公开(公告)号：US3897438A

公开(公告)日：1975-07-29

申请号：US11716171

申请日：1971-02-19

Applicant: BAYER AG

Inventor： DRABER WILFRIED ,  REGEL ERIK

IPC: A01N43/50 ,  A01N43/653 ,  A61K31/42 ,  A61K31/44 ,  A61K31/4427 ,  A61K31/443 ,  A61K31/4433 ,  A61P31/04 ,  A61P31/10 ,  A61P31/12 ,  C07D233/54 ,  C07D233/56 ,  C07D233/58 ,  C07D233/60 ,  C07D233/62 ,  C07D249/08 ,  C07D401/06 ,  C07D405/04 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07D413/06 ,  C07D521/00 ,  C07D31/00 ,  C07D55/02

CPC classification number: C07D233/64 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

Abstract: N-(1,1,1-trisubstituted)-methylazoles are produced by reacting thionyl-imidazole with a substituted carbinol of the formula:

wherein A is aliphatic, cycloaliphatic, aromatic or heteroaromatic, B is aliphatic, cycloaliphatic, aromatic or a 5or 6-membered heteroaromatic ring having 1 to 3 N-heteroatoms or 1 or 2 N-heteroatoms plus an oxygen or sulphur heteroatom and D is aliphatic, cycloaliphatic, aromatic, alkoxycarbonyl, alkoxycarbonylalkyl, aryloxycarbonyl or a 5- or 6-membered heteroaromatic ring having 1 to 3 N-heteroatoms or 1 or 2 Nheteroatoms plus an oxygen or sulphur heteroatom and related carbinols. The reactants are in 1:1 molar ratio and the reaction is carried out in dry inert solvents at a temperature of -20* C. to +150* C.

Abstract translation: N-（1,1,1-三取代） - 甲基唑通过使亚硫酰 - 咪唑与下式的取代的甲醇反应来制备：B | ACD | OH其中A是脂族，脂环族，芳族或杂芳族，B是脂族，脂环族， 芳族或具有1至3个N-杂原子或1或2个N-杂原子加上氧或硫杂原子的5或6元杂芳环，D是脂族，脂环族，芳族，烷氧基羰基，烷氧基羰基烷基，芳氧基羰基或5-或 具有1至3个N-杂原子或1或2个N杂原子加上氧或硫杂原子和相关甲醇的6元杂芳环。 反应物的摩尔比为1:1，反应在干燥的惰性溶剂中，在-20℃至+ 150℃的温度下进行。

公开(公告)号：US3665079A

公开(公告)日：1972-05-23

申请号：US3665079D

申请日：1970-09-02

Applicant: BAYER AG

Inventor： BUCHEL KARL-HEINZ ,  REGEL ERIK ,  GREWE FERDINAND ,  SCHEINPFLUG HANS ,  KASPERS HELMUT

IPC: A01N9/22

CPC classification number: C07D233/56

Abstract: Plant fungicidal compositions are produced which comprises an amount of a compound of the formula:

WHEREIN R is alkyl of one or two carbon atoms substituted by one to five fluoro moieties, sufficient to be effective for killing, combating or controlling plant fungi, in combination with a solid or liquid diluent or carrier. Methods for killing, combatting or controlling fungal diseases in plants comprise applying to the fungi or to the plant to be protected an effective or toxic amount of the above compound.

公开(公告)号：US3887556A

公开(公告)日：1975-06-03

申请号：US31042372

申请日：1972-11-29

Applicant: BAYER AG

Inventor： DRABER WILFRIED ,  BUCHEL KARL HEINZ ,  REGEL ERIK ,  PLEMPEL MANFRED

IPC: A61K31/495 ,  A61K31/505 ,  C07D241/12 ,  C07D403/06 ,  C07D51/36

CPC classification number: C07D403/06 ,  A61K31/495 ,  A61K31/505 ,  C07D241/12

Abstract: N-methyl-imidazole derivatives of the formula:

OR A PHARMACEUTICALLY ACCEPTABLE NON-TOXIC SALT THEREOF, WHEREIN X is an unsubstituted or substituted six-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.

Abstract translation: 下式的N-甲基 - 咪唑衍生物：

公开(公告)号：US3655900A

公开(公告)日：1972-04-11

申请号：US3655900D

申请日：1970-05-11

Applicant: BAYER AG

Inventor： BUCHEL KARL H ,  REGEL ERIK ,  PLEMPEL MANFRED

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

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)-C(-HAL)(-(1,4-PHENYLENE)-(X")N")-),(X'')N''-

BENZENE

N-TRITYL-IMIDAZOLES AND SALTS THEREOF OF THE FORMULA:

1-(((X)N-PHENYL)-C(-(1,4-PHENYLENE)-(X")N")(-(1,4-

PHENYLENE)-(X'')N'')-),2-R,4-R1,5-R2-IMIDAZOLE

WHEREIN

R, R1 AND R2 ARE HYDROGEN, LOWER ALKYL OR PHENYL, OR R1 AND R2 TOGETHER FORM AN ANELLATED BENZEN RING, X, X'' AND X" ARE ALKYL OR 1 TO 12 CARBON ATOMS OR AN ELECTRO-NEGATIVE MOIETY, AND N, N'' N" ARE AN INTEGER FROM 0 TO 2,

公开(公告)号：US3928348A

公开(公告)日：1975-12-23

申请号：US31040072

申请日：1972-11-29

Applicant: BAYER AG

Inventor： DRABER WILFRIED ,  BUCHEL KARL HEINZ ,  REGEL ERIK ,  PLEMPEL MANFRED

IPC: A61K31/495 ,  A61K31/505 ,  C07D241/12 ,  C07D403/06 ,  C07D237/08

CPC classification number: C07D403/06 ,  A61K31/495 ,  A61K31/505 ,  C07D241/12

Abstract: N-methyl-imidazole derivatives of the formula:

OR A PHARMACEUTICALLY ACCEPTABLE NON-TOXIC SALT THEREOF, WHEREIN X is an unsubstituted or substituted 6-membered hetero-aromatic 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.

Abstract translation: 下式的N-甲基 - 咪唑衍生物：

公开(公告)号：US3666862A

公开(公告)日：1972-05-30

申请号：US3666862D

申请日：1970-09-02

Applicant: BAYER AG

Inventor： BUCHEL KARL-HEINZ ,  REGEL ERIK ,  GREWE FERDINAND ,  SCHEINPFLUG HANS ,  KASPERS HELMUT

IPC: C07D233/56 ,  A01N43/50 ,  A01P3/00 ,  C07D233/62 ,  C07D521/00 ,  A01N9/22

CPC classification number: C07D231/12 ,  A01N43/50 ,  C07D233/56 ,  C07D249/08

Abstract: Plant fungicidal compositions are produced which comprise an amount of a compound of the formula:

WHEREIN R is cyano, sufficient to be effective for killing, combatting or controlling plant fungi, in combination with a solid or liquid diluent or carrier. Methods for killing, combatting or controlling fungal diseases in plants comprise applying to the fungi or to the plant to be protected an effective or toxic amount of the above compound.

公开(公告)号：US3655899A

公开(公告)日：1972-04-11

申请号：US3655899D

申请日：1970-05-11

Applicant: BAYER AG

Inventor： BUCHEL KARL H ,  REGEL ERIK ,  PLEMPEL MANFRED

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-TRITYL-IMIDAZOLES AND SALTS THEREOF OF THE FORMULA:

1-(((X)N-PHENYL)-C(-(1,4-PHENYLENE)-(X")N")(-(1,4-

PHENYLENE)-(X'')N'')-),2-R,4-R1,5-R2-IMIDAZOLE

WHEREIN

R, R1 AND R2 ARE HYDROGEN, LOWER ALKYL OR 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-NEGATIVE 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 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)-C(-HAL)(-(1,4-PHENYLENE)-(X")N")-),(X'')N''-

BENZENE

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

公开(公告)号：US3665077A

公开(公告)日：1972-05-23

申请号：US3665077D

申请日：1970-09-02

Applicant: BAYER AG

Inventor： BUCHEL KARL-HEINZ ,  REGEL ERIK ,  GREWE FERDINAND ,  SCHEINPFLUG HANS ,  KASPERS HELMUT

IPC: C07D233/56 ,  A01N43/50 ,  A01P3/00 ,  C07D233/62 ,  C07D521/00 ,  A01N9/22

CPC classification number: C07D231/12 ,  A01N43/50 ,  C07D233/56 ,  C07D249/08

Abstract: Plant fungicidal compositions are produced which comprise an amount of a compound of the formula:

WHEREIN R is alkylmercapto of one to three carbon atoms, sufficient to be effective for killing, combatting or controlling plant fungi, in combination with a solid or liquid diluent or carrier. Methods for killing, combatting or controlling fungal diseases in plants comprises applying to the fungi or to the plant to be protected an effective or toxic amount of the above compound.

公开(公告)号：US3665076A

公开(公告)日：1972-05-23

申请号：US3665076D

申请日：1970-09-02

Applicant: BAYER AG

Inventor： BUCHEL KARL HEINZ ,  REGEL ERIK ,  GREWE FERDINAND ,  SCHEINPFLUG HANS ,  KASPERS HELMUT

IPC: C07D233/56 ,  A01N43/50 ,  A01P3/00 ,  C07D233/62 ,  C07D521/00 ,  A01N9/22

CPC classification number: C07D231/12 ,  A01N43/50 ,  C07D233/56 ,  C07D249/08

Abstract: WHEREIN R is alkoxy of one to three carbon atoms, sufficient to be effective for killing, combatting or controlling plant fungi, in combination with a solid or liquid diluent or carrier. Methods for killing, combatting or controlling fungal diseases in plants comprise applying to the fungi or to the plant to be protected an effective or toxic amount of the above compound.

Plant fungicidal compositions are produced which comprise an amount of a compound of the formula:

Abstract translation: 制备植物杀真菌组合物，其包含一定量的下式的化合物：

公开(公告)号：US3658956A

公开(公告)日：1972-04-25

申请号：US3658956D

申请日：1970-05-11

Applicant: BAYER AG

Inventor： BUCHEL KARL H ,  REGEL ERIK ,  PLEMPEL MANFRED

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-TRITYL-IMIDAZOLES AND SALTS THEREOF OF THE FORMULA:

1-(((X")N"-PHENYL)-C(-PHENYLENE-(X)N)(-PHENYLENE-

(X'')N'')-),2-R,4-R1,5-R2-IMIDAZOLE

WHEREIN

R, R1 AND R2 ARE HYDROGEN, LOWER ALKYL OR PHENYL, OR R1 AND R2 TOGETHER FORM AN ANELATED BENZENE RING, X, X'' AND X" ARE ALKYL OF 1 TO 12 CARBON ATOMS OR AN ELECTRO-NEGATIVE MOIETY, AND N, N'' NAD N" ARE INTEGERS 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)-C(-HAL)(-PHENYLENE-(X")N")-),(X'')N''-

BENZENE

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