Process for preparing 4,6-dichloro-pyrimidine
    1.
    发明授权
    Process for preparing 4,6-dichloro-pyrimidine 失效
    制备4,6-二氯 - 嘧啶的方法

    公开(公告)号:US6018045A

    公开(公告)日:2000-01-25

    申请号:US875896

    申请日:1997-07-17

    IPC分类号: C07D239/30

    CPC分类号: C07D239/30

    摘要: A process for preparing 4,6-dichloropyrimidine is described, comprising treating 4,6-dihydroxypyrimidine with phosphorus oxychloride in the presence of a saturated hindered amine, the hydrochloride salt of a saturated hindered amine, or an unsaturated 5-membered nitrogen containing ring or a mixture thereof, and, as a first step, directly extracting the 4,6-dichloropyrimidine so formed.

    摘要翻译: PCT No.PCT / GB96 / 00013 Sec。 371日期1997年7月17日 102(e)日期1997年7月17日PCT 1996年1月4日PCT PCT。 公开号WO96 / 23776 日本1996年8月8日描述了制备4,6-二氯嘧啶的方法,包括在饱和受阻胺的存在下,用三氯氧化磷处理4,6-二羟基嘧啶,饱和受阻胺的盐酸盐或不饱和5- 并且作为第一步,直接提取如此形成的4,6-二氯嘧啶。

    Processes for the preparation of azoxystrobin using dabco as a catalyst and novel intermediates used in the processes
    4.
    发明授权
    Processes for the preparation of azoxystrobin using dabco as a catalyst and novel intermediates used in the processes 有权
    使用dabco作为催化剂制备嘧菌酯的方法和用于该方法的新型中间体

    公开(公告)号:US08124761B2

    公开(公告)日:2012-02-28

    申请号:US11912675

    申请日:2006-04-13

    IPC分类号: C07D239/52

    摘要: The present invention relates, inter alia, to a process for preparing a compound of formula (I): which comprises either (a) reacting a compound of formula (II): with 2-cyanophenyl, or a salt thereof, in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane, or (b) reacting a compound of the formula (III): with a compound of the formula (IV): in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane; where W is the methyl (E)-2-(3-methoxy)acrylate group C(CO2CH3)═CHOCH3 or the methyl 2-(3,3-dimethoxy)propanoate group C(CO2CH3)CH(OCH3)2, or a mixture of the two groups. In addition, the present invention relates to a novel precursors of the compound of formula (I) and methods for making them.

    摘要翻译: 本发明尤其涉及制备式(I)化合物的方法:其包括(a)使式(II)化合物与2-氰基苯基或其盐在存在下反应: 0.1〜2摩尔%的1,4-二氮杂双环[2.2.2]辛烷,或(b)使式(III)化合物与式(Ⅳ)化合物反应:在0.1〜 2摩尔%的1,4-二氮杂双环[2.2.2]辛烷; 其中W是(E)-2-(3-甲氧基)丙烯酸甲酯基团C(CO 2 CH 3)= CHOCH 3或2-(3,3-二甲氧基)丙酸甲酯基C(CO 2 CH 3)CH(OCH 3)2,或 混合两组。 此外,本发明涉及式(I)化合物的新型前体及其制备方法。

    Processes For the Preparation of Azoxystrobin Using Dabco as a Catalyst and Novel Intermediates Used in the Processes
    8.
    发明申请
    Processes For the Preparation of Azoxystrobin Using Dabco as a Catalyst and Novel Intermediates Used in the Processes 有权
    使用Dabco作为催化剂和用于工艺的新型中间体制备嘧菌酯的方法

    公开(公告)号:US20080214587A1

    公开(公告)日:2008-09-04

    申请号:US11912675

    申请日:2006-04-13

    摘要: The present invention relates, inter alia, to a process for preparing a compound of formula (I): which comprises either (a) reacting a compound of formula (II): with 2-cyanophenyl, or a salt thereof, in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane, or (b) reacting a compound of the formula (III): with a compound of the formula (IV): in the presence of between 0.1 and 2 mol % of 1,4-diazabicyclo[2.2.2]octane; where W is the methyl (E)-2-(3-methoxy)acrylate group C(CO2CH3)═CHOCH3 or the methyl 2-(3,3-dimethoxy)propanoate group C(CO2CH3)CH(OCH3)2, or a mixture of the two groups. In addition, the present invention relates to a novel precursors of the compound of formula (I) and methods for making them.

    摘要翻译: 本发明尤其涉及制备式(I)化合物的方法:其包括(a)使式(II)化合物与2-氰基苯基或其盐在存在下反应: 0.1〜2摩尔%的1,4-二氮杂双环[2.2.2]辛烷,或(b)使式(III)化合物与式(Ⅳ)化合物反应:在0.1〜 2摩尔%的1,4-二氮杂双环[2.2.2]辛烷; 其中W是(E)-2-(3-甲氧基)丙烯酸甲酯基团C(CO 2 CH 3 CH 3) - CHOCH 3或 2-(3,3-二甲氧基)丙酸甲酯基C(CO 2 CH 3 CH 3)CH(OCH 3 3)2 或两组的混合物。 此外,本发明涉及式(I)化合物的新型前体及其制备方法。

    Trisubstituted phenyl derivatives and processes for their preparation
    10.
    发明授权
    Trisubstituted phenyl derivatives and processes for their preparation 失效
    三取代苯基衍生物及其制备方法

    公开(公告)号:US5866593A

    公开(公告)日:1999-02-02

    申请号:US964041

    申请日:1997-11-04

    CPC分类号: C07D413/10

    摘要: Compounds of the general formula (1) ##STR1## are described wherein Y is halogen or --OR.sup.1, where R.sup.1 is optionally substituted alkyl; X is --O--, --S-- or --N(R.sup.8)-, where R.sup.8 is hydrogen or alkyl; R.sup.2 is optionally substituted alkyl, alkenyl, cycloalkyl or cycloalkenyl; R.sup.3 is hydrogen, halogen or --OR.sup.9, where R.sup.9 is hydrogen or optionally substituted alkyl, alkenyl, alkoxyalkyl, or alkanoyl, or formyl, carboxamido or thiocarboxamido; R.sup.4 is --(CH.sub.2).sub.n Ar, where Ar is monocyclic or bicyclic aryl optionally containing one or more heteroatoms selected from oxygen, sulfur and nitrogen atoms, wherein Ar is substituted by an optionally substituted C.sub.3-9 cycloaliphatic group optionally containing one or more heteroatoms selected from oxygen, sulphur or --N(R.sup.8)-, and n is zero or an integer 1, 2 or 3; R.sup.5 is --(CH.sub.2).sub.n Ar' where Ar' is monocyclic or bicyclic aryl optionally containing one or more heteroatoms selected from oxygen, sulfur or nitrogen atoms or is Ar; R.sup.6 is hydrogen or optionally substituted alkyl; and R.sup.7 is hydrogen or optionally substituted alkyl; or a salt, solvate or hydrate thereof. Compounds according to the invention are potent and selective phosphodiesterase type IV inhibitors and are useful in the prophylaxis and treatment of diseases such as asthma where an unwanted inflammatory response or muscular spasm is present.

    摘要翻译: 描述通式(1)的化合物(1)其中Y是卤素或-OR 1,其中R 1是任选取代的烷基; X是-O - , - S-或-N(R 8) - ,其中R 8是氢或烷基; R2是任选取代的烷基,烯基,环烷基或环烯基; R3是氢,卤素或-OR9,其中R9是氢或任选取代的烷基,烯基,烷氧基烷基或烷酰基,或甲酰基,甲酰胺基或硫代羧酰胺基; R4是 - (CH2)nAr,其中Ar是任选地含有一个或多个选自氧,硫和氮原子的杂原子的单环或双环芳基,其中Ar被任选地含有一个或多个选自以下的杂原子的任选取代的C3-9环脂族基团取代: 氧,硫或-N(R8) - ,n为零或整数1,2或3; R5是 - (CH2)nAr',其中Ar'是任选含有一个或多个选自氧,硫或氮原子的杂原子的单环或二环芳基或Ar; R6是氢或任选取代的烷基; 并且R 7是氢或任选取代的烷基; 或其盐,溶剂合物或水合物。 根据本发明的化合物是有效和选择性的磷酸二酯酶IV型抑制剂,并且可用于预防和治疗诸如哮喘的疾病,其中存在不想要的炎症反应或肌肉痉挛。