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    Synthesis of intermediates useful in preparing tricyclic compounds
    1.
    发明授权
    Synthesis of intermediates useful in preparing tricyclic compounds 有权
    可用于制备三环化合物的中间体的合成

    公开(公告)号：US06372909B1

    公开(公告)日：2002-04-16

    申请号：US09442512

    申请日：1999-11-18

    申请人： Charles F. Bernard ,  Michael Casey ,  Frank Xing Chen ,  Denise C. Grogan ,  Marc Poirier ,  Robert P. Williams ,  Yee-Shing Wong ,  George G. Wu

    发明人： Charles F. Bernard ,  Michael Casey ,  Frank Xing Chen ,  Denise C. Grogan ,  Marc Poirier ,  Robert P. Williams ,  Yee-Shing Wong ,  George G. Wu

    IPC分类号： C07F980

    CPC分类号： C07D221/16

    摘要： Disclosed is a process for preparing a compound having the formula: wherein R, R1, R2, R3, and R4 are independently selected from the group consisting of H, Br, Cl, F, alkyl, or alkoxy, by (A) reacting a compound having the formula  wherein RA, RC, RD, and RE are independently selected from the group consisting of H, halo, alkyl, or alkoxy, and R5 is aryl or heteroaryl, with a dehydrating agent to produce an imine having the formula: (B) hydrolyzing the imine produced in step (A) to produce the compound having formula (I). Also disclosed are novel intermediates having the formula:  wherein RA, RB, RC, RD, and RE are independently selected from the group consisting of H, halo, alkyl, or alkoxy, and R5 is aryl or heteroaryl. Also disclosed is a process for preparing a compound having the formula:  comprising: reacting a compound having the formula:  with NH2R5 in the presence of a palladium catalyst, carbon monoxide, a base, and an ether selected from the group consisting of: CH3OCH2CH2OCH3; CH3OCH2CH2OCH2CH2OCH3; and CH3OCH2CH2OCH2CH2OCH2CH2OCH3, wherein X is H, Br, Cl, or F, and R5 is aryl or heteroaryl. The compounds made by these processes are useful intermediates for preparing compounds that are antihistamines or inhibitors of farnesyl protein transferase.

    摘要翻译： 公开了一种制备具有下式的化合物的方法：其中R，R 1，R 2，R 3和R 4独立地选自H，Br，Cl，F，烷基或烷氧基，通过（A）使 具有下式的化合物其中RA，RC，RD和RE独立地选自H，卤素，烷基或烷氧基，R5是芳基或杂芳基，与脱水剂反应生成具有下式的亚胺：（B ）水解步骤（A）中产生的亚胺以制备具有式（I）的化合物。 还公开了具有下式的新型中间体：其中RA，RB，RC，RD和RE独立地选自H，卤素，烷基或烷氧基，R5是芳基或杂芳基。 还公开了制备具有下式的化合物的方法：包括：在钯催化剂，一氧化碳，碱和选自以下的醚的存在下使具有下式的化合物与NH 2 R 5反应：CH 3 OCH 2 CH 2 OCH 3; CH3OCH2CH2OCH2CH2OCH3; 和CH 3 OCH 2 CH 2 OCH 2 CH 2 OCH 2 CH 2 OCH 3，其中X是H，Br，Cl或F，R 5是芳基或杂芳基。 通过这些方法制备的化合物是制备抗组胺剂或法呢基蛋白转移酶抑制剂的化合物的有用中间体。

    Synthesis of intermediates useful in preparing tricyclic compounds
    6.
    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

    申请人： Marc Poirier ,  Yee-Shing Wong ,  George G. Wu

    发明人： Marc Poirier ,  Yee-Shing Wong ,  George G. Wu

    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。

    Synthesis of intermediates useful in preparing tricyclic compounds
    7.
    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：US5998620A

    公开(公告)日：1999-12-07

    申请号：US45803

    申请日：1998-03-23

    申请人： Xing Chen ,  Marc Poirier ,  Yee-Shing Wong ,  Guang-Zhong Wu

    发明人： Xing Chen ,  Marc Poirier ,  Yee-Shing Wong ,  Guang-Zhong Wu

    IPC分类号： C07D221/16 ,  C07D401/04 ,  C07D221/06

    CPC分类号： C07D401/04 ,  C07D221/16

    摘要： The invention relates to a process for preparing a compound of the formula ##STR1## comprising reacting a bromo-substituted pyridine with an amine of the formula NHR.sup.5 R.sup.6, reacting the resulting amide with an iodo-halomethyl-substituted compound and cyclizing the resultant product, wherein R, R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are as defined in the specification; also claimed are a compound of the formula ##STR2## and a process for preparing it from the corresponding halo-substituted benzoic acid.

    摘要翻译： 本发明涉及一种制备下式化合物的方法，其中包括使溴取代的吡啶与式NHR 5 R 6的胺反应，使得到的酰胺与碘代卤代甲基取代的化合物反应，并使得到的产物环化，其中R，R 1 R2，R3和R4如说明书中所定义; 还要求的是下式的化合物及其由相应的卤代取代的苯甲酸制备的方法。

    Synthesis of intermediates useful in preparing bromo-substituted tricyclic compounds
    8.
    发明授权
    Synthesis of intermediates useful in preparing bromo-substituted tricyclic compounds 失效
    可用于制备溴代三环化合物的中间体的合成

    公开(公告)号：US5760232A

    公开(公告)日：1998-06-02

    申请号：US882753

    申请日：1997-06-16

    申请人： Xing Chen ,  Marc Poirier ,  Yee-Shing Wong ,  Guang-Zhong Wu

    发明人： Xing Chen ,  Marc Poirier ,  Yee-Shing Wong ,  Guang-Zhong Wu

    IPC分类号： C07D401/04 ,  C07D221/16

    CPC分类号： C07D401/04

    摘要： The invention relates to a process for preparing a compound of the formula ##STR1## comprising: (a) reacting 2,5-dibromo-3-methylpyridine with an amine of the formula NHR.sup.5 R.sup.6 to obtain an amide; (b) reacting the amide with a compound of formula 3 ##STR2## in the presence of a strong base to obtain a compound of formula 4 ##STR3## (c) converting a compound of formula 4 to the corresponding cyano compound or aldehyde; (d) reacting the cyano compound or aldehyde with a piperidine derivative to obtain an aldehyde or alcohol of formula 7a or 7b, respectively: ##STR4## (e) cyclizing a compound of formula 7a or 7b; wherein R.sup.1 -R.sup.7 are as defined in the specification.

    摘要翻译： 本发明涉及制备式I化合物的方法，其包括：（a）使2,5-二溴-3-甲基吡啶与式NHR 5 R 6的胺反应，得到酰胺; （b）在强碱存在下使酰胺与式3化合物反应，得到式4化合物（c）将式4的化合物转化成相应的氰基化合物或醛 ; （d）使氰基化合物或醛与哌啶衍生物反应，分别得到式7a或7b的醛或醇：（e）使式7a或7b的化合物环化; 其中R1-R7如说明书中所定义。