    发明授权
    Synthesis of intermediates useful in preparing tricyclic compounds 失效
    可用于制备三环化合物的中间体的合成

    公开(公告)号:US06492519B2

    公开(公告)日:2002-12-10

    申请号:US09836605

    申请日:2001-04-17

    IPC分类号: C07D22106

    CPC分类号: C07D213/79 C07D221/16

    摘要: A process is provided for preparing a compound having the formula comprising: (a) reacting a compound having the formula with an isocyanate having the formula R1NCO to produce a compound having the formula (b) optionally hydrolyzing the compound of formula (III) to form an amide having the formula (c) reacting the compound of formula (III) or the amide of formula (IV) with a compound having the formula in the presence of a strong base to produce a compound having the formula and (d) cyclizing the compound of formula (VI) to obtain the compound of formula (I), wherein R is H or Cl; M is selected from the group consisting of Li, Na, K, MgX, ZnRA, and Al(RA)2; RA is alkyl; X is halo; R1 is selected from the group consisting of alkyl, aryl, aralkyl, heteroaryl, heteroaralkyl, cycloalkyl, cycloalkylalkyl, heterocycloalkyl, and heterocycloalkylalkyl; and L is a leaving group.

    摘要翻译: 提供了一种制备具有以下方法的化合物的方法:(a)使具有式R1NCO的异氰酸酯的化合物与具有式(b)的化合物反应,任选地水解式(III)化合物以形成酰胺 具有式(c)使式(III)的化合物或式(IV)的酰胺与具有式的化合物存在强碱反应以产生具有下式的化合物:(d)使式(III)的化合物( VI),得到其中R为H或Cl的式(I)化合物; M选自Li,Na,K,MgX,ZnRA和Al(RA)2; RA是烷基; X是卤素; R 1选自烷基,芳基,芳烷基,杂芳基,杂芳烷基,环烷基,环烷基烷基,杂环烷基和杂环烷基烷基; 而L是离职团体。