LV10074B - Substituted bicycloheptandione derivatives - Google Patents

Substituted bicycloheptandione derivatives Download PDF

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Publication number
LV10074B
LV10074B LVP-92-613A LV920613A LV10074B LV 10074 B LV10074 B LV 10074B LV 920613 A LV920613 A LV 920613A LV 10074 B LV10074 B LV 10074B
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quot
rpynny
substituted
iii
cmc
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LVP-92-613A
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LV10074A (lv
Inventor
Akiyoshi Ueda
Shigemi Suga
Hiroyuki Adachi
Toshio Aihara
Kazuyuki Tomida
Hideki Yamagishi
Hideo Hosaka
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Nippon Soda Co
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Publication of LV10074A publication Critical patent/LV10074A/lv
Publication of LV10074B publication Critical patent/LV10074B/lv

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    • C07D213/00Heterocyclic 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
    • C07D213/02Heterocyclic 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
    • C07D213/04Heterocyclic 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
    • C07D213/60Heterocyclic 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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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Pyridine Compounds (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
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Description

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Bci ΜΗΟΓΜΧ CnyM39X npM BbipamUBaHMM CenbCK0XP3iU'ilCTGSHHblX M canoBbix &lt;ynbTyp, nns 5opb5bi c copHanaMu c uenbva bkohommm 3aTpa7 Tpyna na υημμτοχθημβ cpphskog b nonsix, ncnonb3yioTCsi 3HanMTenbHbte κ o nu m e c r b a pa3HPo6pa3Hbix repSuunaoB. Οαηθκο, b Ηεκοτορωχ cnyMa9x, 2 φΜτοτοκcMMHocTb rep6nuMAoe μοχθτ HāHecīn epea KynbTypaH, μπμ repOMUMflbi, odaramnecs Ha nonsix, noryT npMBecTM k 3arps3HeHmo 0icpyxa«3mepi cpeflbi.
Banay βτογο saxHO« προδπθΜοη aanstercii pa3pa6oTKa χκμμηθοκμχ coeAMHeHMPt, o6nanatcmnx BbicoKOPi 3qnpeKTMBHOCTbio n 5onbiuepi
SesonacHocTbio nna Mfl8KonnTaiomMX. nepeneHb w38ecTHbix naTemoB, pacKpbiBaioiUMX coenMHeHMSi, awanorwMHbie coeanH8HMSM η3ηηογο Μ3θδρβτθΗΜ5ΐ, SKnmHaeT EsponePiCKMH Π3Τ6ΗΤ 137963, t!BponGPfCKMi/i naT9HT 185191, EBponencKMPi naTeHT 136118, EsponeHCSCHfl naTeHT 186119, EBponeiacKMfl naTeHT 186120, Βποηοκμη oTKpbiTbitf naTeHT Nr, Sho 62- 133 146, EeponeHCKHtf naTeHT 278907, EsponeiacKMH naTeHT 2S8795 h EsponeiacKHtf naTeHT 264737.
CoenMHeHMS «aHHoro n2o5peTeHM$i BKmoHSHbi b φορΜνην Μ3θδρθΤ8ΗΜ5ΐ naTeHTa ΦΡΓ 39028 18 /coo rseTCTByiomnižf naTeHTy BenMKo6pnTaHWM 2215333 h SnoHCKOMy οτκpbiτοhy naTenTy Nr. Hei 2-1422/. B onMcaHMH 3Τ0Γ0 naTeHTa οοθημηθημη aaHHoro M3o6peTSHn?i He ο n h c a h bi.
UenbK) ηηηογο μ 3 ο 6 ρ e τ e η m si nsnsieTcsi pa3pa5oTtca rep5nunflOB, Koropbie xapaKTepw3yioTC5i npenMVnecTsaHM e τθχηοαογμμ mx cnnTe3a 8 npoMbiuineHHOM m a c ω τ a 5 s , oānanaioT Tpe5yeMOH ΒφφθΚΤΜΒΗοετΒίο ηρκ MeHbUieia fi03npoBxe, čeaonacHbi μ μμθιοτ xopouiyio ceneKTMBHOCTb no oTHOuieHMio ii KynbTypnbiM pacTeHMStM,
PacKDbITHe CVU1HOCTM H305DeTeHH9l flaHHoe M3o5peTeHne othocmtcs k 3aMemeHHbiM npoM380AHbiM SMUHKnorenTaflHOHa, μμθιοιαμμ HMxecnenyKiiuyio (popMyny /1/:
/rfle R1 npeflCTaBnaeT co6ofl HH3uiyio ajiKHJibHyto rpynny, &lt;I&gt;eHHJibHyto r.pynny/ KOTopan μοκθτ 6biTb 3aMemeHH0ft, apaaKHJibHyio rpynny# KOTopaa MoateT 6biTb 3aMeiueHHofi, hjih reTepouHKnHMecKyto rpynny, KOTopan MoaceT CbiTb 3aMemeHH0ft; R2 MoryT 6biTb oa,hhaκobbiMη hnu pa3HbiMH h npeflCTaBJiHJOT codoft aTOMbi ra/ioreHa, aiiKOKCnrpynny, ajiKnnTnorpynny, anκHπcyπbφoHHπbHy»3 LV10074 rpynny, anKnnbHyio rpynny, anKOKCnanKnnbHyio rpynny linu a/iKOKCMKap5oHMnbHyK) rp.ynny, m npnuMMaeT 3HaqeHnsi ot 0 no 4; R3 H R* MOryT 6bITb OflMHaKOBbIMH ΗΠΗ pa 3HblMH H IipeflCTaBJIiliOT coCofl aTOMbi Boflopofla ηλη ηη31ιιηθ ajiKHJībHbie rpynnbi/, h k hx cojihm. yKa3aHHbie 33M8CTMTenM φθημ^ηορι, apamcunbHOPi m reTepoiļHKnHMeCKOfl rpynn B R1 MOryT 6bITb OflHHaKOBbIMH HJIH pa3HblMH, H npeflCTaB^fliOT co6ofl aTOMbi raaoreHOB, rn,npoKCH.nbHyīo rpynny/
Hmporpynny, unaηorpyη πy, aiunnbHyiū, a η κ e h h π b h y ra , r a π o r e η ο a n k n n b h y la, r a η o r e ι-ι o a η κ e η μ n b h y io, anKOKCn, r a η o r e η o a η κ ο κ c n , rarioreHoanKSHKnoKCM, anKunīno, a/iKennriTno, amcnHH/rruo, ranoreHoanKMfiTno, ranoreHoamceHunTMO, MOHoanKunamiHO, anicoKcnanKunTMO, antinnTUoanKunTUO, anKOKcnKapSoHHiibHyid, anKnnKap60HMfianK0&lt;CM, anKmiKap5oHnnbHyici, an&lt;0KCK3MHH0, anKnncynb(pOHMnbHyKi, anKeHnncynbi|ioHMJibHy(a, anio/iHuncynbņoHnribHyK), ariKo:&lt;cMantinncynbipOHnnbHyto, ariKtiflTHoanKHflcynbņoHnnbHyiū, anKnricynbņoHHiian,&lt;Mncynbi?oHnnbHyra1 ranorBHoani&lt;MncynbipoHMnbHyHJ, ariKOKCMKapSū n μ(13Πκμπτμο , anKOKCHKap5oHnnaniinncynb&lt;pwHMnbHyio, anKOKCMKap5oHnnanKnncynbipoHMnbHyio, ariKunaMuno, n apama/ui0Kcnrpynny, (peHMnbnyio rpynny, KOTopasi μοχθτ 5biTb 3aMemeHH0«, apanKnnbnyK) rpynny, KOTopaa Mcxer 6biTb 3aMeuieHH0K, rerepouMicnMMecKyιο rpynny, KOTOpag μ'οχετ 6biTb saMeiuenHOK, m anKtirtbHyio rpynny, 3aMemeHHyio rerepoiiHKnuMecKoti rpynnow, KOTopas, 8 cboki oqepenb, μοχθτ 5biTb 3 a m e ui 8 H h o w . yKa3aHHafl reTepoumcnuMecKasi rpynna sKniūMaer s ce5si TaKne rpynnbi, κ a κ nupiinunbuaa, nupuMHnunbHafl, TMeHMnbHaa, ņypnnbHasi, nupasonunbHasi, nnpponiinbHasi, MMnna30iinnbHasi, niipMna3MHwnbHasi, nwpa3HHMnbHaa, MHnonunbHaa n n p y r κ e .
CoanMHeHMei naHHoro M3o6peTeHMsi oSnanaioT BbicoKon repSnuunHOK aκτw8ηocτbto b ycno8H9X B03BbiuieHH0w MecTHOCTM tcaK npn o5pa5oTKe mmm noMBbi, τ a κ κ npn o6pa5oTKe mmm η m c t 8 bi pacīeHnn. Ohm ο q e h b ΒφφβΚΤΜΒΗω G Sopb5e C pa3flWMHblMM 8 H fl 3 Μ M C0PH3K0B, Π p 0 H 3 Ρ a C T a (0 φ H X Ha 8038biiueHH0CT5ix, τ a κ n μ μ κβκ, Hanputiep, non3yMun c o p H S K , pncoBasi ocoica, nnMnoxapnc m neSena 6 e n a a , · ocoSeHHO npn o5pa6oiKe hmh HenocpencTseHHO nncTSbi ρβετθΗΐιΐλ nyTeH pa36pbi3rnsaHiia. HeicoTopbie U3 3tmx coeniiHeHMPi o5nanaioT ceneKTHBHOCTbra no οτηοιιιθηιιιο k KyribTypHbiM pacTGHusiM, TaicuM KaK, HanpuMep, nioeHHua n coa KynbtypHaa. H e κ ο τ o p bi e H3 a τ n x coenHHeHnn b bi 3 bi b a ίο τ 3aiienneHne p o c τ a
CenbCK0X03SI?iCTBeHHblX K y Π b T y p , ne&lt;0paTHBHblX ΚΟΜΗΒΤΗΜΧ paCTeHMH M qipyKTOBbix nepeebeB. .
HeKOTopbie H3 btux coenuhehha oSnanaiūT τβκχθ BbicoKOPi certeKTUBHOcTbra no οτηοιιιθημώ k pwcy w EbicoKon repSnuunHo^ aKTMBHOCTblfl ΠΟ Ο T H 0 U16 H H K) K npOCy KypMHOMy , ΗΘΠΚΟΜΒΘΤΗΟΡί CbITl/i 0MspenH0LļB8TH0Pi, CTpenonMCTy i/i sinoHCKOMy κ a μ w iu y , h τ . a . B ηοδβΒΠθΗΜθ &lt; Bbiiuecxa3aHH0My, coeAMHeHMa naHHoro M3o5pereHU3 MoryT δbiTb ncnonb30BaHbi nnsi 6opb6bi c copHstKaMM c raKnx M8CTax, xa&lt; qipyKT08bie canbi, ra30Hbi, ο6ομμημ xene3Hbix nopor, nycTouin m t.r.
Han6onee npennomMTenbHbiPi cnoco6 ocymecTeneHM5i M3o6peTeHMfl
CoennHeHMSi naHHoro M3o6peTeHM9 nonyMaiūT cn8ayramnMM cnoco6aMW.
Cnoco6 nonvMeHna /a/ 1 H ΗΜΘΚ3Τ Τθ 5ΚΘ 3Ha^eHHH, MTO H OnpeReJieHHbie
Bbiuie, a Q npeflCTaBnaeT coCoft yxofl«myio rpynny/. B 3tom cnoco6e coejtHHeHHe /1/ noRyuaK)T cneRj'BDiRHM o6pa30M: coeflHHeHHe /11/ pearnpyeT b pacTBopHTene b npncyTCTBHn 2-χ \iojiefl hjih H36biToqHoro ko Jiim e c tb a ocHOBaHHH πρκ TeMnepaType ot -20°C flG TeMnepaTypbi κ w π e η m s ncnorib3yeMoro pacTBopuTena, npennoMTUTenbHO npn TeMnepaType ot 0°C λο 50°C, b TeneHHe npoMeacyTKa βρθμθηη ot 30 MHHy τ RO ΟΚΟΠΟ 10 H3C0B· yxoflHmafl rpynna Q πρθαοτθβληθτ coGoft aTOM ranoreHa, aRκnπcyπbφoHaτHyκ^ rpynny h φeHHJIcy;IbφoHaτHy^o rpynny.
Hcnonb3ysMbie ocHOBaHua εκπιΟΜβιοτ r i/iapooscMci/t ιαθπομημχ μθτβπποβ, HanpMMep, K 0 H n NaOH, runpooiincM m8noMH038MenbHbix MeTannos, τ p m (C,-C6) anKU/i aMHHbi, πηρη^ηη, , τρβτ-Β OK, Τρητοη Β, .KapfioHaT
HaTpHH, φο οφ3Τ HaTpHH η ημ nofločHbie. Hcno Jib3yeMbie pacTBopHTenii ITpeflCTaBJIHfOT COGoft BOfly, ΟΠΗρΤ, X JIO pH C Tbll3 ΜΘ THJieH , ČeH30JI, TO Jiy 0 J1 , 3THJiapeTaT, αμμθτη,πΦορμθμη,α , ΤΓΦ, λημθτοκοη3Τ8η, atļeTOHHTpmi h nofloāHbie hm pacTBopHTejiH. LV10074
Cnocofi nOJIVMeHHH /&lt;5/
MoH03aMemeHHbie coeflHHeHHfl hs mic/ia coeflHHeHHft λ^μηογο Μ3θ6ρθΤβΗΗΗ, HCKJlKMaH Τβ , y ΚΟΤΟρΜΧ B ΠΟΠΟίΚβΗΗΗ 5 6Η11ΗΚΠΗΜβCKOΓ0 fljīpa HaxoflHTCH aJiKOKCHKap6oHHnbHaH rpynna, MoryT 6biTb nonyMeHbi no cneflyK»meft peaKiļHH.
Ecrtu 3TM coeflMHeHusi conepxaT b πο/ιοχθηιίμ 5 pa3Kbie 33μθοτμτθ(1η /coennHeHusi τΐ/ina (1) /, μπμ conepxaT b nonoxeHnn 5 ohmh 33MecTMTenb / co8flMH8Hnsi τμπ3 (1) /, β u μ κ η ο π p ο π a η o 8 ο m stnpe cyiuecTByH)T CTepeon30MepHbie φοpmw. ripu npaMOM nonyMeHnn coennHeHM« τμπβ (1) s cootb8tct8wk c BbiiueonMcaHHbiM cnocoSoM nonyM8HHsi /a/, o 5 mm η o ofipa3yeTcsi rpaHcmopMa. B 3tom cnocoSe nonyqeHH3 μοχηο pasneiiHTb unc- m TpaHciņopMbi Ha CTanMM (1) . CooTBeTCTByit&gt;utM!a BbiSop cnocoSoB no3Bci/iaeT nonym-iTb τpahc- nnn unc-qiopMy (1)
McxonHoe coennHeHne κ coenuneHne /1/ naHuoro M3o5pereHHsi hmsiot OnTMMĒCKHe M 3 Ο M e p bl , H δ 0 rt b III 0 8 KOflMHeCTBŪ T3yTQM8p08 Μ Ο X 8 T cvmecTBosaTb b cneaynmnx mopMax:
/ ΓβΘ R' , R2 , R3 H R* H HM6IOT Τ Θ ΧΘ 3H θ HH 3 , MTO H Ο Π pefl e ne HHbie Bbiiue/. flaHHoe H3o6peTeHiie 0XBaTbiBaeT TanjKe n ece H30MepHbie h
TayTOfiepHbieņopMbi3TnxcoennH8Hm?i. 6
Ecn n coennH8Hne /1/, nonvMeHHoe BbiuieonncaHHbiM cnocoSoM, cofiepscMT CBo5onHyio rnnpoKcnnbHyio r p y π π y , n 2 3τογο coennHeHns MoryT δbiTb nonyMeHbi ero conn, npneMneMbie ano ncnonb3oeaHnst s centcKOM xo39«C78e n canosoncTes, enaMMHbi n nx ananoru, aKpnnaT, cynb&lt;poHaT, KapSoMaT nnn π p c c τ ο η 3 φ n p .
Conn, npneMneMbie nnst ncnonbsoeaHnsi b cenbCKOM xo38KCT8e n caflOBOūCTee, βκπιομβιοτ conn Harpns, Kanna, Kanbuna, aMMOHns n km nono6Hbie. ΠρηΜβρβΜΜ 3MM0HM«Hbix conen sensticiTCs conn c hohob, η μ e ioinn m qiopMyny N R R R R /rne R , R , R n R , coOTBeTCTeeHHO,
BučupatoT h3 Boflopoaa h anKH^bHbix rpynn, 3aMemeHHbix b HeKOTOpbix cny»iaax, HanpHMep, rHflpoKcmībHOfl rpynnofl/. Ecjih nto6aa H3 rpynn R , R , R n R npeacTasnaeT co5o« saMemeHHyro anKnnbHyra rpynny, ro xenaTenbHO, n r o 6 t.i ara rpynna η m e n a or 1 no 4 a τ ο μ o b yrnepona.
CooTseTCTBymuu'ie enaMnHbi n nx aHanorn npeACTasnsnoT coOon coeflMHeHnst, e κοτορωχ nx OH-rpynnbi npespauieHbi b rpynny ipopMynbi -NR R /rne R npencTaenaeT c ο δ ο n , HanpnMep, anKnnbHyto nnn apnnbHyio rpynny c nncnoM aTOMoa yrnepona ot 1 no 6, KOTOpas b HeKOTopbix cnyMasīx μοχθτ SbiTb aaMemenHon, nnn, HanpnMep, &lt;peHnnbHyKi rpynny, a R npsACTāsnser coSon aTOM sonopona, nnn, HanpnMep, anKnnbHyio nnn apnnbHyio rpynny c nncnoM atOMOB yrnepona ot 1 no 6, KOTopasi b h e η κ ο τ o p bi x c n y m a si χ μοχθτ 5biTb 3aMemeHHon , nnn, HanpnMep, (peHMnbHyra rpynny/, ranoreH nnn rpynny SR /rne R npencTaBnseT co5on TaKy&gt;o x&amp; rpynny, xa&lt; n BbiujeonncaHHasi rpynna R /.
CooTB8TCTByKiuu-ie aKpnnaTHbie npon3BonHbie nnn npocTbie 3pnpbi npencTasnsuoT coSon coennHeHnsi, b KOTopbix nx OH-rpynnbi npeepameHbi, cootbbtctbshho , b rpynny φopMynbι - OCOR nnn b rpynny tp ο p m y n bi -OR /rne R npencTaBnseT co6on τaκyto xe rpynny, κβκ n BbiiueonncaHHaa r p y η π a R / .
CooTBeTCTBy!Oiune KapSaMāTHbie npon3BOflHbie npencTasnaioT οοδοη coennHennsi, s κοτορωχ nx OH-rpynribi npeBpameHbi g rpynny ?opMynbi -QC(0) r R / rne R n R npencTaBnarar co5on, cooTBeTCTseHHP, aTOM sonopona nnn Ty xe rpynny, mto n'BbiuieonncaHHasi rpynna R /.
Bce 3Tn nponssonHbie μοχηο nonynnTb oSbmHbiMn cnocoSaMn. CTpyKTypbi coennHeHnn αβηηογο n3o6peTeHns onpeneneHbi τβκηΜη cnocoāaMn, Kas Hl&lt;-cneKTpocKonnsi, 51ΜP n Macc-cneKTpocKonna. LV10074 flaHHoe M30ūpeT8Ht/fe ηοηροδι·ιο wrimocTpnpyeTCS HHxec/ieuyramnMH npuMepaMM. Π D VIM 8 D 1 3-(2-HHTpo-4-xnop5eH3omi)5nunKno ^4.1.01 renTaH-2,4-awoH /C08flMH6HH8 1 - 9 7/.
C , 5 Γ /1,44 ΜΜΟΠ 9,/ 5-M83HnOKCHMeTHfl-2-( 2-ΗΙΊΤρθ-4-χηορδθΗ30ΜΠ) UMKnoreKcaH-1,3-flMOH3 pacTBopnnn b 15 ηπ 3 t a η ο n a , κ !iOTopoMy π p m nppeMeiUMBaHHM ripu κομηβτηορι TGMri8paType η ο δ a r κ η m 2 μ η βοαηογο pacTBopa runpooKMCH HaTpus /runpaoKMCb Ηβτρνίίΐ: 0,17 r, 4,31 MMons/, n nonyqeHHyra CMecb nepeMsuiMsanu npn κομηητηορι TeMnepaType p τθμθημθ Macoe. Tlocne 3aBGpuieHH?i p e a κ un w pacTBopuTsnb οτογηβπμ. K nonyMeHHOMy ocτaτκy noOasunn 50 μπ arunaueTaTa m 10 μπ soflbi n ri a τογο, MToSbi pacTBopmb 0CT3T0K. 3 a τ e m floSasnanM pa35aeneHHyio consHyra KncnoTy no tsx nop, πακβ βοαημρι cnoti ηθ crar KucnbīM. OpraHUMecKMPi chopi npoMbinn HacbimeHHbiM pacieopoM conu b eone m Bbicymnnn Han cynbqjaTOM Marnna. PacTBopuTerib OTorHann. nonyMeHHbm 0CT3T0K oMMCTunu xpoMaTorpaņnpoBaHMeM h a κ ο η ο η κ e c cunHKarcneM / 3ΠΙ03Τ t χηορορορΜ/ , nony-in8 0,39 r /ebixon: 83%/ uenesoro coennHGHMSi b BHfle neγκηχ KpHCTannoB «enToro ρβθτθ, τ. πη. 132-134°C. 3-(2-xnop“4-MeTMncy/ibpoHnn-3-MeTOiicn5eH30nn)-UMC-5’MeTnn-uMC-δΜρκκηο 4.1.0 renTaH-2,4-flwoH /Οοθπμηθημθ 1-195/. 0 Ο °'/0οΗ5 Cl 0 CKj
CH?
1,13 r /3,6 MMonfl/ 3-(2-xnop-4-M8TaHcynb(poHHfl-3-MeTOKCn5eH30Mn)-TpaHC-5-3TOKcnKap5OHun-i4MC-5-MeTMn-uMC-5Mi4Miino 4.1.0 renTaH-2,4-fiMOHa pacTBopnnn b 7,8 ma /7,8 κμοπθρι/ 1 NaOH npn oxfiaxfleHMM π e a η η ο h soaopi, 3aTeM b e η M p e a k li m to npn κομηβτηορι T8MnepaType b Te^snue 4 nācos. Πο 3aBepuieHMM peatcuMM noBaennn 20 tin nensiHOH eoflbi w 20 Mn 3fnnapeTaTa, npi/t oxnaxneHHM neflaHOia soaopi nposen'/t Hei/iTpartMsauMto IN HC m neKapSoKCunupoEanM. OpraHt/mectcMPt cnoei npOMbinn cciacu?i m s a t 8 μ η h c m iu e η η κι m pacTeopoM conu b eone, m BbicyuiMnM nan cyribtpaTOM MarHMS. PacTeopme/ib ororHann. Οοτβτοκ oMucruinu KonoHūHHūR xpOMaTCirpaņnepf /68H3on:3TMnaueTaT * 5:1/, π ο n y μ m b 0,29 r ueneaoro npofly«Ta b b k a e KpucTannoB Senoro asēta, t. nji. 132-135°C. nony»ieHHaH ijHC“&lt;ī&gt;opMa h TpaHC-ifcopMa, CHHTe3npoBaHHaH cnoco6oM, ii cno Jib30 b aHHbiM b npuMepe 1, 6bIJIH oxapaKTepn30B3Hbi μθτοαομ SIMP. P8npe38HTaTHBHbie npuMepbi coaanneHni^ naHHoro K3o6p9Tem/ist, BKmoMafl cosiļMHSHHa. nonyneHHbie s BbiuienpnseneHHbix npwMepax, n p e a c τ a e n e h bi s T a 5 η m u a x 1-3. R2. npencTaBn^ioT co5ow HnxecnenyiamMe 3aMecTMTertM s ra6nnuax. &quot;TpaHc&quot; n &quot;mmc&quot; g rpape &quot; ipM3wMecKMe CBOPtCTBa&quot; o5o3HaMatoT npocTpaHCTBeHHyra KGHtpnry paunto 3aMectnTensi b ποποχθηκμ 5 SnunKnuMecKoro sinpa u uwxnonponaHOBoro anpa. - Rx:
Rz: C1 C1
LV10074
Tadjmiļa I
Table 1 CTpyKTypHaa $opiiyjia
Structural Formula
/0$&gt;M3MVeCKHe CBOftCTBaR3 R4 X m Physlčal Properties o Sti coP, Bi o co 03e «d 03 es «3 I -00 w C\1 oi_i co i *00P» coe-
EH co co co co co CO35 sc sc as rn as 9 9 9 9 9 9 CM CM CM CM CM CM 000900 C/3 co co co co co
coac co 9 35 CM 9 o CM CO o 00 « 7 o W °o3 tu t— O &quot;B &lt;-lP so ° 2· c o. a oBJ ca o« Bi o co I00 · o
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Structural Formula
Xm \Hetero ring) ΓβΤβρΟΙίΗΚΛΗ ^βοκοβ H^po 2ο CO m Eh O «e *3 “oZ m u O &lt;u o.
O — φ d jj* o
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LO co CO LO co co LO in ss sc sc co in ss sc sc co LO SC IO 3= CM o CP co SS in sc CM o cp co sc in SC CM SC CM &lt;L&gt; o co co sc CP sc CM o o co co sc o sc CM O CM CP CM CO CM co CM CM sc CJ&gt; CM CM CP CM co CM CO CM CM sc CJ&gt; CM CM CJ&gt; CM co CM CP O O SC o Z u. sc ss o o o CP o O sc Ο 3C u. ss ss CP o o C_3 o O sxs o 3S co co CO CP z CP cp CP CP co co co CO co CO cp sc o CP cp cp co co co co co CO o ss o lO LO in LO| LO 1 LO in in to in in in to 10 10 in 5- 5- in ιο 10 in ΙΓ5 lO m LO LO LO ΙΩ LO Φ &lt;u a&gt; α&gt; a&gt; o&gt; o&gt; φ ω (D a&gt; a&gt; d&gt; a&gt; a&gt; ŪJ 03 03 a&gt; 03 03 o&gt; 03 a&gt; 03 03 03 03 03 e cs c cs cs c cs cs es cs cs cs cs cs cs cs CS CS CS cs e cs cs e cs es CS B CS CS Ό Ό •ο -a *o o TS «o •o Ό *o •o •o -a «Ο Ό -a •a o Ό Ό •σ Ό *o -o T3 •o •d —m MM —* MM —M —- —- MM —- •«M *—M —M —&gt;4 «mm «MM ·* ««— ••M ·— MM «Ml •MM mM t« Wm hl Im Ch u. t- u. k- k* Im 1- Im l-N Im u. U Im U Ul t-l tm 1* U· &gt;* &gt;% &gt;* &gt;» &gt;» &gt;. &gt;, &gt;s &gt;» ' 5K &gt;» &gt;* &gt;* &gt;s &gt;s &gt;» &gt;H &gt;* &gt;% &gt;« &gt;« &gt;1 &gt;* &gt;1 &gt;1 &gt;» o. O, O. cs. o, o. o. o. O. o. o. o. o. o. o. O. O. O. o. a. o. o. o. o. a. a. o. o. o. o. cm CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CM CO CO CO co CO co co CO CO co CO CO SC ss sč SC SC sc SC sc SC sc 33 33 ac SS sc H H SC SC SC SC SC sc SC SC sn SC SC H H CP o o o C-3 c_? o C_3 CP CP CP co co co co CO co co co CO co co CO sc sc sc 2C sc sc sc sc sc sc 33 sc rn ss sc H H sc sc SC sc sc sc sc sc sc sc ss H H u o o o CJ&gt; 0-3 cp CP O &lt;P O IIcs
w CO τρ ΙΩ CDco co co co co co I I I I I IW W H W W H co co co CO co CO CO co CO co co CO co co co co co co co co co co CO co ss 33 sc 33 sc 33 ss sc sc 33 sc ss sc sc sc sc 3X3 sc a= ss sc sc ss ss CP CP CP CP CP CP CP CP CP CP CP CP CP CP CP CP CP CP CP CP CP CP CP CP ««4 «-4 M&lt; mH ««4 ««4 1 «M4 - IO IO (O IO IO LO IO LO LO in LO IO c^ co CD o rH CM co -rr IO CO t— 00 03 o r-4 CM co LO co t- co o&gt; o co CO CO -M4 «tļl IO LO IO LO LO LO to LO LO LO co 1 w 1 w 1 w 1 H 1 H 1 W 1 W 1 tt 1 1 W 1 fcl 1 1=1 1 t=l w 1 w 1=1 1 1=1 w 1 1=1 1 H 1 w 1 a 1 1 w * f zv reTepoijHKJiM-yecKoe H^po ΦΗθΗ^βοκΜβ CBoiicTBa (R2)n R3 R4 Hetero ring X m Physlcal Propertles CO CO 33 3C —· O uuco I I I &lt;0 CO CO I I &lt;
• rs : oo co Irt CO co Irt C-3 co CO eo eo : a= ac co in SC ac as co 10 as 1 33 33 33 ac : o 0 co X m s CJ 0 0 eo ac in 32 CJ CO O C_&gt; O 0 : o co co ac 0 as CJ O 0 co co ac 0 sc CJ 0 1 O C9 O 0 ^C^MlOOJNūCJCOCsi COCVIWXONNOWCON CO CO CM OJ CM CM ^32ϋ00ϋ00ϊ02{ί.3χϋ00ϋ00 3:.02^^ϊϊϊ2 UUOWWWWWl/3U2;oauUWWMWWWŪ2UUŪŪWOU 1 «ttll I II tl | I | | l-llltt |«»t II * It wwioininintnwiftiotoioioii)if)ioiflir)ift»r)iou5ioiowNNWWN w ' ϋφννα)υο)υο}φ(ΐ}ΐνιΐ)φννννυνν&lt;»ννα)ΐΐ)θ)υο)ο) eeeeseeeeeeeeeceeeecceeceeeecea T) 73 73 73 ^ ό 73 «o 73 Ό 73 «ņ 73 73 ^ Ό Ό *0 *0 Ό 75 Ό 73 73 73 *0 73 ū.QaQQaaaaaacLaaQaQaaaQ6flQaaaaaa I I I I I I I I I I I I I I I I I I I I · * 1 1 1 1 * 1 1 1 ΜΝΝΝΝΝΝΝΝΙΝΝΙΝΙΜΝΙΝΝΝΝΝΝΝΝΝΝηηηί50«
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CJ5 o o CO CD *4 CM 00 to lO lO * • • «H o o O • • ♦ to lO to CM CM CM a A o c C c
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Kak ynoM'/Ha/iocb Bbiuie, stm coe4RneHRfl o6Ra4aioT ποβμιμθηηοΛ rep6MUM4H0i?i ak τ r b η octbto. Coe4RHeHRflMR mojkho o6pa6aTbiBaīb ηθποορθλοτβθηηο noMBy /o6pa6oTka 40 ποηβλθηιλα coPHflkOB/ rrr r r ct b y pacTeHMfl/ o6pa6oTka copHPkoB noc/e rx nosBReHRfl/6 rrr rx mokho CMeiUMBaTb C Π04Β0&amp;. Coe4RHeHRBMR M05KH0 Ο 6 Pa6a T bl B a T b n04By RRR /ļi/!cτby pacTCHRR b kORRHecTBe 1 r rrr 6o/tee Ha 10 ap. Γθρ6μιιι/μνμθ koMno3RURR, co4epxauiRe οοθ4μηθημβ 4aHHoro '/3θ6ρβτθΗΐ/ΐ9 b kaMecTBe akTMBHoro RHrpe^ReHTa strx kOMno3RURfl, mojkho COCTaBRflTb ΟΜΘΐΰθΗΜΘΜ C. n04X04HlUMMR H0CRT0 R B MR 8 ®OPMaX, B kOTOPblX o 6 b! m h o ncno/ib3yioT ce/ibckoxo3fiflcTBenHbie XMMRkaTbi, Taknx kak, KanpuHep, CMam/iBaeMbifl nopouiok, BO40PacTBOPRMWfl nopouiok, rpaHyRbi, 3My/brMPyeMbifi koHuenTPaT r KM4kocTb, B kasecTBe τβθρ4μχ HOCMTe/ieR MoryT 6biTb RcnoRb30BaHU TaRbk, 6e/ibiR yroRb, /4Byokncb kpeMHRfl/, όθΗΤΟΗΜΤ , Γ R R H a , 4RaT 0MRT OBdfl 3ΘΜ/ΙΒ RRR R Μ Π0406ηΜΘ ΗΟΟΜΤΘ/ΙΜ . B kanecTBe kr4Kmx Hocme/ieR MoryT 6biτb RcnoRb30BaKbi B04a, οπμρτ, 6 s k 3 ο r , kcn/to/1, kepocRH, Mi/mepa/ibHoe Mac/io, tjRkRorekcaH, •4wk4orekcaHOH, 4RMeTRR&lt;P0PMaMH4 R rm πο4ο6η«θ hocrt ©rr . Ecrr Heo6x04RMO, 4/1 λ nO/iyMeHRfl rOMOreHHOrO R yCTOflMRBOr0 COCTaBa ΜΟΧβΤ 6biτb 4o6aū/ieH ποβθρχηοοτηο akTRBHbift aret-ιτ.
Coe4RHeHMfl MoryT Takace npRMeHBTbca b cMecR c 4P9trhr XRMMHeckRMR C0e4RHeHRBMR , kOTOPbie RCnORb3yiOTCfl B arPOHOMR4eekoR R ca403044eckoR npakTRke m BBRflioTCii cosMecTRMRMbi c 4aHHbiMR
coe4RHeHMBMR. TakRe XRMMkaTbi HoryT npRHa4Re)KaTb k kRaccaM XRMRkaTOB, oSblMHO R C Π 0 A b 3 y Θ M bl X B kaMeCTBe ®yHrRUM40B, RHCekTRUR408 , akaPRqR4CB, rep6RUR40B r peryrbtopob POCTa pacTeHRfl, ho ηθ or paHMMRBatoTCP yka3aHHbiMM k/iaccaMVi. B MacTHOCTR, cMeiueHReM CCe4RHeHRR 4aHH0r0 R306PeTeHRB C 4 P y Γ R Μ M reP6RLlR4aMR , ΜΟΧΗΟ yMeHbiiiRTb Rcno/ib3yeMbie 403bi r chr3rtb 3aTpaTbi pa6cmefl crrm Ha rx nPRHBHSHRe , H , kPOMe ΤΟΓΟ, ΜΟΚΗΟ 0X(R4aTb 6θΛΘΘ CM/lbHOTO 30®ekTa B pe3y/ibTaTe CRHeprMseckoro 4ePiCTBRP o6orx XRMRkaT08. 4rb cocras/ieHRP CMecefl coe4RHeHRfl 4aHHoro R3o6peTeHR« c R3secTHbiMR rep6RUR4aMR pekoMeH4yeTca wcn0/ib30BaTb 6eHTRokap6, ΜΥ-93 /S-(2,2-4RMeTW/i6eH3R/0-1-nRnepR4RHkap6oTRoaT/ rrr 4PyrRe rep6RUR4bi kap6aMaTHoro TRna; rep6RUR4bi TMokap6aMaTHoro TRna; 6yTaxR0P, npeTR/iax/iop, Me®eHaueT r 4pyrRe rep6RUR4N kwc/ic&gt;THO-aMR4Horo TRna; χ/ioPMeTokcMHR/t, 6R®enokc r 4PyrRe rep6RUR4bi 4R®eHRR3®RPHoro TRna; aTPa3MH, iļRaHasRH r 4PyrRe rep6RUR4bi TPRa3RHOBoro TRna; X/iopcy/ib®yphop , cy Rb®0MeTypoH-MeTRR r 4pyrwe rep6RUR4bi
CyRb&lt;5OHRRMO4eBRHH0r0 T R Π a ; MCP, MCPB R 4PyrRe reP6RUR4bl TRna a&gt;eH0kcRa/ikaHkap60H0B0fl kRCROTbi; URkRooon-MeTRR r 4PyrRe rep6RUR4bi TRna oeHokcRnPonROHOBoR k r c r ο τ w; 6eH3owRnpon-3TRR, ®/iaMnpon3TR/i r 4PyrRe rep6RUR4bi TRna 6eH30R/taMRH0nP0nR0H0B0ia kRCROTbi r, b kasecTBe 4Pyrwx, πμπθροφοο, 4Rmpoh, 6eHTa30H, 4R®eH3oksapT, HanpoaHR/iR4, HW-52 /4-3TokCR-MeTokcM-6eH30-2,3-4RX/iopaHR/iR4/, KNW-242 /1 -(3-MeTR/i-cpeHR/i )-3-&lt;peHR/i-1 H-1 ,2,4-TpRa30R-3-kap6okcaMR4/, XRHkROPak /3,7-4RX/iop-8-XMHOHkap6oHOBaB k rcr ot a/, r, kPOHe τογο, ceTokCR4RM, a/i/iokcR4RM-HaTpRi?i r 4PyrRe rep6RiļR4bi URk/torekcaH4ROHOBoro TRna. 3tr rep6wuR4bi b pa3/iR4Hbix co4eTaHMfix MoryT 6wTb Tak*e CMeiaaHM c PaCTRTe/lbHbIM Mac/IOM R/IR M3 C R P H bl M kOHlļeHTPaTOM . KOHUeHTPāMRfl akTRBHOTO RH Γ P64RGHTa B ΓθP6mUR4HOR k0Mn03RURR Μ05ΚΘΤ BaPbRPOBaTbCP 8 3a8RCRMOCTR OT TRna COCTaBa, M 3Ta koHiieHTpaiļR?! coctaerαθτ , nanpRHep, ot 5 40 70 Mac. %, npe4noHTRTeRbHo ot 10 40 30 Mac. %, b CMaHRBaeMOM nopouike; ot 3 40 LV10074 70 Mac. %, npennoMTMTenbHO ot 5 no 20 Mac. %, b 3MynbrupyeM0M «OHueHTpaTe; ot 0,01 no 30 Mac. %, npennoMTMTenbHO ot 0,05 no 10 Mac. %, a rpaHynax. flonyMeHHbie τ a κ μ m o5pa20M CMaHMBaeMbiia nopoiuoK nnn 3MynbrnpyeMbiPi KOHueHTpaT MoryT 6birb pa3SaBneHbi sonopi no sanaHHOPi KOHueHTpaunu m ncnonb30saHbi b Bune χΐ/ίηκοκ cycneH3MM nnn χμακοη BMVnbCnn nna οδράδοτκΜ ποΜΒ μπμ ηncτBbi pacT6HMiži. rpaHyriaMK μ ο χ η o HenocpencTeeHHO oGpaoaTbisaTb noMBy nnw 3aMeuiMBaTb wx b noMBy.
He o r p a η μ M w b a κι m w θ oObeMa Μ3θδρθΤ8ΗΜΗ npMMepbi rep5nunnHbix Κ0ΜΠ03Μ14ΜΡ1 npMBenOHbl Η Μ X 8 Ϊ ΠΡΜΜΘΟ 3 CMaMMBaeMblfl ποροωοκ
Becosbie macτm Οοθπμηθημθ nannoro M3o6peTeHMsi 20
Benbīia yronb 20 flUSTOMHTOBaS 3SM(1SI 52 ftriKnncynb?aTHarpM5i 8 Κομποηθητμ cMeiunBatoT no nocTMxenM5i roMoret-iHOCTM, m nonyMeHHHyio cMecb M3MeribMatoT, nonv^aa CMaMMBaeMbisa ηοροωοκ, conepxamma 20% aKTMBHoro MHrpenMeHTa. npM Mcnonb3DBannn ero pa35asnsiHiT no Tpe5yeMO« KOHueHTpauMM βοπομ m pa36pbi3rnsaiOT b sune cycneH3MM. Πρμμβρ 4 3MynbrnpyeMbm κοηρθητρητ
Becosbia m a c τ κ
CoeflMHSHue naHHoro M3o5peTeHM?i 20 KcMnon 55 flMMeTMfiņopMaMMā 15 nOflMOKCMBTMnSHlpeHMnOBbm 3 φ m p 10 Κομποηθητμ CMeuiMBaioT κ pacTBoparaT, nonyMasļ 3MynbrnpyeMbm KūHueHTpaT, conepxainnK 20% θκτμβηογο UHrpenueHTa. Πρκ ncno&lt;ib30BaHMM θγο pa36asnsuoT eonopi no Tpe5yeMoia KOHueHTpaunM, n pa35pbi3r uearaT b
Bune 3MyrtbCMM. Π ο μ m 8 p 5 Γ p a h y n bi
Becoebie macτm 5
CoenMHeHne naHHoro M3o5peTeHMsi
TanbK 40 rnHHa 38 Β8ΗΤ0ΗΙΊΤ 10 AnKnncy AbtpaT Haipust 7 ΚομποηθητιιΙ cMauiMBSKīT ao α ο c τ κ χ e η n a r ο μ ο r ε η η ο c τ u , nony4as r ρ a η y a bi, coaepKamne 5 % βκτι/ιβηογο HHrpeflueHTa. npaKTUMecKoa ncnontsosanne: repSuunflHbiPi 3 ψ ψ θ κ τ coennHeHUPi MAAiocTpnpyeMbiH HnxecneAyK]uinM r e c τ ο m .
Teci 1 05pa5oTica pacTeHni* nocns mx nosBneHMSi
CeH8H3 Γ) Ο A 3 y Μ θ Γ O C Ο p Η Η K a Γ θ Η Ρ K j rnrāHTCKOrO AHCOXBOCTa, pncoBOPi ocokm, nuMnoxapnca, neSeAbi δ e η o ia m 3epHoeoi/i KynbTypbi noceHAH b rjiHHHHbie ropuiKH /200 cm1/, co^epacamHe cītjihhok, m
BbipamHBaH b τβππκμβ. Korfla pacreHHH Bbipocnn λο BbicoTbi 5-10 cm, hx nwcTsy oSpbisranu, Mcnonb3ys ΜΜκροιιιπρκιι, soaHbiMM cycneH3nsiMM, npurOTOBABHHblMM pasSaEAeHMeM 3MVAbrHpyeMOrO KOHLteHTpaTa 800080 AO TpečyeMOPi KOHueHTpaunn /250 pp (γ/μπη)/; A03npos&lt;a cocTaensna 1D0 n/10 ap,
Mepe3 τ p m H8Aenn nocne οδρβδοτκκ αηα Kaxaoro M3 pacTeHMH onpeaensinw cTenenb nosperαθηκ9 , KoTopyra oiļeinusaAK b cootb8tctbmm co uiKanoia bsahmhh ot 0 ao 10, μμθβιιικχ cneAyraiUne 3HaM8HH5i: M h a e κ c 0 2 4 6 8 1 0
CreneHb noBpesaeHusi 0 % 20-29 % 4 0 7 4 9 % 60-69 % 80-89 % 100 % LV10074 MH^eKCbi 1, 3, noBpeKfleHHH Meacfly 0 COOTBeTCTBeHHO. , 7 H 9 03HaHai0T npoMescyTOHHbie οτθπθηη [2,2 H 4, 4 h 6, 6 h 8, h 8 h 10, CBeacufī Bec Ha CBeacHft Bec Ha Heo6pa6oTaHHOM ofipafioTaHHOM yqacTKe ynacTKe ) ------------- CBejKHft Bec Ha CTeneHb noBpe*fleHHH (% -------------x 100
Heo6pa6oTaHHOM yqacTKe
Pe3ynbTaTbi npHBefleHbi b TaāJiHLje 4. 3i
Tačjiima 4 Οοθττκηθ- ļ_Οτθηθκβ εοβρθειιθη'ιη /ηκιιθκο/
Kne JS ĪIoji3y^ic: COpEHK ΓβκρΕ » FEraHT- CKKI; J1ECO- XBOCT ϋΐΙΜΠΟ— xapnc Jledejia dejiaa PECOBan ocoKa SepHOBaa KyjiBTypa 1-10 10 10 10 10 10 3 1-20 10 10 10 10 10 0 1-21 10·· 10 10 10 10 0 1-35 10 10 10 10 10 0 1-36 ' 10 10 10 10 10 0 1-48 10 10 10 10 10 1 1-49 10 10 10 10 10 0 1-50 10 10 10 10 10 0 1-54 10 10 10 10 10 0 1-55 10 10 10 10 10 1 1-56 10 10 ; 10 10 10 0 1-57 10 10 10 10 10 0 1-65 10 10 10 10 10 1 1-81 10 10 10 10 10 0 1-85 10 10 10 10 10 1 1-97 10 10 10 10 10 2 1-98 10 10 10 10 10 2 1-99 10 10 10 10 • 10 0 1-100 10 10 10 10 10 0 1-101 10 10 10 10 10 3 1-109 10 10 10 10 10 0 1-133 10 10 10 10 10 0 1-143 10 10 10 10 10 0 1-144 10 10 10 10 10 1 LV10074 1-145 10 10 10 10 10 0 1-146 10 10 10 10 10 0 1-168 10 10 10 10 10 0 1-169 10 10 ' 10 10 10 0 1-170 10 10 10 10 10 2 1-172 10 10 10 10 10 0 1-173 10 10 10 10 10 2 1-176 10 10 10 10 10 0 1-177 10 10 10 10 10 0 1-178 10 10 10 10 10 0 1-179 10 10 10 10 10 3 1-180 10 10 10 10 10 2 1-181 10 10 10 10 10 3 1-183 10 10 10 10 10 3 1-184 10 10 10 10 10 3 1-185 10 10 10 10 10 0 1-186 10 10 10 10 10 0 1-187 10 10 10 10 10 2 1-188 10 10 10 10 10 3 1-189 10 10 10 10 10 0 1-190 10 10 10 10 10 2 1-191 10 10 10 10 10 0 1-192 10 10 10 10 10 0 1-193. 10 10 10 10 10 0 1-195 10 10 10 10 10 0 1-196 10 10 10 10 10 0 1-197 10 10 10 10 10 3 1-198 10 10 10 10 10 0 1-200 10 10 10 10 10 0 1-201 10 10 10 10 10 0 1-202 10 10 10 10 10 0 1-203 10 10 10 10 10 0 1-204 10 10 10 10 10 1 1-205 10 10 10 10 10 1 1-207 10 10 10 10 10 2 1-208 10 10 10 ίο 10 0 1-209 10 10 10 10 10 0 1-210 10 10 10 . 10 10 2 1-211 10 10 ! 10 10 .10 0 1-212 10 10 10 10 10 2 1-214 10 10 10 10 10 0 1-215 10 10 10 10 10 3 1-216 10 10 10 10 10 0 1-217 10 10 10 10 10 0 1-218 10 10 10 10 10 0 1-219 10 10 10 10 .10 0 1-220 10 10 10 10 10 0 1-222 10 10 10 10 10 0 1-224 10 10 10 10 10 3 1-225 . 10 10 10 10 10 3 1-228 .10 10 10 10 ' 10 0 1-229 10 10 10 10 10 0 LV10074 1-230 10 10 10 10 10 0 1-231 10 10 10 10 10 0 1-232 * 10 10 10 10 10 0 1-233 10 10 10 10 10 0 1-234 10 10 10 10 10 0 1-237 10 10 10 10 10 3 1-238 10 10 10 10 10 0 1-240 10 10 10 10 10 0 1-241 10 10 10 10 10 0 1-244 10 10 10 10 10 2 1-245 10 10 10 10 10 2 1-249 10 10 10 10 10 3 1-250 10 10 10 10 10 0 1-251 10 10 10 10 10 0 1-254 • 10 10 10 10 10 0 Π -102 10 10 10 10 10 3 H -109 10 10 10 10 10 0 1-130 10 10 10 10 10 0 Π -137 10 10 10 10 10 0 1-277 10 10 10 10 • 10 3 -Comparative Compound A 6 7 8 4 · 5 7 -Comparative Compound B 6 5 8. 2 '8 6 &lt;?Ρ3ΒΗΗΤ63Π&gt; noe coean-«eHES A.
CpaEHHTejm M08 coejH-tfeace B •io
CD£SHMTejiī&gt;Hos coesEfiSHKe A
Comparative Compound A:
Comparative Compound B; CpaBHETSJILHOB ΟΟβΒΜΗΘΗΕβ B
ΠετθΗΤ ΦΡΓ 3S023I8 (DE 3902818)
IlaTeHT ΦΡΓ 3902818 (DE 3902818) LV10074
ΦΟΡΜΥΛΑ H30EPETEHHH 1. 3a.viemeHHoe npoH3BO^Hoe 6imiiKJiorenTa,nHOHa, o6mefl φορΜγπω /1/
o (I) /r^e R1 npeacTaanKeT co6o0 HH3ray(0 anKiifihHyto rpynny, 0eHiinbHy!o rpynny, κοτορΒΗ mosbt 6biTb 3aMemeHH0ft, apajiKHJībHjrio rpynny, KOTopaa MOHceT CbiTb 3as.iemeHHoft, hjui reTepotjHK;niqecKyio rpynny, KOTopaa Μοαβτ CbiTb 3aMemeHH0ft; R1 MOr.VT (5bITb OjļūK'uK 0 BbiMII ΗΠΗ pa3HblMH u npe^cTaBJiaioT coCSoft aTOMbi γβ.τογθηοβ, anKOKcnrpynny, aaKnnTiiorpynny/ ajiKnncy:ib&lt;f&gt;oBHnbHyD rpyrmy, a::Kn.TbHyin rpynny, a.TKOKCnaaKiuibHyio rpynny . ηλη a.TKOKC«Kap6oHH.&quot;bHyR3 rpynny, ii fļ npiiHHMaeT 3HaqeHHH ot 0 ao 4; R3 H R* MOT.VT ChITb OaHHaKOBbtMH ΚΛΗ paSHblMH H npeflCTaBJiHioT coGoA ZTOMki BOAopofla u.t.! Kiiaume anKHJīhHbte rpynnwr nnn ero cojib.
/rae R&quot;, R1» RJ, R* η Π ημθώτ Te ace 3HaqeHHH, bto h onpeAe;ieHHbie Bbitne b . n.l/, OT.nmatomuflcH τθμ, mto BKJisoqaeT b ce6n peaKUHfo 3aMbiKanHfl nitKna eoeflUHeHmt, o6mefl φορΜΥΠ^ /11/
1
CnocoC nojiyBeHiis coefliiiieHHH, oOmeii φορΜγΛΜ /1/ / t/υ
/r^e R‘, R3, R3, R4 u HMetoT BbiuieyKa3aHHbie 3Η3ηθηηη, a Q npe^cTaB^fleT co6oft yxoflHmyK&gt; rpynny/ b npncyTCTBHH ocHOBaHHH. 3. repCmjHfl, OT.iHMaīomHftcH τθμ, mto BKJiKmaeT b CBoeft cocTaB oļHO, flaa hjui 6ojiee coe^HHeHHft, npeflCTaBJieHHbix o6meft &lt;J)opMyjioa /1/
(X) /γαθ R1, R3, R3, R4 h fļ ημθγοτ τθ we 3HaMeHiiH/ hto h onpeaejieHHbie Bbirne/ b KaHecTBe βκτηβηηχ κομποηθητοβ. LV10074 P E Φ E P A τ 3aHHoe HsočpeTeHiie othochtch k 3aMeuteHHUM npoH3BO^Hbi\i CHHHK.TorenTa^HOHa, ofi.TaļarouļHM bmcokoū repdHUH^HOfl aKTHBHOCTbio, KOTopbie ΜΜθίοτ odmjio (J&gt;opMy;iy /1/
/r;*e R5 npe,5CTaBn«eT coCofl HH3myio aJiKHjībHj'io rpynny, Φθηιιπβη1μο rpynny, KOTopan MoseT GbiTb 3aMemeHH0fi, apa.iKHJibHyio rpynny, KOTopaa ΜΟ/κετ 6biTb 3aMemeHHoft, ηλη reTeponnK;umecKyīo rpynny, KOTOpaa moscst dbiTb 3aMemeHHofi; R2 MOryT dblTb OfllIHaKCSBbiMII ΗΠΗ pa3HbIMH H npeaCTaBJIHIOT COGoft aTOMbi ranoreHOB, anKOKCiirpynny, anKHJiTHorpynny, ajiKiuicynb&lt;ī&gt;oHn:ibHyio rpynny, . a,iKii;ibHyjo rpynny, a;iKOKCna;iKHJibHyio rpynny nmi a.TKOKCMKap6oHHabHyio rpynny, a npHHHMaeT 3HaaeHHS ot 0 flo 4; RS II R* MOryT GbITb O^HHaKOBbtMH HJIH pa3HblMH II npe^CTaBJI^BOT cofiofi aTOMbi Bo^opo^a naii Hii3iime anKiuibHbie rpynnbi/. ,

Claims (2)

  1. LV10074 IZGUDROJUMA FORMULA 1. Aizvietots bicikloheptāndiona atvasinājums ar vispārējo formulu (I), vai tā sāls:
    kurā R1 ir zemākā alkilgrupa, fenilgrupa, kura varbūt aizvietota, aralkilgrupa, kura var būt aizvietota, vai heterocikliska grupa, kura var būt aizvietota; R2 var būt vienādi vai dažādi un ir halogēna atoms, alkoksigrupa, alkiltiogrupa, alkilsulfonilgrupa, alkilgrupa, alkoksialkilgrupa vai alkoksikarbonilgrupa, kur n ir ar vērtību no 0 līdz 4; R1 un R2 var būt vienādi vai dažādi un ir ūdeņraža atomi vai zemākās alkilgrupas.
  2. 2. Savienojuma ar vispārējo formulu (I), kurā R1, R2, R1, R2 un n ir ar to pašu nozīmi kā definēts 1. punktā, iegūšanas paņēmiens, atšķirīgs ar to, ka ietver sevī savienojuma ar vispārējo formulu (II)
    (kurā R1, R2, R1, R2 un n ir ar iepriekšnorādīto nozīmi, bet Q ir promaizejošā grupa) cikla saslēgšanās reakciju bāzes klātbūtnē. 1 Herbicīds, atšķirīgs ar to, ka savā sastāvā kā aktīvos komponentus 2 ietver vienu, divus vai vairākus savienojumus ar vispārējo formulu (I), kurā R1, R2, R1, R2 un n ir ar iepriekšnorādīto nozīmi.
LVP-92-613A 1989-07-04 1992-12-30 Substituted bicycloheptandione derivatives LV10074B (en)

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JP20750189 1989-08-10
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JP385490 1990-01-11
PCT/JP1990/000850 WO1991000260A1 (en) 1989-07-04 1990-06-29 Substituted bicycloheptandione derivatives

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LV10074B true LV10074B (en) 1995-02-20

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US5294598A (en) * 1990-06-29 1994-03-15 Nippon Soda Co., Ltd. Herbicidal 3-substitutedbenzoyl-bicyclo[4,1,0]heptane-2, 4-dione derivatives
JPH04247052A (ja) * 1991-01-31 1992-09-03 Nippon Soda Co Ltd ビシクロ〔4,1,0〕ヘプタン−2,4−ジオン誘導体、その製造法
WO1993020037A1 (en) * 1992-03-27 1993-10-14 Nippon Soda Co., Ltd. Cyclohexenone compound and production thereof
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AR248126A1 (es) 1995-06-30
LV10074A (lv) 1994-05-10
DK0432275T3 (da) 1995-07-31
BR9006845A (pt) 1991-08-06
CN1048848A (zh) 1991-01-30
JP2921047B2 (ja) 1999-07-19
ATE119146T1 (de) 1995-03-15
EP0432275B1 (en) 1995-03-01
HU905358D0 (en) 1992-01-28
WO1991000260A1 (en) 1991-01-10
KR940005913B1 (ko) 1994-06-24
HUT59075A (en) 1992-04-28
US5228898A (en) 1993-07-20
CN1025186C (zh) 1994-06-29
HU207832B (en) 1993-06-28
JPH03255047A (ja) 1991-11-13
EP0432275A1 (en) 1991-06-19
KR920701120A (ko) 1992-08-11
DE69017383T2 (de) 1995-06-29

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