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    Process for Preparing Pyrido[2,3-d]pyrimidin-7-one and 3,4-Dihydropyrimido[4,5-d]pyrimidin-2(1H)-one Derivatives
    35.
    发明申请
    Process for Preparing Pyrido[2,3-d]pyrimidin-7-one and 3,4-Dihydropyrimido[4,5-d]pyrimidin-2(1H)-one Derivatives 审中-公开
    制备吡啶并[2,3-d]嘧啶-7-酮和3,4-二氢嘧啶并[4,5-d]嘧啶-2（1H） - 酮衍生物的方法

    公开(公告)号：US20090048444A1

    公开(公告)日：2009-02-19

    申请号：US12253327

    申请日：2008-10-17

    Applicant: James F. Callahan ,  Jeffrey C. Boehm ,  Zehong Wan ,  Hongxing Yan ,  Xichen Lin

    Inventor： James F. Callahan ,  Jeffrey C. Boehm ,  Zehong Wan ,  Hongxing Yan ,  Xichen Lin

    IPC: C07D487/04 ,  C07D471/04

    CPC classification number: C07D487/04 ,  C07D471/04

    Abstract: The present invention is directed to a novel method of preparing of 2,4,8-trisubstituted pyrido[2,3-d]pyrimidin-7-one pharmacophores of Formula (II) or (IIa) wherein G1 is CH2; G2 is CH; Rx is chloro, bromo, iodo, or O—S(O)2CF3; Rg is a C1-10 alkyl; m is 0, or an integer having a value of 1, or 2; R3 is a C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted. which comprises reacting a compound of the formula: wherein Ry is chloro, bromo, iodo, O—S(O)2CF3; and Rg is a C1-10 alkyl; with a olefin forming reagent in a suitable base to yield a compound of Formula (II), or (IIa) wherein m=0 and oxidizing the sulphur as necessary or desired.

    Abstract translation: 本发明涉及制备式（II）或（IIa）的2,4,8-三取代吡啶并[2,3-d]嘧啶-7-酮药代动力学的新方法，其中G1是CH2; G2是CH; R x是氯，溴，碘或O-S（O）2 C 3 F 3; Rg为C1-10烷基; m为0，或值为1或2的整数; R 3是C 1-10烷基，C 3-7环烷基，C 3-7环烷基C 1-10烷基，芳基，芳基C 1-10烷基，杂芳基，杂芳基C 1-10烷基，杂环基或杂环基C 1-10烷基部分，并且其中 部分可以任选被取代。 其包括使下式化合物：其中R y是氯，溴，碘，O-S（O）2 C 3 F 3; 且R g为C 1-10烷基; 在合适的碱中加入烯烃形成试剂，得到式（II）化合物或其中m = 0的（IIa），并根据需要氧化硫。

    Process for preparing pyrido[2,3-d]pyrimidin-7-one and 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one derivatives
    36.
    发明授权
    Process for preparing pyrido[2,3-d]pyrimidin-7-one and 3,4-dihydropyrimido[4,5-d]pyrimidin-2(1H)-one derivatives 失效
    制备吡啶并[2,3-d]嘧啶-7-酮和3,4-二氢嘧啶并[4,5-d]嘧啶-2（1H） - 酮衍生物的方法

    公开(公告)号：US07479558B2

    公开(公告)日：2009-01-20

    申请号：US11388375

    申请日：2006-03-24

    Applicant: James F. Callahan ,  Jeffrey C. Boehm ,  Zehong Wan ,  Hongxing Yan ,  Xichen Lin

    Inventor： James F. Callahan ,  Jeffrey C. Boehm ,  Zehong Wan ,  Hongxing Yan ,  Xichen Lin

    IPC: C07D487/04 ,  C07D239/30 ,  C07D413/04 ,  C07D471/04

    CPC classification number: C07D487/04 ,  C07D471/04

    Abstract: The present invention is directed to a novel method of preparing of 2,4,8-trisubstituted pyrido[2,3-d]pyrimidin-7-one pharmacophores of Formula (II) or (IIa) wherein G1 is CH2 or NH: G2 is CH or nitrogen; Rx is chloro, bromo, iodo, or O—S(O)2CF3; Rg is a C1-10alkyl; m is 0, or an integer having a value of 1, or 2; R3 is a C1-10 alkyl, C3-7 cycloalkyl, C3-7 cycloalkyl C1-10 alkyl, aryl, arylC1-10 alkyl, heteroaryl, heteroarylC1-10 alkyl, heterocyclic or a heterocyclylC1-10 alkyl moiety, and wherein each of these moieties may be optionally substituted. which comprises reacting a compound of the formula: wherein Ry is chloro, bromo, iodo, O—S(O)2CF3; and Rg is a C1-10 alkyl; with a olefin forming reagent in a suitable base to yield a compound of Formula (II), or (IIa) wherein m=0 and oxidizing the sulphur as necessary or desired.

    Abstract translation: 本发明涉及一种制备式（II）或（IIa）的2,4,8-三取代吡啶并[2,3-d]嘧啶-7-酮药效团的新方法，其中G1是CH2或NH：G2 是CH或氮; R x是氯，溴，碘或O-S（O）2 C 3 F 3; Rg为C1-10烷基; m为0，或值为1或2的整数; R 3是C 1-10烷基，C 3-7环烷基，C 3-7环烷基C 1-10烷基，芳基，芳基C 1-10烷基，杂芳基，杂芳基C 1-10烷基，杂环基或杂环基C 1-10烷基部分，并且其中 部分可以任选被取代。 其包括使下式化合物：其中R y是氯，溴，碘，O-S（O）2 C 3 F 3; 且R g为C 1-10烷基; 在合适的碱中加入烯烃形成试剂，得到式（II）化合物或其中m = 0的（IIa），并根据需要氧化硫。

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