Process for the manufacture of fluoromethoxymalonic acid derivatives
    2.
    发明申请
    Process for the manufacture of fluoromethoxymalonic acid derivatives 审中-公开
    氟代甲氧基丙二酸衍生物的制备方法

    公开(公告)号:US20130317251A1

    公开(公告)日:2013-11-28

    申请号:US13984179

    申请日:2012-02-07

    IPC分类号: C07C67/287 C07C41/01

    摘要: Process for the manufacture of a compound of formula R1OOC—CH(OCH2F)—COOR, (I) or R3HNOC—CH(OCH2F)—CONHR4(II) wherein R1, R2, R3, R4 are equal or different from each other and are independently selected from H; an alkyl group having from 1 to 10 carbon atoms which is optionally substituted by at least one halogen atom; an aralkyl group; or an aryl group, comprising reacting a compound of formula R1OOC—CH(OCH2X)—COOR2 (III) or R3HNOC—CH(OCH2X)—CONHR4(IV) wherein X is a leaving group that can be substituted by nucleophilic substitution, and wherein R1, R2, R3, R4 have the same meaning as above, with at least one source of nucleophilic fluorine.

    摘要翻译: 制备式R1OOC-CH(OCH2F)-COOR,(I)或R3HNOC-CH(OCH2F)-CONHR4(Ⅱ)化合物的方法,其中R 1,R 2,R 3,R 4彼此相同或不同,为 独立地选自H; 任选被至少一个卤素原子取代的具有1至10个碳原子的烷基; 芳烷基; 包括使式R 1 OOC-CH(OCH 2 X)-COOR 2(III)或R 3 HNOC-CH(OCH 2 X)-CONHR 4(IV)的化合物与其中X是可被亲核取代取代的离去基团反应,其中 R1,R2,R3,R4具有与上述相同的含义,至少有一个亲核氟源。

    Process for the preparation of esters of 4-fluorosubstituted 3-oxo-alcanoic acids
    3.
    发明申请
    Process for the preparation of esters of 4-fluorosubstituted 3-oxo-alcanoic acids 有权
    制备4-氟取代的3-氧代 - 丙酸的酯的方法

    公开(公告)号:US20110301378A1

    公开(公告)日:2011-12-08

    申请号:US12673030

    申请日:2008-08-14

    申请人: Max Josef Braun

    发明人: Max Josef Braun

    IPC分类号: C07C67/30

    摘要: Esters of 4-fluorosubstituted 3-oxo-alcanoic acids can be prepared by addition reaction of ketene with the respective acid chloride, subsequent esterification and hydrodechlorination. Preferred reaction products are esters of 4,4-difluoro-3-oxo-butanoic acid.

    摘要翻译: 4-氟取代的3-氧代 - 丙酸的酯可以通过乙烯酮与各自的酰氯的加成反应制备,随后进行酯化和加氢脱氯。 优选的反应产物是4,4-二氟-3-氧代 - 丁酸的酯。

    Process for the manufacture of Sevoflurane
    4.
    发明授权
    Process for the manufacture of Sevoflurane 有权
    制造七氟烷的方法

    公开(公告)号:US08987524B2

    公开(公告)日:2015-03-24

    申请号:US13389449

    申请日:2010-08-10

    申请人: Max Josef Braun

    发明人: Max Josef Braun

    摘要: A process for the manufacture of Sevoflurane CF3—CH(OCH2F)—CF3 which comprises (a) manufacturing a substituted malonic acid derivative of formula (I): R1OOC—CH(OCH2X)—COOR2 or of formula (II): R3HNOC—CH(OCH2X)—CONHR4, wherein X is OH or a leaving group which can be substituted by nucleophilic substitution and wherein R1, R2 R3, R4, equal to or different from each other, are independently selected from the group consisting of H, an alkyl group having from 1 to 10 carbon atoms which is optionally substituted by at least one halogen atom, an aralkyl group, and an aryl group; and (b) further reacting said malonic acid derivative as intermediate for the manufacture of Sevoflurane CF3—CH(OCH2F)—CF3.

    摘要翻译: 制备七氟烷CF 3 -CH(OCH 2 F)-CF 3的方法,其包括(a)制备式(I)的取代的丙二酸衍生物:R1OOC-CH(OCH2X)-COOR2或式(II):R3HNOC-CH (OCH 2 X)-CONHR 4,其中X是OH或可以被亲核取代取代的离去基团,并且其中R 1,R 2,R 3,R 4彼此相同或不同,独立地选自H,烷基 具有1至10个碳原子的基团,其任选被至少一个卤素原子,芳烷基和芳基取代; 和(b)进一步使所述丙二酸衍生物作为制备七氟醚CF 3 -CH(OCH 2 F)-CF 3的中间体。

    Process for the preparation of esters of 1-substituted-3-fluoroalkyl-pyrazole-4-carboxylic acids
    5.
    发明授权
    Process for the preparation of esters of 1-substituted-3-fluoroalkyl-pyrazole-4-carboxylic acids 有权
    制备1-取代-3-氟烷基 - 吡唑-4-羧酸酯的方法

    公开(公告)号:US08981116B2

    公开(公告)日:2015-03-17

    申请号:US13810626

    申请日:2011-07-22

    IPC分类号: C07D231/14

    CPC分类号: C07D231/14

    摘要: A process for the manufacture of an ester or the respective free acid of a 1-substituted-3-fluoroalkyl-pyrazole-4-carboxylic acid of formula (I), wherein in such formula (I), Y is H, F or an alkyl group having from 1 to 12 carbon atoms which is optionally substituted by at least one halogen atom, an aralkyl group or an aryl group; R1 is H or an organic residue; R2 is H or an organic residue. Such process comprises submitting a compound of formula (II) to a reduction reaction, wherein in such formula (II), Y is the same as defined for formula (I); X is Cl, Br or I; R1′ is H or an organic residue; and R2′ is H or an organic residue.

    摘要翻译: 制备式(I)的1-取代-3-氟烷基 - 吡唑-4-羧酸的酯或各自的游离酸的方法,其中在该式(I)中,Y是H,F或 任选被至少一个卤素原子,芳烷基或芳基取代的具有1至12个碳原子的烷基; R1是H或有机残基; R2是H或有机残基。 这种方法包括将式(II)化合物与还原反应进行反应,其中在式(II)中,Y与式(I)中定义相同; X是Cl,Br或I; R1'是H或有机残基; R2'是H或有机残基。

    Process for the preparation of esters of 4-fluorosubstituted 3-oxo-alcanoic acids
    6.
    发明授权
    Process for the preparation of esters of 4-fluorosubstituted 3-oxo-alcanoic acids 有权
    制备4-氟取代的3-氧代 - 丙酸的酯的方法

    公开(公告)号:US08481778B2

    公开(公告)日:2013-07-09

    申请号:US12673030

    申请日:2008-08-14

    申请人: Max Josef Braun

    发明人: Max Josef Braun

    IPC分类号: C07C69/66

    摘要: Esters of 4-fluorosubstituted 3-oxo-alcanoic acids can be prepared by addition reaction of ketene with the respective acid chloride, subsequent esterification and hydrodechlorination. Preferred reaction products are esters of 4,4-difluoro-3-oxo-butanoic acid.

    摘要翻译: 4-氟取代的3-氧代 - 丙酸的酯可以通过乙烯酮与各自的酰氯的加成反应制备,随后进行酯化和加氢脱氯。 优选的反应产物是4,4-二氟-3-氧代 - 丁酸的酯。

    Process for the preparation of pyrazole-4-carboxamides
    8.
    发明授权
    Process for the preparation of pyrazole-4-carboxamides 有权
    制备吡唑-4-甲酰胺的方法

    公开(公告)号:US08987470B2

    公开(公告)日:2015-03-24

    申请号:US13881366

    申请日:2011-10-25

    申请人: Max Josef Braun

    发明人: Max Josef Braun

    IPC分类号: C07D231/14

    CPC分类号: C07D231/14

    摘要: A process for the manufacture of pyrazole-4-carboxamides, in particular, of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxamides which are useful as pharmaceuticals and agrochemicals. The carboxamides are prepared from the corresponding pyzole-4-carboxylic acid esters and appropriate amine in the presence of a base. The reaction is performed in a reaction medium which is essentially free of water; alternatively, the base is used in an amount equal to or greater than 0.25 equivalents per mole of amine.

    摘要翻译: 用于制备吡唑-4-甲酰胺的方法,特别是用作药物和农用化学品的3-二氟甲基-1-甲基-1H-吡唑-4-甲酰胺。 羧酰胺由相应的吡唑-4-羧酸酯和适当的胺在碱的存在下制备。 反应在基本上不含水的反应介质中进行; 或者,碱的使用量相当于每摩尔胺等于或大于0.25当量。

    Process for the preparation of pyrazole-4-carboxamides
    9.
    发明申请
    Process for the preparation of pyrazole-4-carboxamides 有权
    制备吡唑-4-甲酰胺的方法

    公开(公告)号:US20130225833A1

    公开(公告)日:2013-08-29

    申请号:US13881366

    申请日:2011-10-25

    申请人: Max Josef Braun

    发明人: Max Josef Braun

    IPC分类号: C07D231/14

    CPC分类号: C07D231/14

    摘要: A process for the manufacture of pyrazole-4-carboxamides, in particular, of 3-difluoromethyl-1-methyl-1H-pyrazole-4-carboxamides which are useful as pharmaceuticals and agrochemicals. The carboxamides are prepared from the corresponding pyrazole-4-carboxylic acid esters and appropriate amine in the presence of a base. The reaction is performed in a reaction medium which is essentially free of water; alternatively, the base is used in an amount equal to or greater than 0.25 equivalents per mole of amine.

    摘要翻译: 用于制备吡唑-4-甲酰胺的方法,特别是用作药物和农用化学品的3-二氟甲基-1-甲基-1H-吡唑-4-甲酰胺。 甲酰胺由相应的吡唑-4-羧酸酯和适当的胺在碱的存在下制备。 反应在基本上不含水的反应介质中进行; 或者,碱的使用量相当于每摩尔胺等于或大于0.25当量。

    Process for the preparation of esters of 1-substituted-3-fluoroalkyl-pyrazole-4-carboxylic acids
    10.
    发明申请
    Process for the preparation of esters of 1-substituted-3-fluoroalkyl-pyrazole-4-carboxylic acids 有权
    制备1-取代-3-氟烷基 - 吡唑-4-羧酸酯的方法

    公开(公告)号:US20130123510A1

    公开(公告)日:2013-05-16

    申请号:US13810626

    申请日:2011-07-22

    IPC分类号: C07D231/14

    CPC分类号: C07D231/14

    摘要: A process for the manufacture of an ester or the respective free acid of a 1-substituted-3-fluoroalkyl-pyrazole-4-carboxylic acid of formula (I), wherein in such formula (I), Y is H, F or an alkyl group having from 1 to 12 carbon atoms which is optionally substituted by at least one halogen atom, an aralkyl group or an aryl group; R1 is H or an organic residue; R2 is H or an organic residue. Such process comprises submitting a compound of formula (II) to a reduction reaction, wherein in such formula (II), Y is the same as defined for formula (I); X is Cl, Br or I; R1′ is H or an organic residue; and R2′ is H or an organic residue.

    摘要翻译: 制备式(I)的1-取代-3-氟烷基 - 吡唑-4-羧酸的酯或各自的游离酸的方法,其中在该式(I)中,Y是H,F或 任选被至少一个卤素原子,芳烷基或芳基取代的具有1至12个碳原子的烷基; R1是H或有机残基; R2是H或有机残基。 这种方法包括将式(II)化合物与还原反应进行反应,其中在式(II)中,Y与式(I)中定义相同; X是Cl,Br或I; R1'是H或有机残基; R2'是H或有机残基。