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    • 2. 发明授权
    • Process for producing quinazoline derivatives
    • 喹唑啉衍生物的制备方法
    • US6001831A
    • 1999-12-14
    • US29723
    • 1998-05-22
    • Theodor PapenfuhsRalf PfirmannStefan KrauseDoris Neumann-Grimm
    • Theodor PapenfuhsRalf PfirmannStefan KrauseDoris Neumann-Grimm
    • C07D239/96A01N43/66C07D241/36
    • C07D239/96
    • A process for producing 1,2,3,4-tetrahydro-2,4-dioxo-quinazoline-1-yl acetic acid derivatives of the formula (I) in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are mutually independently hydrogen, halogen, OH, NO.sub.2, (C.sub.1 -C.sub.6) alkoxy, (C.sub.1 -C.sub.6) alkyl, halogen-substituted (C.sub.1 -C.sub.6) alkyl, R.sup.5 is hydrogen, (C.sub.1 -C.sub.6) alkyl, phenyl where the alkyl or phenyl radical may also be substituted by halogen atoms; in which an anthranilic acid derivative of formula (II), in which R.sup.1 to R.sup.5 have the above meaning and R.sup.6 is hydrogen, (C.sub.1 -C.sub.6) alkyl or phenyl, where the alkyl or phenyl radical may also be substituted by halogen atoms, is reacted with a metal cyanate and hydrogen chloride in the presence of an inert solvent. ##STR1##
    • PCT No.PCT / EP96 / 03632 Sec。 371日期:1998年5月22日 102(e)日期1998年5月22日PCT提交1996年8月19日PCT公布。 出版物WO97 / 08154 日期1997年3月6日制备式(I)的1,2,3,4-四氢-2,4-二氧代喹唑啉-1-基乙酸衍生物的方法,其中R 1,R 2,R 3和R 4相互 独立地是氢,卤素,OH,NO2,(C1-C6)烷氧基,(C1-C6)烷基,卤素取代的(C1-C6)烷基,R5是氢,(C1-C6)烷基,苯基,其中烷基或苯基 自由基也可以被卤素原子取代; 其中式(II)的邻氨基苯甲酸衍生物,其中R1至R5具有上述含义,R6为氢,(C1-C6)烷基或苯基,其中烷基或苯基也可被卤素原子取代, 在惰性溶剂存在下与金属氰酸盐和氯化氢反应。
    • 5. 发明授权
    • Process for the preparation of N-carboxymethyleneanthranilic acid
    • 制备N-羧基亚甲基邻氨基苯甲酸的方法
    • US5811572A
    • 1998-09-22
    • US797599
    • 1997-02-07
    • Theodor PapenfuhsAndreas DierdorfStefan KrauseDoris Neumann-Grimm
    • Theodor PapenfuhsAndreas DierdorfStefan KrauseDoris Neumann-Grimm
    • B01J23/40C07B61/00C07C227/08C07C227/18C07C229/56C07C229/00
    • C07C227/18C07C227/08C07C229/56
    • Process for the preparation of N-carboxymethyleneanthranilic acid esters of the formula (3) ##STR1## by reacting a compound of the formula (1) ##STR2## in which R' is hydrogen or a straight-chain or branched alkyl radical having 1 to 4 carbon atoms and R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are identical or different and independently of one another are hydrogen, halogen, NO.sub.2, a straight-chain or branched alkyl, alkoxy or halogenated alkyl radical having in each case 1 to 6 carbon atoms, with a glyoxylic acid ester of the formula (2) OHC--COOR (2) in which R is a straight-chain or branched alkyl radical having 1 to 20 carbon atoms, phenyl radical or benzyl radical, which are unsubstituted or mono- or polysubstituted by halogen or an alkyl or alkoxy group having in each case 1 to 4 carbon atoms, in the presence of a solvent at 0.degree. to 200.degree. C., optionally separating off the water formed during the reaction, and reducing the reaction product with hydrogen in the presence of a hydrogenation catalyst at a temperature of 0.degree. to 200.degree. C. under a pressure of 1 to 150 bar.
    • 通过使式(1)的化合物(1)其中R'是氢或直链的式(1)化合物或其制备方法制备式(3)的N-羧基亚甲基邻氨基苯甲酸酯的方法 具有1至4个碳原子的支链烷基和R 1,R 2,R 3和R 4相同或不同,彼此独立地为氢,卤素,NO 2,直链或支链烷基,烷氧基或卤代烷基,其各自为 具有式(2)的乙醛酸酯,其中R是具有1至20个碳原子的直链或支链烷基,其中R为直链或支链的烷基,苯基或苄基,其为 在0〜200℃下,在溶剂存在下,卤素或具有1〜4个碳原子的烷基或烷氧基单取代或多取代,任选地分离反应中形成的水​​,以及 在氢化催化剂a存在下,用氢还原反应产物 在0〜200℃的温度下,在1〜150巴的压力下进行。