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公开(公告)号:US08436037B2
公开(公告)日:2013-05-07
申请号:US13198739
申请日:2011-08-05
申请人: Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Jones , Paul Bonnett
发明人: Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Jones , Paul Bonnett
IPC分类号: A01N43/56 , C07D231/14
CPC分类号: C07C211/61 , A01N43/56 , C07C205/06 , C07C209/325 , C07C209/70 , C07C2603/66 , C07D231/14
摘要: The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are each independently of the other hydrogen or C1-C5alkyl and R3 is CF3 or CF2H, by a) reaction of a compound of formula II wherein R1 and R2 are as defined for formula I, with at least one reducing agent to form a compound of formula III wherein R1 and R2 are as defined for formula I, and b) reaction of that compound with at least one reducing agent to form a compound of formula IV wherein R1 and R2 are as defined for formula I, and (c) reaction of that compound with a compound of formula V wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C1-C6alkoxy and R3 is as defined for formula I, to form the compound of formula I; and to novel intermediates for use in that process.
摘要翻译: 本发明涉及一种制备式Ⅰ化合物的方法,其中R1和R2分别独立地为氢或C1-C5烷基,R3为CF3或CF2H,通过a)式II化合物与式 R 2如式I所定义,与至少一种还原剂形成式III化合物,其中R 1和R 2如式I所定义,和b)该化合物与至少一种还原剂的反应形成式 式IV其中R1和R2如式I所定义,和(c)该化合物与式V化合物的反应,其中Q是氯,氟,溴,碘,羟基或C 1 -C 6烷氧基,R 3如式 I,形成式I化合物; 以及用于该过程的新型中间体。
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公开(公告)号:US20090163569A1
公开(公告)日:2009-06-25
申请号:US12066683
申请日:2006-09-14
申请人: Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Kevin Jones , Paul Edward Bonnett
发明人: Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Kevin Jones , Paul Edward Bonnett
IPC分类号: A01N43/56 , C07D231/14 , C07C211/45 , C07C205/11 , C07D403/12 , A01P7/00
CPC分类号: C07C211/61 , A01N43/56 , C07C205/06 , C07C209/325 , C07C209/70 , C07C2603/66 , C07D231/14
摘要: The present invention relates to a process for the preparation of compounds of formula (I) wherein R1 and R2 are each independently of the other hydrogen or C1-C5alkyl and R3 is CF3 or CF2H, by a) reaction of a compound of formula (II) wherein R1 and R2 are as defined for formula (I), with at least one reducing agent to form a compound of formula (III) wherein R1 and R2 are as defined for formula (I), and b) reaction of that compound with at least one reducing agent to form a compound of formula (IV) wherein R1 and R2 are as defined for formula (I), and (c) reaction of that compound with a compound of formula (V) wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C1-C6alkoxy and R3 is as defined for formula (I), to form the compound of formula (I); and to novel intermediates for use in that process.
摘要翻译: 本发明涉及制备式(I)化合物的方法,其中R 1和R 2各自独立地为氢或C 1 -C 5烷基,R 3为CF 3或CF 2 H,通过a)式(Ⅱ)化合物 )其中R1和R2如式(I)所定义,与至少一种还原剂形成式(III)化合物,其中R 1和R 2如式(I)所定义,和b)该化合物与 至少一种还原剂形成式(Ⅳ)化合物,其中R1和R2如式(Ⅰ)所定义,和(c)该化合物与式(Ⅴ)化合物的反应其中Q是氯,氟, 溴,碘,羟基或C 1 -C 6烷氧基,R 3如式(I)所定义,形成式(I)化合物; 以及用于该过程的新型中间体。
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公开(公告)号:US07994341B2
公开(公告)日:2011-08-09
申请号:US12066683
申请日:2006-09-14
申请人: Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Kevin Jones , Paul Edward Bonnett
发明人: Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Kevin Jones , Paul Edward Bonnett
IPC分类号: C07D231/14
CPC分类号: C07C211/61 , A01N43/56 , C07C205/06 , C07C209/325 , C07C209/70 , C07C2603/66 , C07D231/14
摘要: The present invention relates to a process for the preparation of compounds of formula (I) wherein R1 and R2 are each independently of the other hydrogen or C1-C5alkyl and R3 is CF3 or CF2H, by a) reaction of a compound of formula (II) wherein R1 and R2 are as defined for formula (I), with at least one reducing agent to form a compound of formula (III) wherein R1 and R2 are as defined for formula (I), and b) reaction of that compound with at least one reducing agent to form a compound of formula (IV) wherein R1 and R2 are as defined for formula (I), and (c) reaction of that compound with a compound of formula (V) wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C1-C6alkoxy and R3 is as defined for formula (I), to form the compound of formula (I); and to novel intermediates for use in that process.
摘要翻译: 本发明涉及制备式(I)化合物的方法,其中R 1和R 2各自独立地为氢或C 1 -C 5烷基,R 3为CF 3或CF 2 H,通过a)式(Ⅱ)化合物 )其中R1和R2如式(I)所定义,与至少一种还原剂形成式(III)化合物,其中R 1和R 2如式(I)所定义,和b)该化合物与 至少一种还原剂形成式(Ⅳ)化合物,其中R1和R2如式(Ⅰ)所定义,和(c)该化合物与式(Ⅴ)化合物的反应其中Q是氯,氟, 溴,碘,羟基或C 1 -C 6烷氧基,R 3如式(I)所定义,形成式(I)化合物; 以及用于该过程的新型中间体。
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公开(公告)号:US20120065239A1
公开(公告)日:2012-03-15
申请号:US13198739
申请日:2011-08-05
申请人: Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Kevin Jones , Paul Edward Bonnett
发明人: Hans Tobler , Harald Walter , Josef Ehrenfreund , Camilla Corsi , Fanny Giordano , Martin Zeller , Gottfried Seifert , Shailesh Shah , Neil George , Ian Kevin Jones , Paul Edward Bonnett
IPC分类号: A01N43/56 , A01P3/00 , C07D231/14
CPC分类号: C07C211/61 , A01N43/56 , C07C205/06 , C07C209/325 , C07C209/70 , C07C2603/66 , C07D231/14
摘要: The present invention relates to a process for the preparation of compounds of formula I wherein R1 and R2 are each independently of the other hydrogen or C1-C5alkyl and R3 is CF3 or CF2H, by a) reaction of a compound of formula II wherein R1 and R2 are as defined for formula I, with at least one reducing agent to form a compound of formula wherein R1 and R2 are as defined for formula I, and b) reaction of that compound with at least one reducing agent to form a compound of formula IV wherein R1 and R2 are as defined for formula I, and (c) reaction of that compound with a compound of formula V wherein Q is chlorine, fluorine, bromine, iodine, hydroxy or C1-C6alkoxy and R3 is as defined for formula I, to form the compound of formula I; and to novel intermediates for use in that process.
摘要翻译: 本发明涉及一种制备式Ⅰ化合物的方法,其中R1和R2分别独立地为氢或C1-C5烷基,R3为CF3或CF2H,通过a)式II化合物的反应其中R 1和 R 2如式I所定义,与至少一种还原剂形成下式化合物,其中R 1和R 2如式I所定义,和b)该化合物与至少一种还原剂的反应形成式 IV其中R1和R2如式I所定义,和(c)该化合物与式V化合物的反应,其中Q是氯,氟,溴,碘,羟基或C 1 -C 6烷氧基,R 3如式I所定义 ,形成式I化合物; 以及用于该过程的新型中间体。
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公开(公告)号:US20090221856A1
公开(公告)日:2009-09-03
申请号:US12096796
申请日:2006-12-11
申请人: Hans Tobler , Harald Walter , Camilla Corsi , Josef Ehrenfreund , Fanny Giordano , Martin Zeller
发明人: Hans Tobler , Harald Walter , Camilla Corsi , Josef Ehrenfreund , Fanny Giordano , Martin Zeller
IPC分类号: C07C211/31
CPC分类号: C07C209/62 , C07B2200/09 , C07C17/23 , C07C17/30 , C07C17/354 , C07C25/22 , C07C25/24 , C07C209/10 , C07C209/70 , C07C211/61 , C07C2603/66 , C07C23/10
摘要: The present invention relates to a novel a process for the preparation of the compound of the general formula (I), wherein R1 and R2 are independently H or C1-6 alkyl, which comprises treating with a reducing agent either a compound of the general formula (II), wherein R1 and R2 have the meanings given for the compound of the formula (I), R3 is H or C1-4alkyl and Ph is phenyl, or a compound of the general formula (III), wherein R1, R2, R3 and Ph have the meanings given for the compound of the formula (II), the reducing agent being effective to cleave the benzyl moiety Ph-CH(R3)— from the benzylamino moiety PhCH(R3)NH— in the compound of the formula (II) or in the compound of the formula (III) to leave an amino group and, in addition, in the case of the compound of the formula (III), to reduce both the 2,3-double bond and the double bond joining the R1R2C— moiety to the 9-position of the benzonorbornene ring to single bonds. It also relates to processes for the preparation of the compounds (II) and (III) and their precursors and to the compounds (II) and (III) themselves and certain of their precursors, which are novel compounds. The compounds (I) are useful for the preparation of various fungicidal heterocyclyl-carboxylic acid benzonorbornen-5-yl-amides.
摘要翻译: 本发明涉及一种制备通式(I)化合物的方法,其中R 1和R 2独立地为H或C 1-6烷基,其包括用还原剂处理通式 (II)化合物,其中R1和R2具有式(I)化合物所给出的含义,R 3是H或C 1-4烷基,Ph是苯基,或通式(III)的化合物,其中R1,R2, R3和Ph具有式(II)化合物所给出的含义,还原剂有效地从式(II)化合物中的苄基氨基部分PhCH(R3)NH-切割苄基部分Ph-CH(R3) (II)化合物或式(III)化合物中,以留下氨基,另外,在式(III)化合物的情况下,为了还原2,3-双键和双键 将R1R2C-部分连接到苯并降冰片烯环的9位到单键。 它还涉及制备化合物(II)和(III)及其前体以及化合物(II)和(III)本身及其某些新型化合物的前体的方法。 化合物(I)可用于制备各种杀真菌性杂环基 - 羧酸苯并降冰片烯-5-基 - 酰胺。
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公开(公告)号:US07781615B2
公开(公告)日:2010-08-24
申请号:US12096796
申请日:2006-12-11
申请人: Hans Tobler , Harald Walter , Camilla Corsi , Josef Ehrenfreund , Fanny Giordano , Martin Zeller
发明人: Hans Tobler , Harald Walter , Camilla Corsi , Josef Ehrenfreund , Fanny Giordano , Martin Zeller
IPC分类号: C07C211/45 , C07C211/48 , C07C209/10 , C07C209/68 , C07C17/266 , C07C25/22
CPC分类号: C07C209/62 , C07B2200/09 , C07C17/23 , C07C17/30 , C07C17/354 , C07C25/22 , C07C25/24 , C07C209/10 , C07C209/70 , C07C211/61 , C07C2603/66 , C07C23/10
摘要: The present invention relates to a novel a process for the preparation of the compound of the general formula (I), wherein R1 and R2 are independently H or C1-6 alkyl, which comprises treating with a reducing agent either a compound of the general formula (II), wherein R1 and R2 have the meanings given for the compound of the formula (I), R3 is H or C1-4alkyl and Ph is phenyl, or a compound of the general formula (III), wherein R1, R2, R3 and Ph have the meanings given for the compound of the formula (II), the reducing agent being effective to cleave the benzyl moiety Ph-CH(R3)— from the benzylamino moiety PhCH(R3)NH— in the compound of the formula (II) or in the compound of the formula (III) to leave an amino group and, in addition, in the case of the compound of the formula (III), to reduce both the 2,3-double bond and the double bond joining the R1R2C— moiety to the 9-position of the benzonorbornene ring to single bonds. It also relates to processes for the preparation of the compounds (II) and (III) and their precursors and to the compounds (II) and (III) themselves and certain of their precursors, which are novel compounds. The compounds (I) are useful for the preparation of various fungicidal heterocyclyl-carboxylic acid benzonorbornen-5-yl-amides.
摘要翻译: 本发明涉及一种制备通式(I)化合物的方法,其中R 1和R 2独立地为H或C 1-6烷基,其包括用还原剂处理通式 (II)化合物,其中R1和R2具有式(I)化合物所给出的含义,R 3是H或C 1-4烷基,Ph是苯基,或通式(III)的化合物,其中R1,R2, R3和Ph具有式(II)化合物所给出的含义,还原剂有效地从式(II)化合物中的苄基氨基部分PhCH(R3)NH-切割苄基部分Ph-CH(R3) (II)化合物或式(III)化合物中,以留下氨基,另外,在式(III)化合物的情况下,为了还原2,3-双键和双键 将R1R2C-部分连接到苯并降冰片烯环的9位到单键。 它还涉及制备化合物(II)和(III)及其前体以及化合物(II)和(III)本身及其某些新型化合物的前体的方法。 化合物(I)可用于制备各种杀真菌性杂环基 - 羧酸苯并降冰片烯-5-基 - 酰胺。
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公开(公告)号:US20100145100A1
公开(公告)日:2010-06-10
申请号:US12443082
申请日:2007-09-26
申请人: Harald Walter , Hans Tobler , Fanny Giordano , Martin Zeller
发明人: Harald Walter , Hans Tobler , Fanny Giordano , Martin Zeller
IPC分类号: C07C209/36
CPC分类号: C07C209/36 , C07C2603/66 , C07C211/61
摘要: The present invention relates to a process for the preparation of syn-enriched 5-amino-9-isopropyl-benzonorbomene in which the ratio of compounds of formula (Ia(syn)) to compounds of formula (Ib(anti)) is from 70:30 to 99:1, which process comprises reacting a compound of formula (Il) in a pressure vessel with hydrogen in the presence of a palladium catalyst and a solvent, at a pressure of at least 2 bar and a temperature of from 00 C to 45° C., to form syn-enriched 5-amino-9-isopropyl-benzonorbomene.
摘要翻译: 本发明涉及制备合成富集的5-氨基-9-异丙基 - 苯并异戊烯的方法,其中式(Ia(顺式))化合物与式(Ib(反))化合物的比例为70 :30至99:1,该方法包括在钯催化剂和溶剂存在下,将压力容器中的式(II)化合物与氢气在至少2巴的压力和0℃的温度下反应 至45℃,以形成合成富集的5-氨基-9-异丙基 - 苯并异戊烯。
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公开(公告)号:US08129560B2
公开(公告)日:2012-03-06
申请号:US12063907
申请日:2006-08-08
申请人: Martin Charles Bowden , Thomas Aitcheson Clark , Fanny Giordano , Beat Jau , Hans-Dieter Schneider , Gottfried Seifert , Martin Zeller , Dominik Faber , Juerg Wiss
发明人: Martin Charles Bowden , Thomas Aitcheson Clark , Fanny Giordano , Beat Jau , Hans-Dieter Schneider , Gottfried Seifert , Martin Zeller , Dominik Faber , Juerg Wiss
IPC分类号: C07C255/37 , C07C231/02 , C07C231/06 , C07C43/23 , C07C213/02
CPC分类号: C07C231/12 , C07C33/46 , C07C59/70 , C07C69/734 , C07C213/02 , C07C235/34 , C07C251/16 , C07C255/37 , C07C315/04 , C07C319/20 , C07C317/46 , C07C323/62
摘要: A process for the preparation of a compound of formula (I), the process comprising: (i) the reaction of a compound of formula (III), with a compound of formula (IV) to give a compound of formula (II), and (ii) the reaction of the compound of formula (II) with a leaving group, to give the compound of formula (I).
摘要翻译: 一种制备式(I)化合物的方法,该方法包括:(i)式(III)化合物与式(IV)化合物的反应,得到式(II)化合物, 和(ii)式(II)化合物与离去基团的反应,得到式(I)化合物。
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公开(公告)号:US20090118532A1
公开(公告)日:2009-05-07
申请号:US12063907
申请日:2006-08-08
申请人: Martin Charles Bowden , Thomas Aitcheson Clark , Fanny Giordano , Beat Jau , Hans-Dieter Schneider , Gottfried Seifert , Martin Zeller , Dominik Faber , Juerg Wiss
发明人: Martin Charles Bowden , Thomas Aitcheson Clark , Fanny Giordano , Beat Jau , Hans-Dieter Schneider , Gottfried Seifert , Martin Zeller , Dominik Faber , Juerg Wiss
IPC分类号: C07C255/37 , C07C231/02 , C07C231/06 , C07C43/23 , C07C213/02
CPC分类号: C07C231/12 , C07C33/46 , C07C59/70 , C07C69/734 , C07C213/02 , C07C235/34 , C07C251/16 , C07C255/37 , C07C315/04 , C07C319/20 , C07C317/46 , C07C323/62
摘要: A process for the preparation of a compound of formula (I) wherein: R is an alkynyl group; R1 is alkyl, alkenyl, alkynyl, cycloalkyl, cycloalkyl-alkyl, phenyl and phenylalkyl, it being possible in turn for all of the receding groups to carry one or more identical or different halogen atoms; alkoxy; alkenyloxy; alkynyloxy; alkoxyalkyl; haloalkoxy; alkylthio; haloalkylthio; alkysulfonyl; formyl; alkanoyl; hydroxy; halogen; cyano; nitro; amino; alkylamino; dialkylamino; carboxyl; alkoxycarbonyl; alkenyloxycarbonyl; or alkynyloxycarbonyl; and n is an integer from 0 to 3, said process comprising: (i) the reaction of a compound of formula (III) wherein R, R1 and n are as hereinbefore defined; m and m′ are independently 0 or 1; when m and m′ are both 0, A is an alkyl, alkenyl or alkynyl group (suitably having up to eight carbon atoms), optionally substituted by one or more groups independently selected from halogen, hydroxy, alkoxy, C1-4 dialkylamino or cyano; when one of m and m′ is 0 and the other is 1, A is an alkanediyl, alkenediyl or alkynediyl group containing at least two carbon atoms (and suitably having up to eight carbon atoms), optionally substituted by one or more groups independently selected from halogen, hydroxy, alkoxy, C1-4 dialkylamino or cyano; when m and m′ are both 1, A is an alkanetriyl, alkenetriyl or alkynetriyl group containing at least three carbon atoms (and suitably having up to eight carbon atoms), optionally substituted by one or more groups independently selected from halogen, hydroxy, alkoxy, C1-4 dialkylamino or cyano; and wherein if the group A contains three or more carbon atoms, one or more of the carbon atoms may each optionally be replaced with an oxygen atom, provided that there is at least one carbon atom between any two oxygen atoms in the molecule, with a compound of formula (IV) to give a compound of formula (II) wherein R, R1 and n are as hereinbefore defined, and (ii) the reaction of a compound of formula (II) with, wherein L is a leaving group, to give the compound of formula (I) as hereinbefore defined, is disclosed.
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公开(公告)号:US07105545B2
公开(公告)日:2006-09-12
申请号:US10472577
申请日:2002-04-02
CPC分类号: C07C327/44 , A01N37/36 , A01N43/08 , A01N43/10 , A01N43/12 , A01N43/30 , A01N43/32 , A01N43/40 , A01N43/54
摘要: The invention relates to N-propargyloxy-phenethyl thioacetic acid amide derivatives of the general formula (I) including the optical isomers thereof and mixtures of such isomers, wherein R1 is hydrogen, alkyl, cycloalkyl or optionally substituted aryl, R2 and R3 are each independently hydrogen or alkyl, R4 is alkyl, alkenyl or alkynyl, R5, R6, R7 and R8 are each independently hydrogen or alkyl, R9 is hydrogen, optionally substituted alkyl, optionally substituted alkenyl or optionally substituted alkynyl, R10 is optionally substituted aryl or optionally substituted heteroaryl, and Z is hydroxy, optionally substituted aryloxy, optionally substituted alkoxy, optionally substituted alkynyloxy, optionally substituted arylthio, optionally substituted alkylthio, optionally substituted alkynylthio, optionally substituted alkylsulfinyl, optionally substituted alkenysulfinyl, optionally substituted alkynylsulfinyl, optionally substituted alkylsulfonyl, optionally substituted alkenylsulfonyl, optionally substituted alkynylsulfonyl or a group —O—CO—R11, —O—CO—O—R11 or —O—CO—CO—O—R11 wherein R11 is hydrogen, optionally substituted alkyl, optionally substituted cycloalkyl, optionally substituted aryl or optionally substituted heteroaryl. These compounds possess useful plant protecting properties and may advantageously be employed in agricultural practice for controlling or preventing the infestation of plants by phytopathogenic microorganisms, especially fungi
摘要翻译: 本发明涉及通式(I)的N-炔丙氧基 - 苯乙基硫代乙酰胺衍生物,其包括其旋光异构体和这些异构体的混合物,其中R 1是氢,烷基,环烷基或任选取代的 芳基,R 2和R 3各自独立地是氢或烷基,R 4是烷基,烯基或炔基,R 5, R 6,R 7,R 8和R 8各自独立地为氢或烷基,R 9为 氢,任选取代的烷基,任选取代的烯基或任选取代的炔基,R 10是任选取代的芳基或任选取代的杂芳基,Z是羟基,任选取代的芳氧基,任选取代的烷氧基,任选取代的炔氧基,任选地 取代的芳硫基,任选取代的烷硫基,任选取代的炔硫基,任选取代的烷基亚磺酰基,任选取代的烯基亚磺酰基,任选的 取代的炔基亚磺酰基,任选取代的烷基磺酰基,任选取代的链烯基磺酰基,任选取代的炔基磺酰基或基团-O-CO-R 11,-O-CO-OR 11或-O- 其中R 11是氢,任选取代的烷基,任选取代的环烷基,任选取代的芳基或任选取代的杂芳基。 这些化合物具有有用的植物保护性质,并且可有利地用于农业实践中以控制或防止由植物病原微生物特别是真菌侵染植物
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