- Preparation method of acaricide of fenazaquin
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The invention discloses a preparation method of an acaricide of fenazaquin, and belongs to the field of a pesticide raw drug process. The preparation method is implemented through the following stepsthat (1) 4-tertiary butyl phenethyl alcohol is used as r
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Paragraph 0025; 0027; 0028; 0030; 0031; 0033; 0034; 0036
(2020/09/20)
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- ACTIVE COMPOUND COMBINATIONS HAVING INSECTICIDAL AND ACARICIDAL PROPERTIES
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The novel active compound combinations comprising a compound of the formula (I-1) or (I-2) and the active compounds (1) to (26) listed in the description have very good insecticidal and acaricidal properties.
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- Insecticidal quinazoline derivatives with (trifluoromethyl)diazirinyl and azido substituents as NADH:ubiquinone oxidoreductase inhibitors and candidate photoaffinity probes
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Two candidate photoaffinity probes are designed from 4-substituted quinazolines known to be potent insecticides/acaricides and NADH:ubiquinone oxidoreductase inhibitors acting at or near the rotenone site. 4-(11- Azidoundecyl-2-amino)quinazoline, based on the undecylamino analog SAN 548A as a prototype, was synthesized in 18% overall yield from ethyl 10- undecenoate by oxidation of the terminal double bond, reductive amination, coupling to 4-chloroquinazoline, and functional group manipulation of the terminal ethyl ester to an alcohol, a mesylate and finally nucleophilic displacement with azide ions. 4-(4-(3-(Trifluoromethyl)-3H-diazirin-3- yl)phenethoxy)quinazoline [the (trifluoromethyl)diazirinyl analog of fenazaquin insecticide/acaricide] was prepared from 4-bromophenethyl alcohol in 31% overall yield by first introducing the trifluoromethylketone moiety followed by its conversion to the (trifluoromethyl)-diazirine and finally coupling to 4-chloroquinazoline as above. Both candidate photoaffinity probes have the inhibitory potency of rotenone (IC50 of 3-4 nM in each case). The azidoundecylamino compound has inadequate photoreactivity whereas that of the (trifluoromethyl)diazirinyl analog is ideal at 350 nm. Radiosynthesis of the latter photoaffinity ligand included introduction of the diazirinyl moiety as the carbene precursor, oxidation of (trifluoromethyl)diazirinylphenethyl alcohol to the corresponding acid with Jones' reagent, and reduction of the phenacetyl chloride intermediate with sodium borotritide to incorporate tritium.
- Latli, Bachir,Wood, Edgardo,Casida, John E.
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p. 445 - 450
(2007/10/03)
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- Quinazoline derivatives
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Substituted quinazolines of the formula (1): STR1 wherein: R1 to R4 are independently H, halo, (C1 -C4) alkyl, branched (C3 -C4) alkyl, halo (C1 -C4) alkyl, (C1 -C4) alkoxy, NO2, or NH2, provided that at least two of R1 to R4 are H; Y is H, Cl, X--W--Ar, or O--Alk; X is O, NR7, or CR8 R9 ; Z is H, Cl, OCH3, CH3, or --NR7 --W--Ar, provided that Z can be --NR7 --W--Ar only if Y is H, Cl, or NR7 --W--Ar and Z must be --NR7 --W--Ar if Y is H or Cl, which are plant fungicides, miticides, and insecticides.
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