RU96120072A - DERIVATIVES 2- (4-PYRAZOLYLOXY-Pyrimidin-5-IL) -CATTY ACID AND METHOD FOR THEIR PRODUCTION - Google Patents

DERIVATIVES 2- (4-PYRAZOLYLOXY-Pyrimidin-5-IL) -CATTY ACID AND METHOD FOR THEIR PRODUCTION

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Publication number
RU96120072A
RU96120072A RU96120072/04A RU96120072A RU96120072A RU 96120072 A RU96120072 A RU 96120072A RU 96120072/04 A RU96120072/04 A RU 96120072/04A RU 96120072 A RU96120072 A RU 96120072A RU 96120072 A RU96120072 A RU 96120072A
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Russia
Prior art keywords
formula
methyl
compound according
chlorophenyl
compounds
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RU96120072/04A
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Russian (ru)
Inventor
Мартин Эберле
Клеменс Ламберт
Фриц Шауб
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Новартис Аг
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Publication of RU96120072A publication Critical patent/RU96120072A/en

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Claims (16)

1. Соединение формулы I
Figure 00000001

в которой R1 - водород, С1-4алкил, С1-4алкокси, С1-С4алкилтио, С3-С6циклоалкил, или ди-С1-4алкиламин;
R2 - водород, С1-4алкил, С1-4алкокси, С1-С4алкилтио или ди-С1-4алкиламино;
R3 - водород или метил;
R4 - арил, арил-С1-4алкил, гетероарил или гетероарилС1-4алкил, в которых каждое из ароматических колец может быть факультативно замещенным;
Х - СН-группа или азот.1. The compound of formula I
Figure 00000001

in which R 1 is hydrogen, C 1-4 alkyl, C 1-4 alkoxy, C 1 -C 4 alkylthio, C 3 -C 6 cycloalkyl, or di C 1-4 alkylamine;
R 2 is hydrogen, C 1-4 alkyl, C 1-4 alkoxy, C 1 -C 4 alkylthio or di-C 1-4 alkylamino;
R 3 is hydrogen or methyl;
R 4 - aryl, aryl-C1-4alkyl, heteroaryl or geteroarilS 1-4 alkyl, in which each of the aromatic rings may be optionally substituted;
X is a CH group or nitrogen. 2. Соединение согласно п.1, отличающееся тем, что ароматические кольца в R4 являются факультативно замещенными одним, двумя или тремя радикалами, выбранными из группы: галоген, С1-4алкокси, С1-4алкил, С1-4галоалкил, С1-4галоалкоксил, С1-4алкилтио, циан, фенил, феноксил, нитро, или группой - С(СН3)=N-O-С1-4алкил.2. The compound according to claim 1, characterized in that the aromatic rings in R 4 are optionally substituted by one, two or three radicals selected from the group: halogen, C 1-4 alkoxy, C 1-4 alkyl, C 1-4 haloalkyl , C 1-4 haloalkoxy, C 1-4 alkylthio, cyan, phenyl, phenoxyl, nitro, or - C (CH 3 ) = NO - C 1-4 alkyl. 3. Соединение по п.1 или 2, в котором R1 - метил, этил или циклопропил.3. The compound according to claim 1 or 2, in which R 1 is methyl, ethyl or cyclopropyl. 4. Соединение по п.1 или 2, в котором R2 - метил или метоксил.4. The compound according to claim 1 or 2, in which R 2 is methyl or methoxy. 5. Соединение по п.1 или п.2, отличающееся тем, что пиразольное кольцо связано с кислородным мостиком в 3 или 4 позиции. 5. The compound according to claim 1 or claim 2, characterized in that the pyrazole ring is connected to the oxygen bridge in 3 or 4 positions. 6. Соединение по п. 1 или 2, отличающееся тем, что R4-хлорфенил, дихлорфенил, фтор - фенил, метил-хлорфенил, трифторметилфенил, трифторметил-хлорфенил, дифторметоксифенил, трифторметоксифенил, метилфенил или диметилфенил.6. The compound according to claim 1 or 2, wherein R 4 is chlorophenyl, dichlorophenyl, fluoro is phenyl, methyl chlorophenyl, trifluoromethylphenyl, trifluoromethyl chlorophenyl, difluoromethoxyphenyl, trifluoromethoxyphenyl, methylphenyl or dimethylphenyl. 7. Соединение по п.1, отличающееся тем, что R1 и R2 - метил, R4-хлорфенил, дихлорфенил, фтор - фенил, метил-хлорфенил, трифторметилфенил, трифторметил-хлорфенил, дифторметоксифенил, трифторметоксифенил, метилфенил или диметилфенил.7. The compound according to claim 1, wherein R 1 and R 2 are methyl, R 4 -chlorophenyl, dichlorophenyl, fluorine-phenyl, methyl chlorophenyl, trifluoromethylphenyl, trifluoromethyl-chlorophenyl, difluoromethoxyphenyl, trifluoromethoxyphenyl, methylphenyl or dimethylphenyl. 8. Соединение по п.7, отличающееся тем, что Х - является СН. 8. The compound according to claim 7, characterized in that X - is CH. 9. Соединение по п.1, выбранное из группы:
метил 2-[2,4-диметил-6-(1-(3-трифторметилфенил)-1Н-пиразол-3-илоксил)-пиримидин-5-ил]-3-метоксиакрилат;
метил 2-[2,4-диметил-6-(1-(3,5-диметилфенил)-1Н-пиразол-4-илокси)-пиримидин-5-ил]-3-метоксиакрилат;
метил 2-[2,4-диметил-6-(1-(5-хлор-2-метилфенил)-1Н-пиразол-3-илокси)-пиримидин-5-ил]-3-метоксиакрилат; и
метил 2-[2-метил-4-метокси-6-(1-(5-хлор-2-метилфенил)-1Н-пиразол-3-илокси)-пиримидин-5-ил]-3-метоксиакрилат.9. The compound according to claim 1, selected from the group:
methyl 2- [2,4-dimethyl-6- (1- (3-trifluoromethylphenyl) -1H-pyrazol-3-yloxy) -pyrimidin-5-yl] -3-methoxyacrylate;
methyl 2- [2,4-dimethyl-6- (1- (3,5-dimethylphenyl) -1H-pyrazol-4-yloxy) -pyrimidin-5-yl] -3-methoxyacrylate;
methyl 2- [2,4-dimethyl-6- (1- (5-chloro-2-methylphenyl) -1H-pyrazol-3-yloxy) -pyrimidin-5-yl] -3-methoxyacrylate; and
methyl 2- [2-methyl-4-methoxy-6- (1- (5-chloro-2-methylphenyl) -1H-pyrazol-3-yloxy) -pyrimidin-5-yl] -3-methoxyacrylate. 10. Способ борьбы с фитопатогенными грибками, заключающийся в обработке грибков или мест их распространения фунгицидно эффективным количеством соединения формулы I согласно п.1. 10. A method of combating phytopathogenic fungi, which consists in the treatment of fungi or their distribution sites with a fungicidally effective amount of a compound of formula I according to claim 1. 11. Фунгицидный состав, содержащий соединение формулы I по п.1 и приемлемый в сельском хозяйстве разбавитель. 11. A fungicidal composition containing a compound of formula I in accordance with claim 1 and an agriculturally acceptable diluent. 12. Способ получения соединения формулы I по п.1, отличающийся тем, что включает О-метилирование соединения формулы II
Figure 00000002

в которой R1, R2, R3, R4 и Х - определенные в п.1.12. The method of obtaining the compounds of formula I according to claim 1, characterized in that it includes O-methylation of the compounds of formula II
Figure 00000002

in which R 1 , R 2 , R 3 , R 4 and X are as defined in claim 1. 13. Соединения формулы II
Figure 00000003

в которой R1, R2, R3, R4 и Х - определенные для формулы I в п.1.13. Compounds of formula II
Figure 00000003

in which R 1 , R 2 , R 3 , R 4 and X are as defined for formula I in claim 1. 14. Соединения формулы III
Figure 00000004

в которой R1, R2, R3, R4 - определенные для формулы I в п.1.14. The compounds of formula III
Figure 00000004

in which R 1 , R 2 , R 3 , R 4 - defined for formula I in paragraph 1. 15. Соединения формулы IX
Figure 00000005

в которой R1, R3 и R4 - определенные для формулы I в п.1.15. The compounds of formula IX
Figure 00000005

in which R 1 , R 3 and R 4 - defined for formula I in claim 1. 16. Способ получения соединения формулы V
Figure 00000006

в которой R4 - арил или гетероарил, причем каждый факультативно замещенный как определено в п.1, включающий окисление арил или гетероарилпиразолидона формулы XI
Figure 00000007

в которой R4-арил или гетероарил, причем каждый факультативно замещен окисляющим агентом, in situ полученным из H2O2 и катализатора.16. The method of obtaining the compounds of formula V
Figure 00000006

in which R 4 is aryl or heteroaryl, each optionally substituted as defined in claim 1, including oxidation of the aryl or heteroarylpyrazolidone of formula XI
Figure 00000007

in which R 4 -aryl or heteroaryl, each optionally substituted with an oxidizing agent, in situ derived from H 2 O 2 and a catalyst.
RU96120072/04A 1995-09-28 1996-09-26 DERIVATIVES 2- (4-PYRAZOLYLOXY-Pyrimidin-5-IL) -CATTY ACID AND METHOD FOR THEIR PRODUCTION RU96120072A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
GB9519787.7 1995-09-28

Publications (1)

Publication Number Publication Date
RU96120072A true RU96120072A (en) 1999-02-20

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