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公开(公告)号:US5763481A
公开(公告)日:1998-06-09
申请号:US678002
申请日:1996-07-10
IPC分类号: A01C1/00 , A01N37/18 , A01N37/22 , A01N37/24 , A01N41/06 , A01N41/10 , A01N55/00 , A01N55/10 , C07C51/38 , C07C57/52 , C07C57/76 , C07C69/63 , C07C69/65 , C07C233/09 , C07C233/12 , C07C233/33 , C07C233/55 , C07C237/42 , C07C255/60 , C07C311/46 , C07C317/38 , C07C317/40 , C07C323/37 , C07C323/41 , C07D213/70 , C07D239/38 , C07D291/00 , C07D295/16 , C07D295/192 , C07F7/08 , C07F7/12 , C07F7/18
CPC分类号: C07D295/192 , A01N37/22 , A01N37/24 , A01N41/06 , A01N41/10 , A01N55/00 , C07C233/09 , C07C233/33 , C07C233/55 , C07C237/42 , C07C255/60 , C07C311/46 , C07C317/40 , C07C323/41 , C07C51/38 , C07C57/52 , C07C69/63 , C07C69/65 , C07F7/0818 , C07F7/184 , C07C2101/02 , C07C2101/14 , C07C2101/18
摘要: Compounds of the formula ##STR1## wherein R.sub.1 is C.sub.3 -C.sub.8 cycloalkyl, halo-C.sub.3 -C.sub.8 cycloalkyl, C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, halo-C.sub.3 -C.sub.8 cycloalkyl-C.sub.1 -C.sub.6 alkyl, --Si(R.sub.3).sub.3, --S--R.sub.4, --SO.sub.2 --R.sub.6 or --CO--R.sub.9 ;R.sub.2 is halogen, C.sub.1 -C.sub.4 alkyl or CF.sub.3, the substituents R.sub.2 being identical or different when n is 2; R.sub.3 each independently of the others is C.sub.1 -C.sub.6 alkyl, halo-C.sub.1 -C.sub.6 alkyl, C.sub.1 -C.sub.6 alkoxy or phenyl; R.sub.4 is aryl or heteroaryl each of which is unsubstituted or substituted; R.sub.6 is unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.1 -C.sub.20 -alkoxy, C.sub.2 -C.sub.6 alkenyloxy, C.sub.2 -C.sub.6 alkynyloxy, C.sub.1 -C.sub.4 alkylthio, aryl, aryloxy or arylthio, or is optionally substituted amino; R.sub.9 is hydroxy, unsubstituted or substituted C.sub.1 -C.sub.10 alkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.3 -C.sub.8 cycloalkyl, aryl or aryloxy, or is optionally substituted amino; R.sub.12 is hydrogen or unsubstituted or substituted C.sub.1 -C.sub.10 alkyl; m is 1,3,5,7,9 or 11; n is 0,1 or 2; X is fluorine or chlorine; and Y is hydrogen, fluorine or methyl; ps in free form or in salt form, can be used as pesticides and can be prepared in a manner known per se.
摘要翻译: 式(I)的化合物,其中R 1是C 3 -C 8环烷基,卤代-C 3 -C 8环烷基,C 3 -C 8环烷基-C 1 -C 6烷基,卤代-C 3 -C 8环烷基-C 1 -C 6烷基,-Si(R 3)3,-S -R4,-SO2-R6或-CO-R9; R2是卤素,C1-C4烷基或CF3,当n为2时,取代基R2相同或不同; R 3各自独立地为C 1 -C 6烷基,卤代-C 1 -C 6烷基,C 1 -C 6烷氧基或苯基; R4是芳基或杂芳基,其各自为未取代或取代的; R 6是未取代的或取代的C 1 -C 10烷基,C 2 -C 6烯基,C 2 -C 6炔基,C 1 -C 20烷氧基,C 2 -C 6烯氧基,C 2 -C 6炔氧基,C 1 -C 4烷硫基,芳基,芳氧基或芳硫基,或任选取代的氨基; R 9为羟基,未取代或取代的C 1 -C 10烷基,C 2 -C 6烯基,C 2 -C 6炔基,C 3 -C 8环烷基,芳基或芳氧基,或任选取代的氨基; R 12是氢或未取代的或取代的C 1 -C 10烷基; m为1,3,5,7,9或11; n为0,1或2; X是氟或氯; Y为氢,氟或甲基; ps为游离形式或盐形式,可用作农药,可以以本身已知的方式制备。
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公开(公告)号:US5358957A
公开(公告)日:1994-10-25
申请号:US116156
申请日:1993-09-02
申请人: Peter Maienfisch , Manfred Boger , Thomas Pitterna
发明人: Peter Maienfisch , Manfred Boger , Thomas Pitterna
IPC分类号: A01N37/18 , A01N43/40 , A01N43/42 , A01N43/46 , A01N43/54 , A01N43/60 , A01N43/653 , A01N43/74 , A01N43/80 , A01N43/82 , A01N43/88 , A61K31/16 , C07C67/08 , C07C69/63 , C07C233/15 , C07D211/20 , C07D211/26 , C07D213/75 , C07D215/20 , C07D215/36 , C07D215/38 , C07D217/22 , C07D223/10 , C07D223/12 , C07D239/42 , C07D241/20 , C07D249/14 , C07D261/14 , C07D263/58 , C07D277/20 , C07D277/46 , C07D277/48 , C07D277/58 , C07D277/82 , C07D285/06 , C07D285/08 , C07D285/10 , C07D285/12 , C07D285/125 , C07D285/13 , C07D285/135 , C07D285/14 , C07D285/16 , C07D307/33 , C07D311/08 , C07D319/18 , C07D413/04 , A61K31/425 , A61K31/44 , C07D277/34 , C07D277/38
CPC分类号: C07D213/75 , A01N43/40 , A01N43/42 , A01N43/46 , A01N43/54 , A01N43/60 , A01N43/653 , A01N43/74 , A01N43/80 , A01N43/82 , A01N43/88 , C07D215/38 , C07D223/12 , C07D239/42 , C07D241/20 , C07D249/14 , C07D261/14 , C07D263/58 , C07D277/46 , C07D277/58 , C07D277/82 , C07D285/135 , C07D285/16 , C07D307/33 , C07D413/04
摘要: Compounds of the formula ##STR1## wherein A is a substituted or unsubstituted, aromatic or non-aromatic, monocyclic or bicyclic, heterocyclic radical that is bonded by way of a carbon atom to X; each of R.sub.1 and R.sub.2, independently of the other, is hydrogen or C.sub.1 -C.sub.6 alkyl; X is NR.sub.3, 0 or S; and R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl, in free form or in salt form, can be used as agrochemical active ingredients and can be prepared in a manner known per se.
摘要翻译: 式(I)的化合物,其中A是通过碳原子与X键合的取代或未取代的芳族或非芳族单环或双环杂环基; R 1和R 2各自独立地为氢或C 1 -C 6烷基; X为NR3,0或S; 和R 3为氢或C 1 -C 4烷基,为游离形式或盐形式,可用作农业化学活性成分,并且可以以本身已知的方式制备。
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公开(公告)号:US5439908A
公开(公告)日:1995-08-08
申请号:US969628
申请日:1992-10-30
申请人: Peter Maienfisch , Manfred Boger , Thomas Pitterna
发明人: Peter Maienfisch , Manfred Boger , Thomas Pitterna
IPC分类号: A01N37/18 , A01N43/40 , A01N43/42 , A01N43/46 , A01N43/54 , A01N43/60 , A01N43/653 , A01N43/74 , A01N43/80 , A01N43/82 , A01N43/88 , A61K31/16 , C07C67/08 , C07C69/63 , C07C233/15 , C07D211/20 , C07D211/26 , C07D213/75 , C07D215/20 , C07D215/36 , C07D215/38 , C07D217/22 , C07D223/10 , C07D223/12 , C07D239/42 , C07D241/20 , C07D249/14 , C07D261/14 , C07D263/58 , C07D277/20 , C07D277/46 , C07D277/48 , C07D277/58 , C07D277/82 , C07D285/06 , C07D285/08 , C07D285/10 , C07D285/12 , C07D285/125 , C07D285/13 , C07D285/135 , C07D285/14 , C07D285/16 , C07D307/33 , C07D311/08 , C07D319/18 , C07D413/04 , A61K31/50 , A61K31/495 , A61K31/505 , C07D237/14 , C07D237/18 , C07D237/20 , C07D239/32 , C07D241/18
CPC分类号: C07D213/75 , A01N43/40 , A01N43/42 , A01N43/46 , A01N43/54 , A01N43/60 , A01N43/653 , A01N43/74 , A01N43/80 , A01N43/82 , A01N43/88 , C07D215/38 , C07D223/12 , C07D239/42 , C07D241/20 , C07D249/14 , C07D261/14 , C07D263/58 , C07D277/46 , C07D277/58 , C07D277/82 , C07D285/135 , C07D285/16 , C07D307/33 , C07D413/04
摘要: Compounds of the formula ##STR1## wherein A is a substituted or unsubstituted, aromatic or non-aromatic, monocyclic or bicyclic, heterocyclic radical that is bonded by way of a carbon atom to X; each of R.sub.1 and R.sub.2, independently of the other, is hydrogen or C.sub.1 -C.sub.6 alkyl; X is NR.sub.3, O or S; and R.sub.3 is hydrogen or C.sub.1 -C.sub.4 alkyl, in free form or in salt form, can be used as agrochemical active ingredients and can be prepared in a manner known per se.
摘要翻译: 式(I)的化合物,其中A是通过碳原子与X键合的取代或未取代的芳族或非芳族单环或双环杂环基; R 1和R 2各自独立地为氢或C 1 -C 6烷基; X是NR 3,O或S; 和R 3为氢或C 1 -C 4烷基,为游离形式或盐形式,可用作农业化学活性成分,并且可以以本身已知的方式制备。
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公开(公告)号:US5481013A
公开(公告)日:1996-01-02
申请号:US81598
申请日:1993-06-23
申请人: Peter Maienfisch , Thomas Pitterna , Manfred Boger
发明人: Peter Maienfisch , Thomas Pitterna , Manfred Boger
IPC分类号: A01N37/06 , A01N37/12 , A01N37/18 , A01N37/20 , A01N37/38 , A01N43/40 , A01N43/82 , C07C67/08 , C07C67/14 , C07C69/63 , C07C69/65 , C07C69/773 , C07C69/96 , C07C205/34 , C07C255/54 , C07C271/58 , C07C323/20 , C07D213/26 , C07D213/30 , C07D213/61 , C07D213/64 , C07D213/643 , C07D257/04 , C07D285/08 , C07D285/12 , C07D285/13 , C07D291/02 , C07D317/54 , C07D333/32 , C07C69/62
CPC分类号: C07D213/30 , A01N37/12 , A01N37/20 , A01N37/38 , A01N43/40 , A01N43/82 , C07C205/34 , C07C255/54 , C07C271/58 , C07C323/20 , C07C69/65 , C07C69/96 , C07D213/643 , C07D285/08
摘要: Compounds of the formula ##STR1## in which A is oxygen, sulfur or --NR.sub.1 --;B is C.sub.2 -C.sub.6 alkylene,D-E is --O--E, --S--E, --O--CH.sub.2 --E, --O--C(.dbd.O)--E, --O--C(.dbd.O)--O--E, --O--C(.dbd.O)--N(H)--E or --O--C(.dbd.S)--N(H)--E;E is phenyl; phenyl which is substituted by one to three substituents; a five-membered aromatic heterocycle having one to three hetero atoms; a five-membered aromatic heterocycle which has one to three hetero atoms and which is substituted by one or two substituents; a six-membered aromatic heterocycle which has one to three nitrogen atoms; or a six-membered aromatic heterocycle which has one to three nitrogen atoms and which is substituted by one or two substituents;L is halogen or methyl;X is fluorine;Y is chlorine or fluorine;Z is hydrogen, fluorine or methyl;m is the number zero, one, two, three, four or five;n is the number zero, one or two andR.sub.1 is hydrogen, C.sub.1 -C.sub.4 alkyl, phenylthio or tolylthio, in free form or in salt form, can be used as pesticides and can be prepared in a manner known per se.
摘要翻译: 式(I)的化合物,其中A是氧,硫或-NR 1; B为C2-C6亚烷基,DE为-OE,-SE,-O-CH2-E,-OC(= O)-E,-OC(= O)-OE,-OC(= O)-N(H) -E或-OC(= S)-N(H)-E; E是苯基; 被一至三个取代基取代的苯基; 具有1至3个杂原子的5元芳族杂环; 具有一至三个杂原子并被一个或两个取代基取代的五元芳族杂环; 具有一至三个氮原子的六元芳族杂环; 或具有一至三个氮原子并被一个或两个取代基取代的六元芳族杂环; L是卤素或甲基; X是氟; Y是氯或氟; Z是氢,氟或甲基; m是数字零,一,二,三,四或五; n为0,1或2,R 1为氢,C 1 -C 4烷基,苯硫基或甲硫基,为游离形式或盐形式,可用作农药,可以以本身已知的方式制备。
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公开(公告)号:US20090198054A1
公开(公告)日:2009-08-06
申请号:US12424594
申请日:2009-04-16
申请人: Thomas Pitterna , Henry Szczepanski , Peter Maienfisch , Ottmar Franz Huter , Thomas Rapold , Marcel Senn , Thomas Gobel , Anthony Cornelius O'Sullivan
发明人: Thomas Pitterna , Henry Szczepanski , Peter Maienfisch , Ottmar Franz Huter , Thomas Rapold , Marcel Senn , Thomas Gobel , Anthony Cornelius O'Sullivan
IPC分类号: C07D413/02 , C07D277/20 , C07D277/70
CPC分类号: C07D277/32 , C07D277/16 , C07D277/36 , C07D277/70 , C07D277/74
摘要: The present disclosure is directed to a process for the preparation of a compound having the formula: wherein R is unsubstituted or substituted C1-C12alkyl, unsubstituted or substituted C2-C4alkenyl, unsubstituted or substituted C2-C4alkynyl, unsubstituted or substituted C3-C6cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, or —SR1; R1 is unsubstituted or substituted C1-C12alkyl, unsubstituted or substituted C2-C4alkenyl, unsubstituted or substituted C2-C4alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; and X is a selected leaving group that is not halogen, and may specifically be methylsulfonate, trifluoromethylsulfonate, and p-toluenesulfonate. These compounds are valuable intermediates useful in the synthesis of compounds having pesticidal activity. Generally, the process includes reacting a water-removing reagent, with a compound having the formula Water-removing agents that may be used include thionyl chloride (SOCl2), thionyl bromide (SOBr2), phosphorus oxychloride (POCl3), phosphorus oxybromide (POBr3), phosphorus pentachloride or a sulfonic acid chloride or bromide.
摘要翻译: 本公开涉及制备具有下式的化合物的方法:其中R是未取代的或取代的C 1 -C 12烷基,未取代或取代的C 2 -C 4烯基,未取代或取代的C 2 -C 4炔基,未取代或取代的C 3 -C 6环烷基,未取代的 或取代的芳基,未取代或取代的杂芳基或-SR1; C 1 -C 12烷基,未取代或取代的C 2 -C 4烯基,未取代或取代的C 2 -C 4炔基,未取代或取代的环烷基,未取代或取代的芳基或未取代或取代的杂芳基; X是不是卤素的选择的离去基团,可以具体为甲基磺酸酯,三氟甲基磺酸酯和对甲苯磺酸酯。 这些化合物是有用的合成具有杀虫活性的化合物的中间体。 通常,该方法包括使除水试剂与具有式的化合物反应可以使用的除水剂包括亚硫酰氯(SOCl 2),亚硫酰溴(SOBr 2),三氯氧化磷(POCl 3),三溴氧化磷(POBr 3) ,五氯化磷或磺酰氯或溴化物。
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公开(公告)号:US07538229B2
公开(公告)日:2009-05-26
申请号:US11947891
申请日:2007-11-30
申请人: Thomas Pitterna , Henry Szczepanski , Peter Maienfisch , Ottmar Franz Huter , Thomas Rapold , Marcel Senn , Thomas Gobel , Anthony Cornelius O'Sullivan
发明人: Thomas Pitterna , Henry Szczepanski , Peter Maienfisch , Ottmar Franz Huter , Thomas Rapold , Marcel Senn , Thomas Gobel , Anthony Cornelius O'Sullivan
IPC分类号: C07D277/36
CPC分类号: C07D277/32 , C07D277/16 , C07D277/36 , C07D277/70 , C07D277/74
摘要: A process for the preparation of a compound of formula I wherein R is a range of organic groups and X is a leaving group which process comprises a) reacting a compound of the formula II where R is defined for formula (I) with a water-removing reagent; or b) for the preparation of a compound of formula (I) wherein K is halogen or a sulfonate, reacting a compound of the formula III where R is defined for formula (I) with a halogenating agent or a sulfonylating agent; or c) for the preparation of a compound of formula (I) wherein X is halogen, reacting a compound of the formula IV where R is as defined for formula (I) and R2 and R3 are defined organic groups with a compound of the formula halogen-C(—O)—O—C1-C8alkyl, halogen-C(—O)—O-aryl or halogen-C(—O)—O-benzyl.
摘要翻译: 一种制备式I化合物的方法,其中R是有机基团的范围,X是离去基团,该方法包括:a)将式II化合物(其中R定义为式(I))与水 - 去除试剂; 或b)用于制备其中K为卤素或磺酸盐的式(I)化合物,其中R为式(I)所定义的式III化合物与卤化剂或磺酰化剂反应; 或c)用于制备其中X为卤素的式(I)化合物,使式IV化合物(其中R如式(I)所定义)与R 2和R 3定义为有机基团的化合物与式 卤素-C(-O)-O-C 1 -C 8烷基,卤素-C(-O)-O-芳基或卤素-C( - ) - O-苄基。
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公开(公告)号:US06369233B1
公开(公告)日:2002-04-09
申请号:US09628392
申请日:2000-08-01
申请人: Thomas Pitterna , Henry Szczepanski , Peter Maienfisch , Ottmar Franz Hüter , Thomas Rapold , Marcel Senn , Thomas Göbel , Anthony Cornelius O'Sullivan , Gottfried Seifert
发明人: Thomas Pitterna , Henry Szczepanski , Peter Maienfisch , Ottmar Franz Hüter , Thomas Rapold , Marcel Senn , Thomas Göbel , Anthony Cornelius O'Sullivan , Gottfried Seifert
IPC分类号: C07D27716
CPC分类号: C07D277/32 , C07D277/16 , C07D277/36 , C07D417/06
摘要: The Invention relates to a process for the preparation of a compound of the formula wherein Q, Y, Z, R1, R2, R3, R4 and R5 are as defined in the specification, which comprises a) reacting a compound of the formula with a halogenating agent to form a compound of the formula b) converting a compound of formula (II) by means of a halogenating agent into a compound of the formula optionally c) converting the compound of formula (IV) into a compound of formula (III); d) converting a compound of formula (III) by means of a compound of the formula e) converting a compound (IV) by means of a compound (V) into a compound (VI); and f) converting a compound (VI) by means of a chlorinating agent into a compound (I); a compound (IV); to a process for the preparation of a compound (III) and to a process for the preparation of a compound (IV).
摘要翻译: 本发明涉及制备糠醛的化合物的方法,其中Q,Y,Z,R 1,R 2,R 3,R 4和R 5如本说明书中所定义,其包括:a)使下式的化合物与卤化剂 将式(II)化合物通过卤化剂转化成式的化合物,任选地c)将式(Ⅳ)化合物转化为式(Ⅳ)化合物; d)转化 将化合物(Ⅳ)用化合物(Ⅴ)转化成化合物(Ⅵ),将式(Ⅳ)化合物与下式化合物反应; 和(f)通过氯化剂将化合物(VI)转化为化合物(I);化合物(IV); 涉及制备化合物(III)的方法和制备化合物(IV)的方法。
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公开(公告)号:US06265585B1
公开(公告)日:2001-07-24
申请号:US09341716
申请日:1999-07-15
申请人: Thomas Pitterna , Peter Maienfisch , David John Wadsworth , Laurenz Gsell , Thomas Rapold , Henry Szczepanski
发明人: Thomas Pitterna , Peter Maienfisch , David John Wadsworth , Laurenz Gsell , Thomas Rapold , Henry Szczepanski
IPC分类号: C07D27732
CPC分类号: C07D277/32
摘要: A process for the preparation of a compound of formula (I), wherein X is a leaving group; which process comprises, a) for the preparation of a compound of formula (I) wherein X is —OS(═O)2A and A is as defined in the specification, reacting a compound of formula (II) with a sulfonylating agent; or, b) for the preparation of a compound of formula (I) wherein X is iodine, reacting a compound of formula (III) with an iodinating agent, preferably sodium iodide; or, c) for the preparation of a compound of formula (I) whrein X is bromine, reacting a compound of formula (IV) with a brominating agent; or, d) for the preparation of a compound (I) wherein X is chlorine or bromine, reacting a compound (V), wherein R and X are as defined in the specification, with a chlorinating agent, a compound of formula (Ib), the use thereof and a process for the preparation of a compound of formula (II) and a compound of formula (A) are described.
摘要翻译: 一种制备式(I)化合物的方法,其中X是离去基团; 该方法包括a)制备式(I)化合物,其中X为-OS(= O)2A且A如说明书中所定义,式(II)化合物与磺酰化剂反应; 或b)制备其中X为碘的式(I)化合物,使式(III)化合物与碘化剂,优选碘化钠反应; 或者,c)制备式(I)化合物,其中X是溴,式(Ⅳ)化合物与溴化剂反应; 或者d)制备其中X为氯或溴的化合物(I),其中R和X如说明书中所定义的化合物(Ⅴ)与氯化剂,式(Ib)化合物反应, 描述了其用途和制备式(II)化合物和式(A)化合物的方法。
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公开(公告)号:US6121455A
公开(公告)日:2000-09-19
申请号:US331432
申请日:1999-08-13
申请人: Thomas Pitterna , Henry Szczepanski , Peter Maienfisch , Ottmar Franz Huter , Thomas Rapold , Marcel Senn , Thomas Gobel , Anthony Cornelius O'Sullivan , Gottfried Seifert
发明人: Thomas Pitterna , Henry Szczepanski , Peter Maienfisch , Ottmar Franz Huter , Thomas Rapold , Marcel Senn , Thomas Gobel , Anthony Cornelius O'Sullivan , Gottfried Seifert
IPC分类号: C07D277/16 , C07D277/20 , C07D277/22 , C07D277/28 , C07D277/32 , C07D277/36 , C07D277/74 , C07D417/06 , C07D417/14
CPC分类号: C07D277/32 , C07D277/16 , C07D277/36 , C07D417/06
摘要: The invention relates to a process for the preparation of a compound of the formula ##STR1## and, where applicable, its E/Z-isomers, mixtures of E/Z-isomers and/or tautomers, in each case in free form or in salt form, whereinQ is CH or N,Y is NO.sub.2 or CN,Z is CHR.sub.3, O, NR.sub.3 or S,R.sub.1 and R.sub.2 are either each independently of the other hydrogen or unsubstituted or R.sub.4 -substituted C.sub.1 -C.sub.8 alkyl, or together form an alkylene bridge having two or three carbon atoms, and said alkylene bridge may additionally contain a hetero atom selected from the group consisting of NR.sub.5, O and S,R.sub.3 is H or unsubstituted or R.sub.4 -substituted C.sub.1 -C.sub.12 alkyl,R.sub.4 is unsubstituted or substituted aryl or heteroaryl, andR.sub.5 is H or C.sub.1 -C.sub.12 alkyl; which comprisesa) reacting a compound of the formula ##STR2## and, where applicable, its E/Z-isomers, mixtures of E/Z-isomers and/or tautomers, in each case in free form or in salt form, which is known or can be prepared by processes known.
摘要翻译: PCT No.PCT / EP97 / 07087第 371日期1999年8月13日 102(e)日期1999年8月13日PCT 1997年12月17日PCT公布。 第WO98 / 27074号公报 日期1998年6月25日本发明涉及一种制备下式化合物和(如适用的话)其E / Z-异构体,E / Z-异构体和/或互变异构体的混合物的方法,在每种情况下为游离形式 或盐形式,其中Q是CH或N,Y是NO 2或CN,Z是CHR 3,O,NR 3或S,R 1和R 2各自独立地是另一个氢或未取代的或者R 4取代的C 1 -C 8烷基,或一起 形成具有两个或三个碳原子的亚烷基桥,并且所述亚烷基桥可以另外含有选自NR5,O和S的杂原子,R3是H或未取代的或R4取代的C1-C12烷基,R4是未取代的或 取代的芳基或杂芳基,R5是H或C1-C12烷基; 其包括:a)使游离形式或盐形式的下式化合物和/或其可能的E / Z-异构体,E / Z-异构体和/或互变异构体的混合物在各种情况下反应,其为已知或可以 由已知的方法准备。
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公开(公告)号:US20070055063A1
公开(公告)日:2007-03-08
申请号:US11552255
申请日:2006-10-24
申请人: Thomas Pitterna , Henry Szczepanski , Peter Maienfisch , Ottmar Huter , Thomas Rapold , Marcel Senn , Thomas Gobel , Anthony O'Sullivan
发明人: Thomas Pitterna , Henry Szczepanski , Peter Maienfisch , Ottmar Huter , Thomas Rapold , Marcel Senn , Thomas Gobel , Anthony O'Sullivan
IPC分类号: C07D417/02
CPC分类号: C07D277/32 , C07D277/16 , C07D277/36 , C07D277/70 , C07D277/74
摘要: A process for the preparation of a compound of the formula and, where applicable, its E/Z-isomers, mixtures of E/Z-isomers and/or tautomers and acid addition products thereof, in each case in free form or in salt form, wherein: R is unsubstituted or substituted C1-C12alkyl, unsubstituted or substituted C2-C4alkenyl, unsubstituted or substituted C2-C4alkynyl, unsubstituted or substituted C3-C6cycloalkyl, unsubstituted or substituted aryl, unsubstituted or substituted heteroaryl, or —SR1; R1 is unsubstituted or substituted C1-C12alkyl, unsubstituted or substituted C2-C4alkenyl, unsubstituted or substituted C2-C4alkynyl, unsubstituted or substituted cycloalkyl, unsubstituted or substituted aryl or unsubstituted or substituted heteroaryl; and X is a leaving group; The process comprises reacting a compound of the formula: with a halogenating agent or a sulfonylating agent. Alternatively, when X is a selected halogen, the process can comprise reacting a compound of the formula with a compound having a formula selected from the group consisting of halogen-C(═O)—O—C1-C8alkyl; halogen-C(═O)—O-aryl; and halogen-C(═O)—O-benzyl.
摘要翻译: 制备下式化合物及其E / Z-异构体的方法,E / Z-异构体和/或互变异构体的混合物及其酸加成产物,各自为游离形式或盐形式 ,其中:R是未取代或取代的C 1 -C 12烷基,未取代或取代的C 2 -C 4 烯基,未取代或取代的C 2 -C 4炔基,未取代或取代的C 3 -C 6环烷基 ,未取代或取代的芳基,未取代或取代的杂芳基或-SR 1 N; R 1是未取代或取代的C 1 -C 12烷基,未取代或取代的C 2 -C 3 未取代或取代的C 2 -C 4炔基,未取代或取代的环烷基,未取代或取代的芳基或未取代或取代的杂芳基; X为离去群; 该方法包括使下式化合物与卤化剂或磺酰化剂反应。 或者,当X是选择的卤素时,该方法可以包括使下式的化合物与具有选自以下的式的化合物反应:卤素-C( - ) - O-C 1 -C 烷基; 卤素-C( - ) - O-芳基; 和卤素-C( - ) - O-苄基。
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