Insecticidal pyrazolines

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

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548379, 544 82, 544130, 544140, 546187, 546211, 5142322, 5142365, 514316, 514326, C07D23106, A01N 4356

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active

050914057

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BRIEF SUMMARY
BACKGROUND OF THE INVENTION

Vaughan, J. Org. Chem., 20 (1955), pages 1619 to 1626, discloses 1,5-diphenyl-2-pyrazoline-3-carboxamide. No utility is given for the disclosed compound which, in any event, does not suggest a compound of the instant invention.
U.S. Pat. No. 4,070,365 discloses insecticidal compounds of the formula ##STR1## wherein X is halogen, and Y is halogen, NO.sub.2 or alkyl.
EP 153,127 discloses insecticidal compounds of the formula ##STR2## wherein A is unsubstituted or substituted phenyl;
Harhash et al., J. Heterocyclic Chem., 21 (1984), at page 1013, discloses the preparation of five pyrazoline compounds, none of which is disclosed in the instant application. No utility is given for any of said compounds: ##STR3## where R/Ar are C.sub.6 H.sub.5 /C.sub.6 H.sub.5 ; CO.sub.2 C.sub.2 H.sub.5 /C.sub.6 H.sub.5 ; C(O)NHC.sub.6 H.sub.5 /C.sub.6 H.sub.5 ; CH.dbd.CHC.sub.6 H.sub.5 /C.sub.6 H.sub.5 ; and CH.sub.3 /4-NO.sub.2 --C.sub.6 H.sub.4.


SUMMARY OF THE INVENTION

This invention concerns certain 4,5-dihydro-1H-pyrazole-3-carboxamides (hereinafter referred to as pyrazolines) and intermediates to said compounds, including all geometric and stereoisomers of the pyrazolines and the intermediates. This invention also concerns agricultural compositions comprising at least one of said pyrazolines as active ingredient and an agriculturally suitable carrier therefor. This invention also concerns a method for controlling insects comprising contacting them or their environment with an effective amount of a pyrazoline of this invention.
More specifically, this invention pertains to pyrazolines of Formula I and agriculturally suitable salts thereof: ##STR4## wherein: X is O or S; to C.sub.4 alkylthio, C.sub.1 to C.sub.4 haloalkylthio, phenylthio, or phenylthio substituted with 1 to 3 substituents independently selected from W, C.sub.2 to C.sub.4 alkoxycarbonyl, C(O)H, C.sub.2 to C.sub.4 alkylcarbonyl or C.sub.2 to C.sub.4 haloalkylcarbonyl; (R.sub.5).sub.p, CN, CO.sub.2 R.sub.3, C(O)R.sub.3, C(O)NR.sub.3 R.sub.4, C(S)NR.sub.3 R.sub.4, C(S)R.sub.3 or C(S)SR.sub.3 ; C.sub.6 alkoxyalkyl, C.sub.2 to C.sub.6 cyanoalkyl, C.sub.3 to C.sub.8 alkoxycarbonylalkyl, C.sub.2 to C.sub.6 alkenyl, C.sub.2 to C.sub.6 alkynyl, C.sub.2 to C.sub.6 alkoxycarbonyl, phenyl, phenyl substituted with 1 to 3 substituents independently selected from W, benzyl or benzyl substituted with 1 to 3 substituents independently selected from W; haloalkyl, C.sub.1 to C.sub.2 alkoxy, C.sub.1 to C.sub.2 haloalkoxy, C.sub.1 to C.sub.2 alkylthio, C.sub.1 to C.sub.2 haloalkylthio, C.sub.1 to C.sub.2 alkylsulfonyl or C.sub.1 to C.sub.2 haloalkylsulfonyl; N.sub.3, SCN, NO.sub.2, OR.sub.3, SR.sub.3, S(O)R.sub.3, S(O).sub.2 R.sub.3, OC(O)R.sub.3, OS(O).sub.2 R.sub.3, CO.sub.2 R.sub.3, C(O)R.sub.3, C(O)NR.sub.3 R.sub.4, S(O).sub.2 NR.sub.3 R.sub.4, NR.sub.3 R.sub.4, NR.sub.4 C(O)R.sub.3, OC(O)NHR.sub.3, NR.sub.4 C(O)NHR.sub.3, NR.sub.4 S(O).sub.2 R.sub.3, or when m, n or p is 2, R.sub.1, R.sub.2 or R.sub.5 can be taken together as --OCH.sub.2 O--, --OCF.sub.2 O--, --OCH.sub.2 CH.sub.2 O--, --CH.sub.2 C(CH.sub.3).sub.2 O--, --OCF.sub.2 CF.sub.2 O--, or --CF.sub.2 CF.sub.2 O-- to form a cyclic bridge; provided R.sub.1 is other than H; C.sub.2 to C.sub.4 alkenyl, C.sub.2 to C.sub.4 haloalkenyl, C.sub.2 to C.sub.4 alkynyl, C.sub.2 to C.sub.4 haloalkynyl, C.sub.2 to C.sub.4 alkoxyalkyl, C.sub.2 to C.sub.4 alkylthioalkyl, C.sub.1 to C.sub.4 nitroalkyl, C.sub.2 to C.sub.4 cyanoalkyl, C.sub.3 to C.sub.6 alkoxycarbonylalkyl, C.sub.3 to C.sub.6 cycloalkyl, C.sub.3 to C.sub.6 halocycloalkyl, phenyl, benzyl, or phenyl or benzyl substituted with 1 to 3 substituents independently selected from W; attached to a single nitrogen atom, they can be taken together as CH.sub.2 4, CH.sub.2 5 or CH.sub.2 CH.sub.2 OCH.sub.2 CH.sub.2 ;
In the above definitions, the term "alkyl", used either alone or in compound words such as "alkylthio" or "haloalkyl", means straight chain or branched alkyl such as methyl, ethyl, n-propyl, isopropyl or the different butyl, pentyl, hexyl is

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patent: 4045169 (1977-08-01), Mengler
patent: 4070365 (1978-01-01), van Daalen et al.
patent: 4767779 (1988-08-01), Duggan
Vaughan, J. Org. Chem., 20 (1955), pp. 1619-1626.
Hassaneen et al., J. Heterocyclic Chem., 21 (1984), pp. 1013-1016.
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Gaudiano et al., Chem. Abst. 69, 27327y (1968).
Ezmirly et al., J. Heterocyclic Chem., 25, 257 (1988).
Meyer et al., Chemical Abstracts, vol. 52, Entry 7274c (1958).

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