IP Library Granted Patent US 8,759,527
Granted Patent B2
US 8,759,527 · App. 13/216,033 · Granted Jun 24, 2014

Heteroarylpiperidine and -piperazine derivatives as fungicides

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Quick Facts
Patent No.
US 8,759,527
App. No.
13/216,033
Granted
Jun 24, 2014
Kind
B2
Abstract

Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols A, X, Y, L 1 , L 2 , G, Q, p, R 1 , R 2 and R 10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).

Claims (50)

1. A compound of formula (I) and/or a salt, metal complex and/or N-oxides of a compound of the formula (I),

wherein

A is pyrazol-1-yl which may contain up to two substituents, where the substituents are each independently selected from the following list:

substituents on carbon:

halogen, cyano, hydroxyl, nitro, —NR 3 R 4 , C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkenyl, C 3 -C 6 -cycloalkyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 2 -C 6 -haloalkynyl, C 3 -C 6 -halocycloalkyl, C 1 -C 4 -alkoxy, C 1 -C 4 -haloalkoxy, C 1 -C 4 -alkylthio, C 1 -C 4 -alkylsulphonyl, C 1 -C 4 -haloalkylthio, C 1 -C 4 -haloalkylsulphonyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, hydroxy-C 1 -C 4 -alkyl, C 1 -C 6 -alkylcarbonyl, C 1 -C 6 -alkoxycarbonyl, C 1 -C 6 -alkylcarbonyloxy or phenyl, substituents on nitrogen:

C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 2 -C 6 -haloalkynyl, C 3 -C 10 -cycloalkyl-C 1 -C 6 -alkyl, C 1 -C 6 -haloalkylcarbonyl, phenyl, benzyl, C 1 -C 4 -alkylsulphonyl, C 1 -C 4 -haloalkylsulphonyl, phenylsulphonyl, —C(C═O)H, or C 1 -C 6 -alkylcarbonyl,

R G1 is the same or different and is independently hydrogen, halogen, hydroxyl, thiol, nitro, cyan, —C(C═O)H, —C(C═O)OH, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, cycloalkyl, halocycloalkyl, hydroxyalkyl, formylalkyl, alkoxyalkyl, alkylcarbonylalkyl, alkylcycloalkyl, alkoxy, alkylcycloalkylalkyl, alkylthio, aloalkylthio, alkynylthio, alkenyloxy, alkynyloxy, haloalkoxy, alkoxyalkoxy, alkylcarbonyloxy, haloalkylcarbonyloxy, cycloalkylcarbonylamino, alkylsulphonylamino, haloalkylsulphonylamino, phenylsulphonylamino, cycloalkylalkyl, halocycloalkylalkyl, cycloalkylcycloalkyl, alkoxycarbonyloxy, alkylcarbonylthio, alkylsulphinyl, haloalkylsulphinyl, alkylsulphonyl, haloalkylsulphonyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl, alkylaminocarbonyloxy, —C(C═O)NR 3 R 4 or —NR 3 R 4 ,

R 3 and R 4 are the same or different and are each independently hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, benzyl or phenyl,

L 1 is C(R L11 ) 2 ,

R L11 is the same or different and is independently hydrogen, halogen, hydroxyl, cyano, —C(C═O)H, —C(C═O)OH, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, alkoxyalkyl, alkylthioalkyl, alkylaminoalkyl, dialkylaminoalkyl, alkoxy, alkylthio, haloalkylthio, haloalkoxy, alkylcarbonyloxy, alkylcarbonylamino, alkylcarbonylthio, alkylsulphonyl, haloalkylsulphonyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl, trialkylsilyloxy, —NR 3 R 4 or —C(C═O)NR 3 R 4 , or the two R L11 radicals, together with the carbon atom to which they are bonded, form a cyclopropyl ring, or the two R L11 radicals are ═CH 2 , ═COR 3 , ═NOR 3 or ═CHN(R 9 ) 2 ,

R 9 is alkyl, alkenyl, alkynyl, haloalkyl, cycloalkyl, benzyl or phenyl,

Y is sulphur or oxygen,

X is carbon,

R 2 is hydrogen,

R 10 is oxo, alkyl, alkenyl, haloalkyl, alkoxy, halogen, cyano or hydroxyl,

p is 0 or 1,

G is

where the bond identified by “v” is bonded directly to X and where the bond identified by “w” is bonded directly to Q,

Q is

where the bond is identified by “*” is bonded directly to G or L 2 , and where the bond identified by “#” is bonded directly to L 2 or G, or where the bond identified by “*” is bonded directly to L 2 , and the bond identified by “#” is at the same time bonded directly to G,

R 5 is the same or different and is independently:

bonded to carbon of Q:

hydrogen, oxo, halogen, cyano, hydroxyl, nitro, —CHO, —C(C═O)OH, —C(C═O)NH 2 , —C(C═O)NR 3 R 4 , —NR 3 R 4 , alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, cycloalkyl, halocycloalkyl, alkylcycloalkyl, cycloalkylalkyl, cycloalkylcycloalkyl, halocycloalkylalkyl, alkylcycloalkylalkyl, cycloalkenyl, halocycloalkenyl, alkoxyalkyl, haloalkoxyalkyl, cycloalkoxyalkyl, alkoxyalkoxyalkyl, alkylthioalkyl, formylalkyl, alkylcarbonylalkyl, alkylsulphinylalkyl, alkylsulphonylalkyl, alkylaminoalkyl, dialkylaminoalkyl, haloalkylaminoalkyl, cycloalkylaminoalkyl, alkylcarbonyl, haloalkylcarbonyl, cycloalkylcarbonyl, alkoxycarbonyl, cycloalkoxycarbonyl, cycloalkylalkoxycarbonyl, cycloalkylaminocarbonyl, hydroxyalkyl, alkoxy, haloalkoxy, cycloalkoxy, halocycloalkoxy, cycloalkylalkoxy, alkenyloxy, haloalkenyloxy, alkynyloxy, haloalkynyloxy, alkoxyalkoxy, alkylcarbonyloxy, haloalkylcarbonyloxy, cycloalkylcarbonyloxy, alkylcarbonylalkoxy, alkylthio, haloalkylthio, cycloalkylthio, alkylsulphinyl, haloalkylsulphinyl, alkylsulphonyl, haloalkylsulphonyl, cycloalkylsulphonyl, trialkylsilyl, alkylsulphonylamino, haloalkylsulphonylamino,

bonded to nitrogen of Q:

hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, cycloalkyl, halocycloalkyl, alkylcycloalkyl, cycloalkylalkyl, phenyl, benzyl, alkylsulphonyl, —C(C═O)H, alkoxycarbonyl or alkylcarbonyl,

L 2 is a direct bond,

m is 0, 1 or 2,

R 20 is hydrogen, alkyl or haloalkyl,

R 1 is phenyl which is substituted at least once by a substituent Z 4 and may otherwise be unsubstituted or substituted, where the substituents are each independently selected from Z 4 and optionally from Z 1 ,

Z 1 is hydrogen, halogen, hydroxyl, —SH, nitro, cyano, C(═O)H, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, cycloalkyl, cycloalkenyl, halocycloalkyl, halocycloalkenyl, hydroxyalkyl, alkoxyalkyl, haloalkoxyalkyl, cycloalkoxyalkyl, alkylthioalkyl, alkylsulphinylalkyl, alkylaminoalkyl, haloalkylaminoalkyl, cycloalkylaminoalkyl, dialkylaminoalkyl, alkylsulphonylalkyl, alkylcycloalkyl, alkoxy, alkylcycloalkylalkyl, halocycloalkoxy, alkylthio, haloalkylthio, cycloalkylthio, alkenyloxy, alkynyloxy, haloalkoxy, haloalkenyloxy, haloalkynyloxy, cycloalkoxy, alkoxyalkoxy, cycloalkylalkoxy, alkylcarbonyloxy, haloalkylcarbonyloxy, cycloalkylcarbonyloxy, cycloalkylamino, alkylsulphonylamino, haloalkylsulphonylamino, cycloalkylalkyl, halocycloalkylalkyl, cycloalkylcycloalkyl, alkoxyalkoxyalkyl, alkylcarbonylalkoxy, cycloalkylaminocarbonyl, cycloalkylalkoxycarbonyl, alkylcarbonylthio, alkylsulphinyl, haloalkylsulphinyl, alkylsulphonyl, haloalkylsulphonyl, cycloalkylsulphonyl, alkylcarbonyl, haloalkylcarbonyl, cycloalkylcarbonyl, alkoxycarbonyl, cycloalkoxycarbonyl, trialkylsilyl, —NR 3 R 4 , —C(C═O)NR 3 R 4 or -L 3 Z 3 ,

L 3 is a direct bond, —CH 2 —, —C(C═O)—, sulphur, oxygen, —C(C═O)O—, —C(C═O)NH—, —OC(═O)— or —NHC(═O)—,

or

L 3 is —NR 20 —, —C(═S)—, —S(O) m —, —CHR 20 —, —CHR 20 —CHR 20 —, —CR 20 ═CR 20 , —OCHR 20 —, —CHR 20 O—,

Z 3 is a phenyl radical, naphthalenyl radical or a 5- or 6-membered heteroaryl radical, each of which may contain 0, 1, 2 or 3 substituents, where the substituents are each independently selected from the following list:

substituents on carbon: halogen, cyano, nitro, hydroxyl, amino, —SH, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, cycloalkyl, halocycloalkyl, alkoxyalkyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl, alkoxy, haloalkoxy, cycloalkoxy, halocycloalkoxy, alkenyloxy, alkynyloxy, alkoxyalkoxy, alkylamino, dialkylamino, alkylthio, haloalkylthio, alkylsulphinyl, haloalkylsulphinyl, alkylsulphonyl, haloalkylsulphonyl, trisilylalkyl or phenyl,

substituents on nitrogen: hydrogen, —C(C═O)H, alkyl, alkenyl, alkynyl, haloalkyl, haloalkenyl, haloalkynyl, cycloalkyl, halocycloalkyl, alkylcycloalkyl, cycloalkylalkyl, alkoxyalkyl, alkylsulphonyl, haloalkylsulphonyl, cycloalkylsulphonyl, phenylsulphonyl, alkylcarbonyl, haloalkylcarbonyl, alkoxycarbonyl, haloalkoxycarbonyl, cycloalkoxycarbonyl, —C(C═O)NR 3 R 4 , phenyl or benzyl,

Z 4 is alkylsulphonyloxy.

2. A compound according to claim 1 , in which

R 5 is the same or different and is independently:

bonded to carbon of Q:

hydrogen, cyano, —NR 3 R 4 , C 1 -C 6 -alkyl, C 2 -C 6 -alkenyl, C 2 -C 6 -alkynyl, C 1 -C 6 -haloalkyl, C 2 -C 6 -haloalkenyl, C 2 -C 6 -haloalkynyl, C 3 -C 8 -cycloalkyl, C 3 -C 8 -halocycloalkyl, C 3 -C 8 -halocycloalkyl, C 1 -C 4 -alkyl-C 3 -C 8 -cycloalkyl, C 3 -C 8 -cycloalkyl-C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, C 3 -C 8 -cycloalkoxy-C 1 -C 4 -alkyl, C 1 -C 4 -alkoxy-C 1 -C 4 -alkoxy-C 1 -C 4 -alkyl, C 1 -C 4 -alkylthio-C 1 -C 4 -alkyl, C 1 -C 6 -alkoxy, C 1 -C 6 -haloalkoxy, C 3 -C 8 -cycloalkoxy, C 3 -C 8 -halocycloalkoxy, C 3 -C 8 -cycloalkyl-C 1 -C 4 -alkoxy, C 2 -C 6 -alkenyloxy, C 2 -C 6 -haloalkenyloxy, C 2 -C 6 -alkynyloxy, C 2 -C 6 -haloalkynyloxy, C 1 -C 6 -alkoxy-C 1 -C 4 -alkoxy, C 1 -C 6 -alkylcarbonyloxy, C 1 -C 6 -haloalkylcarbonyloxy, C 3 -C 8 -cycloalkylcarbonyloxy, C 1 -C 6 -alkylcarbonyl-C 1 -C 6 -alkoxy, C 1 -C 6 -alkylthio, C 1 -C 6 -haloalkylthio, C 3 -C 8 -cycloalkylthio,

bonded to nitrogen of Q:

hydrogen, —C(C═O)H, C 1 -C 3 -alkyl, C 1 -C 6 -alkylcarbonyl, C 1 -C 6 -alkoxycarbonyl or benzyl.

3. A compound according to claim 1 , in which

Z 4 is C 1 -C 6 -alkylsulphonyloxy.

4. Method for controlling phytopathogenic harmful fungi, comprising applying a compound according to claim 1 to the phytopathogenic harmful fungi and/or their habitat.

5. Composition for controlling phytopathogenic harmful fungi, wherein said composition comprises at least one compound according to claim 1 and at least one extender and/or surfactant.

6. A bis(difluoromethyl)pyrazole derivative according to claim 1 for controlling phytopathogenic harmful fungi.

7. Process for producing a composition for controlling phytopathogenic harmful fungi, comprising mixing a bis(difluoromethyl)pyrazole derivative according to claim 1 with at least one extender and/or surfactant.

8. A compound according to claim 1 that is suitable for treatment of transgenic plants.

Assignments (4)
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Nov 2, 2018
From: BAYER INTELLECTUAL PROPERTY GMBH
To: BAYER CROPSCIENCE AKTIENGESELLSCHAFT
Reel/Frame 047403/0243 →
CORRECTIVE ASSIGNMENT TO CORRECT THE ASSIGNEE ADDRESS PREVIOUSLY RECORDED AT REEL: 034892 FRAME: 0286. ASSIGNOR(S) HEREBY CONFIRMS THE ASSIGNMENT. Recorded Feb 19, 2015
From: BAYER CROPSCIENCE AG
To: BAYER INTELLECTUAL PROPERTY GMBH
Reel/Frame 035071/0680 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Feb 4, 2015
From: BAYER CROPSCIENCE AG
To: BAYER INTELLECTUAL PROPERTY GMBH
Reel/Frame 034892/0286 →
ASSIGNMENT OF ASSIGNOR'S INTEREST Recorded Jan 31, 2012
From: TSUCHIYA, TOMOKI, DR.; WASNAIRE, PIERRE, DR.; HOFFMANN, SEBASTIAN, DR.; CRISTAU, PIERRE, DR.; SEITZ, THOMAS, DR.; KLUTH, JOACHIM, DR.; HILLEBRAND, STEFAN, DR.; BENTING, JUERGEN, DR.; PORTZ, DANIELA, DR.; WACHENDORFF-NEUMANN, ULRIKE, DR.
To: BAYER CROPSCIENCE AG
Reel/Frame 027626/0229 →