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    • 4. 发明授权
    • Method for the preparation of pyrido benzoxazine derivatives
    • 吡啶并苯并恶嗪衍生物的制备方法
    • US5952494A
    • 1999-09-14
    • US443884
    • 1995-05-26
    • Youseung KimSoon Bang KangSeonhee Park
    • Youseung KimSoon Bang KangSeonhee Park
    • C07D498/06
    • C07D498/06
    • There is disclosed a method for the preparation of pyrido benzoxazine derivative having the following formula I, that is improved in both production coat and yield.The method comprises reacting a compound of the following general formula II with tetraalkyl ammonium fluoride or with a mixture of tetraalkyl ammonium halide and metal fluoride in an organic solvent at a reaction temperature of about 30 to about 100.degree. C. for 1 to 3 hours under stirring; and reacting the resulting solution with a metal hydroxide or a metal carboxylate dissolved in water or in a mixture of water and alcohol, for 1 to 3 hours under heat. ##STR1## wherein X is a fluorine or chlorine atom and X.sub.1 and X.sub.2 each is a halogen atom or a nitro group, R is an alkyl group containing 1 to 4 carbon atoms and R.sub.1, R.sub.2, R.sub.3 and R.sub.4 each is an alkyd group or allyl group containing 1 to 8 carbon atoms.
    • 公开了制备具有下式I的吡啶并苯并恶嗪衍生物的方法,其在生产涂层和产率方面都得到改善。 该方法包括将下列通式II的化合物与四烷基氟化铵或四烷基卤化铵和金属氟化物的混合物在有机溶剂中在约30至约100℃的反应温度下反应1-3小时, 搅拌 并将所得溶液与溶于水中或在水和醇的混合物中的金属氢氧化物或金属羧酸酯反应1至3小时。 其中X为氟或氯原子,X 1和X 2各自为卤原子或硝基,R为含有1至4个碳原子的烷基,R 1,R 2,R 3和R 4各自为醇酸基或含烯丙基 1至8个碳原子。
    • 5. 发明授权
    • Process for preparation of (-)3(S)-methylbenzoxazine derivative
    • ( - )3(S) - 甲基苯并恶嗪衍生物的制备方法
    • US5756731A
    • 1998-05-26
    • US613299
    • 1996-03-11
    • Youseung KimSoon Bang KangEu Jin Ahn
    • Youseung KimSoon Bang KangEu Jin Ahn
    • B01J23/40B01J23/42B01J23/44C07B43/04C07B53/00C07B55/00C07B61/00C07D265/36
    • C07D265/36
    • A process for preparing (-)3(S)-methylbenzoxazine derivative of formula (I) comprising the steps of reacting the compound of formula (II) with benzoic acid, triphenylphosphine and diethyl azodicarboxylate in an organic solvent to obtain the compound of formula (III); hydrogenating the compound of formula (III) in the presence of a metallic catalyst to provide the compound of formula (IV); hydrolyzing the compound of formula (IV) to give the compound of formula (V); and reacting the compound of formula (V) with diethyl azodicarboxylate, triphenylphosphine, and zinc chloride in an organic solvent. The obtained (-)3(S)-methylbenzoxazine derivative is a useful intermediate for preparing an antibacterial agent which has a potent bacteriocidal effect. ##STR1##
    • 制备式(I)的( - )3(S) - 甲基苯并恶嗪衍生物的方法,包括使式(II)化合物与苯甲酸,三苯基膦和偶氮二羧酸二乙酯在有机溶剂中反应,得到式 III); 在金属催化剂存在下氢化式(III)化合物,得到式(Ⅳ)化合物; 水解式(Ⅳ)化合物,得到式(Ⅴ)化合物; 并在有机溶剂中使式(Ⅴ)化合物与偶氮二羧酸二乙酯,三苯基膦和氯化锌反应。 得到的( - )3(S) - 甲基苯并恶嗪衍生物是制备具有强效杀菌作用的抗菌剂的有用中间体。 (I)(II)(III)(IV)(V)\!