FUNGICIDES Fungicides used in agriculture to control plant diseases belong to various chemical

1.4 FUNGICIDES Fungicides used in agriculture to control plant diseases belong to various chemical

classes. A wide variation of physicochemical properties of these substances can be observed, according to the different chemical structures of fungicides. Some fungi- cides are stereoisomers and they are normally commercialized as mixtures of these isomers. Fungicides can be applied pre- or postharvest for the protection of cereals, fruits, and vegetables from fungal diseases.

1.4.1 A ZOLES

N Cyproconazole

The imidazole ring is present in several biologically active compounds, while others have a triazole ring. These compounds are fungicides with systemic action, effective against several phytopathogenous fungi and recommended for seed dressing, as well as foliage fungicide and postharvest application in fruits. They are scarcely soluble in water, although their salts are soluble in water (Table 1.18).

1.4.2 B ENZIMIDAZOLES

HN

Thiabendazole

Fungicides of the benzimidazole type have a systemic action. Generally, they are taken up by the roots of the plants, and the active substances are then acropetally translocated through the xylem to the leaves. These compounds have been used in plant protection in the form of their insoluble salts. They are foliage and soil

24 TABLE 1.17 Chemical Names and Properties of Pyrethroid Insecticides

Water Solubility Half-Life in Common Name

Vapor Pressure

K ow

mg=L (258C) Soil (Days) Acrinathrin

IUPAC Name

mPa (208C)

log P

(S)-a-Cyano-3-phenoxybenzyl (Z)-(1R,3S)-2,2-dimethyl- 4.4 3 10 5 5.6 5 –100 C 26 H 21 F 6 NO 5 3-[2-(2,2,2-trifluoro-1-trifluoromethyl ethoxycarbonyl)vinyl] cyclopropanecarboxylate

Analysis Cyfluthrin

(RS)-a-Cyano-4-fluoro-3-phenoxybenzyl(1RS,3RS;

56 C 22 H 18 Cl 2 FNO 3 1RS,3SR)-3-(2,2-dichlorovinyl)-2,2-dimethyl

I: 2.2 3 10 3a –63 cyclopropanecarboxylate

IV: 2.9 3 10 3 Pesticides Cypermethrin

IV: 8.5 3 10 5 IV:5.9

60 C 22 H 19 Cl 2 NO 3 3-(2,2-dichlorovinyl)-2,2-dimethyl cyclopropanecarboxylate Deltamethrin

(RS)-a -Cyano-3-phenoxybenzyl(1RS,3RS; 1RS,3SR)-

(S)-a-Cyano-3-phenoxybenzyl(1R,3R)-3-(2,2-dibromovinyl)- 1.24 3 10 5b 4.6 <0.2 3 10 3 23 in C 22 H 19 Br 2 NO 3 2,2-dimethyl cyclopropanecarboxylate

Food Esfenvalerate

35 –88 C 25 H 22 ClNO 3 3-methylbutyrate Tau-fluvalinate

(S)-a-Cyano-3-phenoxybenzyl-(S)-2-(4-chlorophenyl)-

2 3 10 4b 6.22 0.002

(RS)-a-Cyano-3-phenoxybenzyl-N-(2-chloro- 9 3 10 8 4.26 0.001 a 12 –92 and

Environmental Permethrin

C 26 H 22 ClF 3 N 2 O 3 a ,a,a-trifluoro-p-tolyl)- D -valinate

3-Phenoxybenzyl-(1RS,3RS;1RS,3SR)-

6.1 a 6 3 10 3a <38 C 21 H 20 Cl 2 O 3 3-(2,2-dichlorovinyl)-2,2-dimethylcyclopropane carboxylate

cis : 0.0025

trans : 0.0015

Sources: Data from Tomlin, C. (Ed.) in The Pesticide Manual, British Crop Protection Council, 2000; http:==ec.europa.eu=food=plant=protection=evaluation=exist _subs_rep_en.htm; http:==www.epa.gov=opprd001=factsheets=; Hornsby, A.G., Wauchope, R.D., and Herner, A.E. in Pesticide Properties in the Environment, Springer-Verlag, New York, 1996; De Liñan, C. in Farmacología Vegetal, Ediciones Agrotecnicas S.L., 1997.

Samples a 208C. b 258C.

Pesticides:

TABLE 1.18 Chemical Names and Properties of Azole Fungicides

Classi

Water Solubility Half-Life in Common Name

Vapor Pressure

K ow

mg=L (208C) Soil (Days) fi cation Cyproconazole

IUPAC Name

mPa (208C)

log P

(2RS,3RS;2RS,3SR)-2-(4-Chlorophenyl)-3-cyclopropyl-1-(1H-1,2,4-triazol-1-yl) 0.04 2.91 140 a 90 C 15 H 18 ClN 3 O

butan-2-ol and Flusilazole

Bis(4-fluorophenyl)(methyl)(1H-1,2,4-triazol-1-ylmethyl)silane 0.04 a 3.74 54 95 C 16 H 15 F 2 N 3 Si

Properties Hexaconazole

3.9 17 — C 14 H 17 Cl 2 N 3 O Imazalil

(RS)-2-(2,4-Dichlorophenyl)-1-(1H-1,2,4-triazol-1-yl)hexan-2-ol

3.82 180 150 C 14 H 14 Cl 2 N 2 O Prochloraz

N -Propyl-N-[2-(2,4,6-trichlorophenoxy)ethyl]imidazole-1-carboxamide 0.09 4.12 34.4 a 120 C 15 H 16 Cl 3 N 3 O 2 Propiconazole

0.03 3.72 100 110 C 15 H 17 Cl 2 N 3 O 2 Tebuconazole

3.7 36 — C 16 H 22 ClN 3 O Triadimefon

(RS)-1-p-Chlorophenyl-4,4-dimethyl-3-(1H-1,2,4-triazol-1-ylmethyl)pentan-3-ol

(1-(4-Chlorophenoxy)-3,3-dimethyl-1-(1H-1,2,4-triazol-1-yl)butan-2-one 0.02 3.11 64 6 –60 C 14 H 16 ClN 3 O 2

Sources: Data from Tomlin, C. (Ed.) in The Pesticide Manual, British Crop Protection Council, 2000; http:==ec.europa.eu=food=plant=protection=evaluation=exist _subs_rep_en.htm; http:==www.epa.gov=opprd001=factsheets=; Hornsby, A.G., Wauchope, R.D., and Herner, A.E. in Pesticide Properties in the Environment, Springer-Verlag, New York, 1996; De Liñan, C. in Farmacología Vegetal, Ediciones Agrotecnicas S.L., 1997.

a 258C. 25

26 Analysis of Pesticides in Food and Environmental Samples

TABLE 1.19 Chemical Names and Properties of Benzimidazole Fungicides

Water Half-Life Common

Vapor

K ow Solubility in Soil Name

IUPAC

Pressure

log P mg=L (258C) (Days) Benomyl

Name

mPa (258C)

1.37 0.003 67 C 14 H 18 N 4 O 3 benzimidazol-2-ylcarbamate Carbendazim

Methyl 1-(butyl carbamoyl)

Methyl benzimidazol- 0.15 1.51 8 120 C 9 H 9 N 3 O 2 2-yl carbamate Thiabendazole

2-(Thiazol-4-yl)benzimidazole 4.6 3 10 4 2.39 30 a 33 –120 C 10 H 7 N 3 S

Sources: Data from Tomlin, C. (Ed.) in The Pesticide Manual, British Crop Protection Council, 2000; http:==ec.europa.eu=food=plant=protection=evaluation=exist_subs_rep_en.htm; http:==www.epa .gov=opprd001=factsheets=; Hornsby, A.G., Wauchope, R.D., and Herner, A.E. in Pesticide Properties in the Environment , Springer-Verlag, New York, 1996; De Liñan, C. in Farmacología Vegetal , Ediciones Agrotecnicas S.L., 1997.

a 208C.

fungicides with a specific and broad spectrum of action, also used for seed treatment and in postharvest (Table 1.19).

1.4.3 D ITHIOCARBAMATES Ethylenebisdithiocarbamates are prepared from ethylene diamine H 2 N –CH 2 –

CH 2 –NH 2 . [SC(S)NHCH 2 CH 2 NHCSSMn] x Zn y

Mancozeb

These compounds are heavy metal salts of ethylenebisdithiocarbamate and these salts are unusually stable and suitable as fungicides. The dithiocarbamate fungicides are the most widely used organic fungicides and have a wide spectrum of activity as foliar sprays for fruits, vegetables, and ornamentals and as seed protectants (Table 1.20).

1.4.4 M ORPHOLINES

CH 3

CH 3

(H 3 C) 3 C CH 2 CHCH 2 N

CH 3

Fenpropimorph

Morpholines are specific systemic fungicides against powdery mildew fungi and are used to control the disease in cereals, cucumbers, apples, and so on. These

Pesticides: Classification and Properties 27

TABLE 1.20 Chemical Names and Properties of Dithiocarbamate Fungicides

Vapor

Water

Solubility Half-Life Common

Pressure

K ow mg=L in Soil Name

IUPAC

mPa

log P (258C) (Days) Mancozeb

Name

(208C)

1.8 6.2 6 –15 (C 4 H 6 MnN 2 S 4 ) x (Zn) y

Manganese ethylenebis

(dithiocarbamate) (polymeric) complex with zinc salt

Maneb Manganese

0.45 257 25 C 4 H 6 MnN 2 S 4 ethylenebis (dithiocarbamate)

Metiram Zinc ammoniate

0.3 0.1 20 (C 16 H 33 N 11 S 16 Zn 3 ) x

ethylenebis (dithiocarbamate)- poly(ethylenethiuram disulfide)

Nabam Disodium ethylenebis

Negligible

C 4 H 6 N 2 Na 2 S 4 (dithiocarbamate) Zineb

10 23 (C 4 H 6 N 2 S 4 Zn) x

Zinc ethylenebis

(dithiocarbamate) (polymeric)

Ziram Zinc bis

1.23 1.58 –18.3 a 2 C 6 H 12 N 2 S 4 Zn

(dimethyldithiocarbamate) Sources: Data from Tomlin, C. (Ed.) in The Pesticide Manual, British Crop Protection Council, 2000;

http:==ec.europa.eu=food=plant=protection=evaluation=exist_subs_rep_en.htm; http:==www.epa .gov=opprd001=factsheets=; Hornsby, A.G., Wauchope, R.D., and Herner, A.E. in Pesticide Properties in the Environment , Springer-Verlag, New York, 1996; De Liñan, C. in Farmacología Vegetal , Ediciones Agrotecnicas S.L., 1997.

a 208C.

compounds are distributed in the plants by translocation from the root and foliage and protect the plants against infection by phytopathogenic fungi. They have a certain persistence in soil (Table 1.21).

1.4.5 M ISCELLANEOUS

CN

Cl

Cl

SCCl 3

Cl

CN

Cl

Captan

Chlorothalonil

28 Analysis of Pesticides in Food and Environmental Samples

TABLE 1.21 Chemical Names and Properties of Morpholine Fungicides

Water

Vapor

Solubility Half-Life

K ow mg=L in Soil Common Name

Pressure

log P (208C) (Days) Dodemorph

IUPAC Name

mPa (208C)

4-Cyclododecyl- 0.48 4.14 <100 73 C 18 H 35 NO

2,6-dimethyl morpholine

Fenpropimorph 3.5 4.2 4.3 15 –93 C 20 H 33 NO

Butylphenyl)- 2-methylpropyl]-2, 6-dimethylmorpholine

Tridemorph 2,6-Dimethyl- 12 4.2 1.1 14 –34 C 19 H 39 NO

4-tridecyl morpholine Sources: Data from Tomlin, C. (Ed.) in The Pesticide Manual, British Crop Protection Council, 2000;

http:==ec.europa.eu=food=plant=protection=evaluation=exist_subs_rep_en.htm; http:==www.epa .gov=opprd001=factsheets=; Hornsby, A.G., Wauchope, R.D., and Herner, A.E. in Pesticide Properties in the Environment , Springer-Verlag, New York, 1996; De Liñan, C. in Farmacología Vegetal , Ediciones Agrotecnicas S.L., 1997.

Captan and folpet are fungicides used in foliar treatment of fruits, vegetables, and ornamentals, in soil and seed treatments, and in postharvest applications.

Procymidone is a dicarboximide-derived fungicide with moderate systemic action. It is rapidly absorbed not only through the roots but also through the stem or the leaves. It is used for the control of storage roots of fruits and vegetables and it is effective for seed dressing of cereals. Table 1.22 summarizes the properties of various frequently used fungicides belonging to different chemical classes.