公开(公告)号：US3818029A

公开(公告)日：1974-06-18

申请号：US21543772

申请日：1972-01-04

Applicant: BAYER AG

Inventor： REGEL E ,  BUCHEL K ,  HAMMANN I ,  UNTERSTENHOFER G

IPC: A01N47/24 ,  C07D233/54 ,  C07D233/64 ,  C07D401/06 ,  C07D405/06 ,  C07D413/06 ,  C07D49/36

CPC classification number: C07D233/64

Abstract: Imidazolyl-ketoxime-carbamates of the general formula

IN WHICH X and Y each independently is hydrogen, halogen, methyl, ethyl or optionally substituted aryl, or X and Y together constitute a (CH)4 group forming a fused benzene ring with the two imidazole-ring carbon atoms to which they are attached, R and R'''' each independently is alkyl or alkenyl with up to 6 carbon atoms; or aryl or aralkyl optionally carrying at least one halogen, nitro or alkyl substituent, R'' is alkyl, haloalkyl, optionally substituted aryl or a fiveor six-membered heteroaromatic ring optionally carrying at least one halogen, alkyl, aryl or substituted aryl substituent, and R'''''' is hydrogen, or alkyl or alkenyl with up to four carbon atoms, which possess insecticidal, acaricidal and bactericidal properties.

Abstract translation: 咪唑基 - 酮肟基 - 氨基甲酸酯，其中X和Y各自独立地为氢，卤素，甲基，乙基或任选取代的芳基，或X和Y一起构成（CH）4基团，与两个咪唑形成稠合苯环 它们连接的碳原子，R和R“各自独立地是具有至多6个碳原子的烷基或烯基; 或任选携带至少一个卤素，硝基或烷基取代基的芳基或芳烷基，R'是烷基，卤代烷基，任选取代的芳基或任选携带至少一个卤素，烷基，芳基或取代的芳基取代基的五元或六元杂芳环 ，R“是氢，或具有至多4个碳原子的烷基或烯基，其具有杀虫，杀螨和杀菌性质。

公开(公告)号：US3787415A

公开(公告)日：1974-01-22

申请号：US3787415D

申请日：1971-03-02

Applicant: BAYER AG

Inventor： DRABER W ,  PLEMPEL M ,  BUECHEL K ,  REGEL E

IPC: C07D403/10 ,  A61K31/495 ,  A61K31/505 ,  C07D241/12 ,  C07D403/06 ,  C07D521/00 ,  C07D51/76

CPC classification number: C07D231/12 ,  A61K31/495 ,  A61K31/505 ,  C07D233/56 ,  C07D241/12 ,  C07D249/08 ,  C07D403/06

Abstract: N-METHYL-IMIDAZOLE DERIVATIVES OF THE FORMULA

1-(Y-C(-X)(-Z)-)IMIDAZOLE

OR A PHARAMECUTICALLY ACCEPTABLE NON-TOXIC SALT THEREOF, WHEREIN X IS AN UNSUBSTITUTED OR SUBSTITUTED 6-MEMBERED HETEROAROMATIC MOIETY HAVING TWO NITRO HETEROATOMS, Y IS AN UNSUBSTITUTED OR SUBSTITUTED ALIPHATIC MOIETY, AN UNSUBSTITUTED OR SUBSTITUTED CYCLOALIPHATIC MOIETY, AN UNSUBSTITUTED OR SUBSTITUTED ARALKYL MOIETY OR AN UNSUBSTITUTED OR SUBSTITUTED ARYL MOIETY, AND Z IS AN UNSUBSTITUTED OR SUBSTITUTED ALIPHATIC MOIETY, AN UNSUBSTITUTED OR SUBSTITUTED CYCLOALIPHATIC MOIETY, AN UNSUBSTITUTED OR SUBSTITUTED ARALKYL MOIETY, AN UNSUBSTITUTED OR SUBSTITUTED ARYL MOIETY, AN UNSUBSTITUTED OR SUBSTITUTED PYRIDYL MOIETY OR AN ALKOXYCARBONYL MOIETY ARE USEFUL AS ANTIMYCOTIC AGENTS.

公开(公告)号：US3772315A

公开(公告)日：1973-11-13

申请号：US3772315D

申请日：1970-05-18

Applicant: BAYER AG

Inventor： REGEL E ,  BUCHEL K

IPC: C07D233/66 ,  A01N43/50 ,  C07D233/54 ,  C07D233/90 ,  C07D235/12 ,  C07D401/06 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/06 ,  C07D49/36 ,  C07D49/38

CPC classification number: C07D233/64 ,  C07D233/54 ,  C07D233/90

Abstract: THE INVENTION RELATES TO 2-ACYL-1-ALKYL- OR -ARYL-IMIDAZOLES, WHEREIN THE 4- AND 5-POSITIONS OF THE IMIDAZOLE RING AS WELL AS THE 1-ALKYL OR -ARYL SUBSTITUTENT MAY BE SUBSTITUTED, WHICH, IN THE FORM OF THEIR ACID ADDITION SALTS, POSSES FUNGICIDAL ACTIVITY, AND WHICH ARE ALSO USEFUL AS INTERMEDIATES IN FURTHER SYNTHESES. THE INVENTION ALSO PROVIDES A PROCESS FOR PRODUCING SUCH COMPOUNDS BY ACYLATION OF THE CORRESPONDING IMIDAZOLE, UNSUBSTITUTED IN THE 2-POSITION, WITH THE APPROPRIATE ACID HALIDE.

公开(公告)号：US3764690A

公开(公告)日：1973-10-09

申请号：US3764690D

申请日：1972-03-03

Applicant: BAYER AG

Inventor： DRABER W ,  REGEL E ,  BUCHEL K ,  PLEMPEL M

IPC: C07D233/54 ,  A61K27/00

CPC classification number: C07D233/56

Abstract: Substituted N-benzylimidazoles of the formula:

WHEREIN

WHEREIN A, B, X and m are as above defined and Z is chlorine or bromine, with at least the theoretically necessary amount of imidazole, optionally in the presence of an acid acceptor, in a polar organic solvent, at a temperature of from 20* to 150* C. These substituted N-benzylimidazoles are useful as antimycotics and are effective against both yeasts and dermatophytes. These compounds are effective against a wide range of fungi pathogenic to humans and animals.

WHEREIN D is CH or N, E is oxygen, sulphur, N-lower alkyl or N-aryl, Y is hydrogen, 1 or 2 lower alkyls, 1 or 2 halogens, aryl or substituted aryl, and N IS 1 OR 2, ARE PRODUCED BY REACTING A COMPOUND OF THE FORMULA:

WHEREIN R1, R2 and R3 are each hydrogen, straight or branched chain lower alkyl or straight or branched chain lower alkenyl, X is hydrogen, lower alkyl, lower alkoxy, lower alkylmercapto, lower alkenylmercapto, trifluoromethyl, halogen, nitro, cyano, amino or amino substituted by 1 or 2 aliphatic moieties, M IS 1 OR 2, A is phenyl; substituted phenyl, pyridyl, lower alkyl or cycloalkyl, B is a 5-membered heteroaromatic ring of the formula:

Abstract translation: 下式的取代的N-苄基咪唑：

公开(公告)号：US3720770A

公开(公告)日：1973-03-13

申请号：US3720770D

申请日：1971-03-19

Applicant: BAYER AG

Inventor： PLEMPEL M ,  BUCHEL K ,  REGEL E

IPC: C07D233/62 ,  C07D235/06 ,  C07D235/08 ,  C07D235/18 ,  C07D521/00 ,  A61K27/00

CPC classification number: C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D235/06 ,  C07D235/08 ,  C07D235/18

Abstract: N-TRITRYL-IMIDAZOLES AND SALTS THEREOF THE FORMULA:

1-(((X)N-PHENYL-)((X'')N''-PHENYL)((X")N"-PHENYL)-C-),2-R,

4-R1,5-R2-IMIDAZOLE

WHEREIN R, R1 AND R2 ARE HYDROGEN, LOWER ALKYL OF PHENYL, OR R1 AND R2 TOGETHER FORM AN ANELLATED BENZENE RING, X, X'' AND X''" ARE ALKYL OF 1 TO 12 CARBON ATOMS OR AN ELECTRO-NETATIVE MOIETY, AND N N'' AND N" ARE AN INTEGER FROM 0 TO 2, OR PHARMACEUTICALLY ACCEPTABLE ACID SALTS THEREOF MAY BE PRODUCED BY REACTING A SILVER SALT OF ALKALI METAL SALT OF AN IMIDAZOLE OF THE FORMULA:

2-R,4-R1,5-R2-IMIDAZOLE

WITH A TRITYL HALIDE OF THE FORMULA:

((X)N-PHENYL)((X'')N''-PHENYL)((X")N"-PHENYL)-C-HAL

WHEREIN THE SUBSTITUENTS ARE AS BORE DEFINED AND HAL IS HALOGEN. THESE COMPONENTS ARE USEFUL AS ANTIMYCOTICS.

公开(公告)号：US3711500A

公开(公告)日：1973-01-16

申请号：US3711500D

申请日：1972-01-17

Applicant: BAYER AG

Inventor： PLEMPEL M ,  BUCHEL K ,  REGEL E

IPC: C07D233/62 ,  C07D235/06 ,  C07D235/08 ,  C07D235/18 ,  C07D521/00 ,  C07D49/36

CPC classification number: C07D249/08 ,  C07D231/12 ,  C07D233/56 ,  C07D235/06 ,  C07D235/08 ,  C07D235/18

Abstract: N-TRITYL:IMIDAZOLES AND SALTS THEREOF OF THE FORMULA:
WHEREIN R, R1 AND R2 ARE HYDROGEN, LOWER ALKYL OR PHENYL, OR R1 ANS R2 TOGETHER FORM AN ANELLATED BENZENE RING, X, R'' AND X" ARE ALKYL OF 1 TO 12 CARBON ATOMS OR AN ELECTRO-NEGATIVE MOIETY, AND N, N'' AND N" ARE IN INTEGER FROM 0 TO 2, OR PHARMACEUTICALLY ACCEPTABLE ACID SALTS THEREOF MAY BE PRODUCED BY REACTING A SILVER SALT OR ALKALI METAL SALT OF AN IMIDAZOLE OF THE FORMULA:

2-R,4-R1,5-R2-IMIDAZOLE

WITH A TRITYL HALIDE OF THE FORMULA:

(((X)N-PHENYL-),((X'')N-PHENYL-)((X")N"-PHENYL-)C-HAL

WHEREIN THE SUBSTITUENTS ARE AS ABOVE DEFINED AND HAL IS HALOGEN. THESE COMPOUNDS ARE USEFUL AS ANTIMYCOTICS.

4-R1,5-R2-IMIDAZOLE

1-(((X)N-PHENYL-)((X'')N''-PHENYL-)((X")N"-PHENYL-)C-),2-R,