SI20356B - 2-piridilmetilaminski derivati uporabni kot fungicidi - Google Patents
2-piridilmetilaminski derivati uporabni kot fungicidi Download PDFInfo
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- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
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- A61K31/4402—Non condensed pyridines; Hydrogenated derivatives thereof only substituted in position 2, e.g. pheniramine, bisacodyl
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/24—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with substituted hydrocarbon radicals attached to ring carbon atoms
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- C07D213/42—Radicals substituted by singly-bound nitrogen atoms having hetero atoms attached to the substituent nitrogen atom
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- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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- C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
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Abstract
Spojine s formulo (I) in njihove soli kot fitopatogeni fungicidi, kjer je A1 substituiran 2-piridil; je A2 po izbiri substituiran fenil, je L-(C=O)-,-SO2- ali -(C=S)-; je R1 vodik, po izbiri substituiran alkil ali acil; in je R2 vodik ali po izbirisubstituiran alkil, so uporabni fitopatogeni fungicidi.
Claims (20)
1 Patentni zahtevki 1. Uporaba spojin s formulo I in njihovih soli kot fitopatogenih fungicidov R2
R1 kjer je A1 2-piridil, ki je substituiran z do štirimi substituenti, ki so izbrani neodvisno drug od drugega, in so halogen; hidroksi; ciano; nitro; SF5; trialkilsilil; amino skupina, ki je po izbiri substituirana z enim ali dvema E ali acilnima skupinama, pri čemer je vsak izmed njih lahko enak ali različen; acil; skupina E, OE ali SE, kjer je E alkil, alkenil, alkinil, cikloalkil, cikloalkenil, fenil ali heterociklil, pri čemer je vsak izmed njih po izbiri substituiran s halogenom, ciano, alkoksi, alkiltio, merkapto, hidroksi, nitro, amino, acilom, aciloksi, aciltio, fenilom, heterociklilom, feniltio, fenoksi, heterocikliloksi ali heterocikliltio; ali skupina -C(E)=N-Q, kjer je Q E, OE, SE ali amino skupina, po izbiri substituirana z enim ali dvema E ali acilnima skupinama, pri čemer je vsak izmed njih lahko enak ali različen; dva sosednja substituenta skupaj z atomi, na katere sta vezana, lahko tvorita obroč, ki lahko vsebuje do 3 heteroatome; je A2 fenil, ki je po izbiri substituiran z do 5 substituenti, ki so izbrani neodvisno drug od drugega in so halogen; hidroksi; ciano; nitro; SF5; trialkilsilil; amino skupina, ki je po izbiri substituirana z enim ali dvema E ali acilnima skupinama, pri čemer je vsak izmed njih lahko enak ali različen; acil; skupina E, OE ali SE, kjer je E alkil, alkenil, alkinil, cikloalkil, cikloalkenil, fenil ali heterociklil, pri čemer je vsak izmed njih po izbiri substituiran s halogenom, ciano, alkoksi, alkiltio, 2 merkapto, hidroksi, nitro, amino, acilom, aciloksi, aciltio, fenilom, heterociklilom, feniltio, fenoksi, heterocikliloksi ali heterocikliltio; ali skupina -C(E)=N-Q, kjer je Q E, OE, SE ali amino skupina, po izbiri substituirana z enim ali dvema E ali acilnima skupinama, pri čemer je vsak izmed njih lahko enak ali različen; dva sosednja substituenta skupaj z atomi, na katere sta vezana, lahko tvorita obroč, ki lahko vsebuje do 3 heteroatome. je L -(C=0)-, -S02- ali -(C=S)-; je R1 vodik, alkil, ki je po izbiri substituiran z alkoksi, haloalkoksi ali alkiltio, pri čemer vsak vsebuje od 1 do 5 ogljikovih atomov, halogen ali fenil; ali acil; in λ je R vodik ali alkil, ki je po izbiri substituiran z alkoksi, haloalkoksi ali alkiltio, pri čemer vsak vsebuje od 1 do 5 ogljikovih atomov, halogen ali fenil.
2. Uporaba po zahtevku 1, označena s tem, da je 2-piridilna skupina A1 substituirana z do dvema substituentoma.
3. Uporaba po zahtevku 2, označena s tem, da je 2-piridilna skupina A1 substituirana v položaju 3 in/ali 5.
4. Uporaba po kateremkoli izmed zahtevkov od 1 do 3, označena s tem, da je 2-piridilna skupina A1 substituirana z alkoksi, alkilom, ciano, halogenom, nitro, alkoksikarbonilom, alkilsulfinilom, alkilsulfonilom ali trifluorometilom.
5. Uporaba po zahtevku 4, označena s tem, da je 2-piridilna skupina A1 substituirana s klorom in/ali trifluorometilom. 3
6. Uporaba po kateremkoli izmed zahtevkov od 1 do 5, označena s tem, da je fenilna skupina A2 substituirana z do tremi substituenti.
7. Uporaba po zahtevku 6, označena s tem, da je fenilna skupina A2 substituirana z do dvema substituentoma.
8. Uporaba po kateremkoli izmed zahtevkov od 1 do 7, označena s tem, da je fenilna skupina A2 substituirana z alkoksi, alkilom, halogenom, nitro ali trifluorometilom.
9. Uporaba po kateremkoli izmed zahtevkov od 1 do 8, označena s tem, da je L -(OO)-.
10. Uporaba po kateremkoli izmed zahtevkov od 1 do 9, označena s tem, da je R1 vodik.
11. Spojina s formulo I in njene soli A 1
(D R1 kjer je A1 2-piridil, ki ima substituente na položaju 3 in/ali 5, ki so izbrani neodvisno drug od drugega, in so halogen; hidroksi; ciano; nitro; SF5; trialkilsilil; amino skupina, kije po izbiri substituirana z enim ali dvema E ali acilnima skupinama, pri čemer je vsak izmed njih lahko enak ali različen; acil; skupina E, OE ali SE, kjer je E alkil, alkenil, alkinil, cikloalkil, cikloalkenil, fenil ali heterociklil, pri čemer je vsak izmed njih po izbiri substituiran s halogenom, ciano, alkoksi, alkiltio, merkapto, hidroksi, nitro, amino, acilom, aciloksi, aciltio, fenilom, heterociklilom, feniltio, fenoksi, 4 heterocikliloksi ali heterocikliltio: ali skupina -C(E)=N-Q, kjer je Q E, OE, SE ali amino skupina, po izbiri substituirana z enim ali dvema E ali acilnima skupinama, pri čemer je vsak izmed njih lahko enak ali različen; dva sosednja substituenta skupaj z atomi, na katere sta vezana, lahko tvorita obroč, ki lahko vsebuje do 3 heteroatome; je A fenil, ki je po izbiri substituiran z do 5 substituenti, ki so izbrani neodvisno drug od drugega in so halogen; hidroksi; ciano; nitro; SF5; trialkilsilil; amino skupina, ki je po izbiri substituirana z enim ali dvema E ali acilnima skupinama, pri čemer je vsak izmed njih lahko enak ali različen; acil; skupina E, OE ali SE, kjer je E alkil, alkenil, alkinil, cikloalkil, cikloalkenil, fenil ali heterociklil, pri čemer je vsak izmed njih po izbiri substituiran s halogenom, ciano, alkoksi, alkiltio, merkapto, hidroksi, nitro, amino, acilom, aciloksi, aciltio, fenilom, heterociklilom, feniltio, fenoksi, heterocikliloksi ali heterocikliltio; ali skupina -C(E)=N-Q, kjer je Q E, OE, SE ali amino skupina, po izbiri substituirana z enim ali dvema E ali acilnima skupinama, pri čemer je vsak izmed njih lahko enak ali različen; dva sosednja substituenta skupaj z atomi, na katere sta vezana, lahko tvorita obroč, ki lahko vsebuje do 3 heteroatome. je L -(C=0)-, -S02- ali -(OS)-; sta R1 in R2 vodik.
12. Spojina po zahtevku 11, označena s tem, da je 2-piridilna skupina A1 substituirana z alkoksi, alkilom, ciano, halogenom, nitro, alkoksikarbonilom, alkilsulfmilom, alkilsulfonilom ali trifluorometilom.
13. Spojina po zahtevku 12, označena s tem, daje 2-piridilna skupin A1 substituirana s klorom in/ali trifluorometilom. 5
14. Spojina po zahtevku 13, označena s tem, daje 2-piridilna skupina A1 2-(3-kloro-5-trifluorometil)piridil.
15. Spojina po kateremkoli izmed zahtevkov od 11 do 14, označena s tem, daje L (CK)).
16. Spojina po kateremkoli izmed zahtevkov od 11 do 15 , označena s tem, daje fenilna skupina A substituirana s halogenom.
17. Pesticidni sestavek, ki obsega spojine, kot so definirane v kateremkoli izmed zahtevkov od 11 do 16 v zmesi z agrikulturno sprejemljivim razredčilom ali nosilcem.
18. Postopek za zatiranje fitopatogenih gliv na lokusu, ki je inficiran ali je nagnjen k infekciji z njimi, označen s tem, da obsega nanašanje na lokus spojine s formulo I, kot je definirana v kateremkoli izmed zahtevkov od 1 do 10 ali v kateremkoli od zahtevkov od 11 do 16.
19. Postopek za pripravo interemediatnih spojin s formulo Ha
H (Ha) ki obsega stopnje: a) presnovo, pod bazičnimi pogoji, spojin s formulo IV s spojinami s formulo V, da dobimo intermediate s formulo VI, 6
(VI) (IV) (V) b) pretvorbo intermediatov s formulo VI v intermediate s formulo VII,
m c) pretvorbo intermediatov s formulo VII v spojine s formulo Ha,
(VII) (Ha) kjer sta Ra in Rb, ki sta lahko enaka ali različna, alkil, alkenil, alkinil, cikloalkil, cikloalkenil, heterociklil ali fenil, pri čemer je vsak od njih lahko substituiran; (prednostno po izbiri substituiran fenil): je E1 tako elektron odvzemna skupina kot skupina, ki je lahko nadomeščena z vodikom ob uporabi metodologije, znane usposobljenemu kemiku, skladno s stopnjo c); (prednostno karboksi skupina ali karboksi estrska skupina); je X1 odhodna skupina; in je A1 kot je definiran v zahtevku 11.
20. Kot intermediati, spojine s formulo Ilb in njihove soli, 7 A V /NH2 R1 (llb) kjer je A1 kot je definiran v zahtevku 11 in je R1 alkil, kije po izbiri substituiran z alkoksi, haloalkoksi ali alkiltio, pri čemer vsak vsebuje od 1 do 5 ogljikovih atomov, halogen ali fenil, pod pogojem, da kadar je A1 2-(5-n-butil)-piridil, potem R1 ni etil; spojina (llb) ni l-amino-5-etoksi-l-(3-metil-2-piridil)pentan; spojina (llb) ni l-amino-5-etoksi-l-(5-metil-2-piridil)pentan; spojina (llb) ni l-amino-4-etoksi-l-(3-metil-2-piridil)butan; in spojina (llb) ni l-amino4-etoksi-l-(5-metil-2-piridil)butan.
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| GBGB9803413.5A GB9803413D0 (en) | 1998-02-19 | 1998-02-19 | Fungicides |
| GBGB9813998.3A GB9813998D0 (en) | 1998-06-30 | 1998-06-30 | Fungicides |
| GBGB9817353.7A GB9817353D0 (en) | 1998-08-11 | 1998-08-11 | Fungicides |
| PCT/GB1999/000304 WO1999042447A1 (en) | 1998-02-19 | 1999-02-16 | 2-pyridylmethylamine derivatives useful as fungicides |
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| Publication Number | Publication Date |
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| SI20356A SI20356A (sl) | 2001-04-30 |
| SI20356B true SI20356B (sl) | 2008-04-30 |
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| Application Number | Title | Priority Date | Filing Date |
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| SI9920016A SI20356B (sl) | 1998-02-19 | 1999-02-16 | 2-piridilmetilaminski derivati uporabni kot fungicidi |
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| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
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- 1999-02-16 UA UA2000095275A patent/UA72204C2/uk unknown
- 1999-02-16 WO PCT/GB1999/000304 patent/WO1999042447A1/en not_active Ceased
- 1999-02-16 JP JP2000532399A patent/JP4749542B2/ja not_active Expired - Lifetime
- 1999-02-16 DE DE69937633T patent/DE69937633T2/de not_active Expired - Lifetime
- 1999-02-16 RS YUP-514/00A patent/RS50017B/sr unknown
- 1999-02-16 SK SK1239-2000A patent/SK286310B6/sk not_active IP Right Cessation
- 1999-02-16 KR KR1020007009044A patent/KR100603172B1/ko not_active Expired - Lifetime
- 1999-02-16 ID IDW20001839A patent/ID26626A/id unknown
- 1999-02-16 NZ NZ505954A patent/NZ505954A/xx not_active IP Right Cessation
- 1999-02-16 ES ES99904953T patent/ES2293717T3/es not_active Expired - Lifetime
- 1999-02-16 DK DK99904953T patent/DK1056723T3/da active
- 1999-02-16 EP EP99904953A patent/EP1056723B1/en not_active Expired - Lifetime
- 1999-02-16 TR TR2001/01071T patent/TR200101071T2/xx unknown
- 1999-02-16 CN CN998030589A patent/CN1132816C/zh not_active Expired - Lifetime
- 1999-02-16 RO ROA200000790A patent/RO120970B1/ro unknown
- 1999-02-16 IL IL13757399A patent/IL137573A0/xx active IP Right Grant
- 1999-02-16 US US09/622,651 patent/US6503933B1/en not_active Expired - Lifetime
- 1999-02-16 BR BRPI9908007-9B1A patent/BR9908007B1/pt active IP Right Grant
- 1999-02-16 CA CA002319005A patent/CA2319005C/en not_active Expired - Lifetime
- 1999-02-16 CZ CZ20002993A patent/CZ298746B6/cs not_active IP Right Cessation
- 1999-02-16 PT PT99904953T patent/PT1056723E/pt unknown
- 1999-02-23 AR ARP990100655A patent/AR017459A1/es active IP Right Grant
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2000
- 2000-07-28 IL IL137573A patent/IL137573A/en not_active IP Right Cessation
- 2000-08-18 NO NO20004159A patent/NO317105B1/no not_active IP Right Cessation
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2002
- 2002-11-25 US US10/303,464 patent/US6828441B2/en not_active Expired - Lifetime
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2006
- 2006-02-09 IL IL173648A patent/IL173648A/en not_active IP Right Cessation
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| IF | Valid on the event date | ||
| SP73 | Change of data on owner |
Owner name: BAYER CROPSCIENCE LIMITED; GB Effective date: 20071004 |
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| OU02 | Decision according to article 73(2) ipa 1992, publication of decision on partial fulfilment of the invention and change of patent claims |
Effective date: 20080228 |