33509-43-2

Basic information

• Product Name: 4-Amino-6-(tert-butyl)-3-mercapto-1,2,4-triazin-5(4H)-one
• Synonyms: 4-triazin-5(2h)-one,4-amino-6-(1,1-dimethylethyl)-3,4-dihydro-3-thioxo-2;BUTTPARK 22\07-82;4-AMINO-6-(TERT-BUTYL)-3-MERCAPTO-4,5-DIHYDRO-1,2,4-TRIAZIN-5-ONE;4-amino-6-tert-butyl-3-mercapto-1,2,4-triazin-5(4H)-one;4-AMINO-6-(1,1DIMETHYLETHYL)-3,4-DIHYDRO-3-THIOXO-1,2,4-TRIAZIN-5(2H)-ONE;4-Amino-3-mercapto-6-tert-butyl-1,2,4-triazine-5(4H)-one;4-amino-6-tert-butyl-3-sulfanylidene-2H-1,2,4-triazin-5-one
• CAS NO: 33509-43-2
• Molecular Formula: C₇H₁₂N₄OS
• Molecular Weight: 200.26
• EINECS: 251-548-4
• Mol File: 33509-43-2.mol
• Article Data: 15

Chemical Properties

• Melting Point: 215 °C(Solv: acetone (67-64-1); toluene (108-88-3))
• Boiling Point: 284.7 °C at 760 mmHg
• Flash Point: 126 °C
• Appearance: /
• Density: 1.4 g/cm³
• Vapor Pressure: 0.00293mmHg at 25°C
• Refractive Index: 1.656
• Storage Temp.: under inert gas (nitrogen or Argon) at 2–8 °C
• Solubility: Acetonitrile (Slightly), Chloroform (Slightly)
• PKA: 15.20±0.40(Predicted)
• CAS DataBase Reference: 4-Amino-6-(tert-butyl)-3-mercapto-1,2,4-triazin-5(4H)-one(CAS DataBase Reference)
• NIST Chemistry Reference: 4-Amino-6-(tert-butyl)-3-mercapto-1,2,4-triazin-5(4H)-one(33509-43-2)
• EPA Substance Registry System: 4-Amino-6-(tert-butyl)-3-mercapto-1,2,4-triazin-5(4H)-one(33509-43-2)

Safety Data

• Hazard Codes: Xi
• Hazardous Substances Data: 33509-43-2(Hazardous Substances Data)

Usage

Chemical Properties

White powder

InChI:InChI=1/C7H12N4OS/c1-7(2,3)4-5(12)11(8)6(13)10-9-4/h8H2,1-3H3,(H,10,13)

Synthetic route

trimethylpyruvic acid N-acetyl-amide (79848-80-9) + Thiocarbohydrazide (2231-57-4) → 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2)

Conditions	Yield
In hydrogenchloride; ethanol	95%
In hydrogenchloride; ethanol	95%

Thiocarbohydrazide (2231-57-4) + trimethylpyruvic acid (815-17-8) → 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2)

Conditions	Yield
With hydrogenchloride In water at 50 - 80℃; for 5h; pH=2 - 3;	85.3%
In ethanol for 12h; Reflux;
With hydrogenchloride In water at 50 - 80℃; for 5h; pH=2 - 3;	50 g
With hydrogenchloride at 20℃; for 6h; Large scale;
In ethanol for 12h; Reflux;

sulfuric acid (7664-93-9) + Thiocarbohydrazide (2231-57-4) + pivaloyl cyanide (42867-40-3) → 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2)

Conditions	Yield
With hydrogenchloride In water
With acetic anhydride In hydrogenchloride; water
With acetic anhydride In water

Thiocarbohydrazide (2231-57-4) + pivaloyl cyanide (42867-40-3) → 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2)

Conditions	Yield
With hydrogenchloride; hydrogen bromide In water; acetic acid
With hydrogenchloride In water; acetic acid

2,2-dibromo-3,3-dimethyl butyric acid (59742-86-8) + 2-bromo-2-tert-butyl acetic acid (50364-40-4) + tert-Butylacetic acid (1070-83-3) + Thiocarbohydrazide (2231-57-4) + phosphorus trichloride (7719-12-2, 52843-90-0) → 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2)

Conditions	Yield
With bromine In methanol; water

pyridinium 2,2-dibromo-3,3-dimethyl butyrate (59742-88-0) + Thiocarbohydrazide (2231-57-4) → 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2)

Conditions	Yield
In methanol; water

morpholine (110-91-8) + 3,3-dimethyl-butan-2-one (75-97-8) → 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2)

Conditions	Yield
With sulphur dichloride In water

1,1-dichloro-3,3-dimethylbutan-2-one (22591-21-5) → 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2)

Conditions	Yield
Multi-step reaction with 3 steps 1: sodium carbonate; dimethyl sulfoxide / 2 h / 80 °C 2: dihydrogen peroxide / water / 1 h / 25 °C 3: hydrogenchloride / water / 5 h / 50 - 80 °C / pH 2 - 3 View Scheme
Multi-step reaction with 3 steps 1: water / 20 °C / Alkaline conditions; Large scale 2: dihydrogen peroxide; 1-butyl-3-methylimidazolium Tetrafluoroborate / 8 h / 20 °C / Large scale 3: hydrogenchloride / 6 h / 20 °C / Large scale View Scheme

1-chloro-3,3-dimethyl-butan-2-one (13547-70-1) → 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2)

Conditions	Yield
Multi-step reaction with 3 steps 1: sodium hydroxide / water / 2 h / 110 °C 2: sodium carbonate; oxygen; palladium 10% on activated carbon / water / 5 h / 25 °C / pH 8 - 9 3: hydrogenchloride / water / 5 h / 50 - 80 °C / pH 2 - 3 View Scheme

3,3-dimethyl-butan-2-one (75-97-8) → 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2)

Conditions	Yield
Multi-step reaction with 4 steps 1: chlorine / 40 - 50 °C / Large scale 2: water / 20 °C / Alkaline conditions; Large scale 3: dihydrogen peroxide; 1-butyl-3-methylimidazolium Tetrafluoroborate / 8 h / 20 °C / Large scale 4: hydrogenchloride / 6 h / 20 °C / Large scale View Scheme

C11H5Cl3O3 + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → 7-[5-(2,4,5-trichlorophenyl)-2-furyl]-3-t-butyl-4(H)-1,3,4-thiadiazolo[2,3-c]-1,2,4-triazin-4-one

Conditions	Yield
With trichlorophosphate for 6h; Heating;	95%

5-(4-chloro-2-nitrophenyl)-2-furoic acid (95611-88-4) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → C18H14ClN5O4S

Conditions	Yield
With trichlorophosphate for 6h; Heating;	95%

methyl chlorosulfate (812-01-1) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → 4-amino-6-tert-butyl-3-methylthio-1,2,4-triazin-5(4H)-one (21087-64-9)

Conditions	Yield
In sulfuric acid	95%

4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) + methyl trifluoromethanesulfonate (333-27-7) → 4-amino-6-tert-butyl-3-methylthio-1,2,4-triazin-5(4H)-one (21087-64-9)

Conditions	Yield
With trifluorormethanesulfonic acid In toluene at 8 - 25℃; for 3h; Temperature;	94%

dimethyl sulfate (77-78-1) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → 4-amino-6-tert-butyl-3-methylthio-1,2,4-triazin-5(4H)-one (21087-64-9)

Conditions	Yield
With sodium carbonate; potassium iodide In acetone at 25 - 30℃; for 5h; Temperature;	93.56%
With sodium carbonate; potassium iodide In acetone at 40 - 45℃; for 4h; Temperature; Concentration;	93.56%
With sulfuric acid In para-xylene at 70 - 80℃; for 7.5h; Temperature;	92.1%
With sodium carbonate; potassium iodide In acetone at 30 - 35℃; for 3h; Temperature;	293.6 g

methyl bromide (74-83-9) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → 4-amino-6-tert-butyl-3-methylthio-1,2,4-triazin-5(4H)-one (21087-64-9)

Conditions	Yield
With sodium hydroxide; sodium sulfite In water at 50℃; for 1h; pH=8.5; Reagent/catalyst; Temperature; Inert atmosphere;	93.5%
With sodium hydroxide In MML (metribuzin mother liquor, which is filtrate from a prior metribuzin synthesis) at 25 - 55℃; for 2.5 - 3h; Product distribution / selectivity;
With sodium hydroxide In MML (metribuzin mother liquor, which is filtrate from a prior metribuzin synthesis); water at 25 - 50℃; for 2.5h; Product distribution / selectivity;
With sodium hydroxide In water at 25 - 50℃; for 2.5 - 3.16667h; Product distribution / selectivity;
Stage #1: 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one With sodium hydroxide; sodium sulfite In MML (metribuzin mother liquor, which is filtrate from a prior metribuzin synthesis) for 0.5h; pH=10.5 - 11.0; Stage #2: methyl bromide In MML (metribuzin mother liquor, which is filtrate from a prior metribuzin synthesis) at 15 - 55℃; for 3.16667h; Product distribution / selectivity;

5-(3,4-dichlorophenyl)furan-2-carboxylic acid (54023-01-7) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → C18H14Cl2N4O2S

Conditions	Yield
With trichlorophosphate for 6h; Heating;	92%

5-(2-chloro-5-trifluoromethylphenyl)furan-2-carboxylic acid (302911-88-2) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → C19H14ClF3N4O2S

Conditions	Yield
With trichlorophosphate for 6h; Heating;	91%

5-((4-methoxy)phenyl)furan-2-carboxylic acid (52938-99-5) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → C19H18N4O3S

Conditions	Yield
With trichlorophosphate for 6h; Heating;	90%

5-(3-trifluoromethylphenyl)furan-2-carboxylic acid (54022-99-0) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → C19H15F3N4O2S

Conditions	Yield
With trichlorophosphate for 6h; Heating;	90%

5-(2-(trifluoromethyl)phenyl)furan-2-carboxylic acid (92973-24-5) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → 7-[5-(2-trifluoromethylphenyl)-2-furyl]-3-t-butyl-4H-1,3,4-thiadiazolo[2,3-c]-1,2,4-triazin-4-one

Conditions	Yield
With trichlorophosphate for 6h; Heating;	88%

5-p-tolyl-furan-2-carboxylic acid (52938-98-4) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → C19H18N4O2S

Conditions	Yield
With trichlorophosphate for 6h; Heating;	87%

5-(3-nitro-phenyl)-furan-2-carboxylic acid (13130-13-7) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → C18H15N5O4S

Conditions	Yield
With trichlorophosphate for 6h; Heating;	86%

4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) + 5-(2,4-dichlorophenyl)furan-2-carboxylic acid (134448-46-7) → 3-tert-butyl-7-[5-(2,4-dichloro-phenyl)-furan-2-yl]-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one

Conditions	Yield
With trichlorophosphate for 5h; Heating;	85%

4-Fluorobenzoic acid (456-22-4) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → 3-tert-butyl-7-(4-fluoro-phenyl)-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one

Conditions	Yield
With trichlorophosphate In toluene; acetonitrile for 6h; Heating;	85%

4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) + 4-fluoro-3-phenoxy benzoic acid (77279-89-1) → 3-tert-butyl-7-(4-fluoro-3-phenoxy-phenyl)-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one

Conditions	Yield
With trichlorophosphate In toluene; acetonitrile for 6h; Heating;	85%

5-(2,5-dichlorophenyl)furan-2-carboxylic acid (186830-98-8) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → C18H14Cl2N4O2S

Conditions	Yield
With trichlorophosphate for 6h; Heating;	85%

5-(4-methyl-2-nitrophenyl)furan-2-carboxylic acid (55377-91-8) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → C19H17N5O4S

Conditions	Yield
With trichlorophosphate for 6h; Heating;	85%

oxalic acid (144-62-7) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → 3,3'-di-tert-butyl-[7,7']bi[[1,3,4]thiadiazolo[2,3-c][1,2,4]triazinyl]-4,4'-dione

Conditions	Yield
With trichlorophosphate for 5h; Heating;	84%

5-(4-methoxy-2-nitrophenyl)-2-furancarboxylic acid (95611-90-8) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → C19H17N5O5S

Conditions	Yield
With trichlorophosphate for 6h; Heating;	84%

5-(4-nitrophenyl)-furan-2-carboxylic acid (28123-73-1) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → 3-tert-butyl-7-[5-(4-nitro-phenyl)-furan-2-yl]-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one

Conditions	Yield
With trichlorophosphate for 5h; Heating;	83%

5-(4-bromophenyl)furan-2-carboxylic acid (52938-96-2) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → 7-[5-(4-bromo-phenyl)-furan-2-yl]-3-tert-butyl-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one

Conditions	Yield
With trichlorophosphate for 5h; Heating;	82%

4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) + 5-(3-chloro-4-fluorophenyl)-2-furoic acid (496044-15-6) → 3-tert-butyl-7-[5-(3-chloro-4-fluoro-phenyl)-furan-2-yl]-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one

Conditions	Yield
With trichlorophosphate for 5h; Heating;	81%

5-(4-chlorophenyl)-2-furoic acid (41019-45-8) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → 3-tert-butyl-7-[5-(4-chloro-phenyl)-furan-2-yl]-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one

Conditions	Yield
With trichlorophosphate for 5h; Heating;	80%

4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) + 2,4-dichloro-5-fluoro-benzoic acid (86522-89-6) → 3-tert-butyl-7-(2,4-dichloro-5-fluoro-phenyl)-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one

Conditions	Yield
With trichlorophosphate In toluene; acetonitrile for 6h; Heating;	80%

dimethyl sulfate (77-78-1) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → 4-amino-6-t-butyl-2,3-dihydro-2-methyl-3-thioxo-1,2,4-triazin-5(4H)-one + 4-amino-6-tert-butyl-3-methylthio-1,2,4-triazin-5(4H)-one (21087-64-9)

Conditions	Yield
With sodium methylate In methanol for 1h; Heating;	A 78% B 26%
With sodium methylate In methanol for 1h; Heating;	A 68% B 26%

malonic acid (141-82-2) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → C17H20N8O2S2

Conditions	Yield
With trichlorophosphate for 5h; Heating;	78%

2,4,5-Trichlorophenoxyacetic acid (93-76-5) + 4-amino-3-mercapto-6-tert-butyl-1,2,4-triazin-5-one (33509-43-2) → 3-tert-butyl-7-[(2,4,5-trichlorophenoxy)methyl]-4H-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one (1621091-21-1)

Conditions	Yield
With trichlorophosphate at 90℃; for 8h;	78%

Upstream product

• 2231-57-4 Thiocarbohydrazide 
• 42867-40-3 pivaloyl cyanide 
• 79848-80-9 trimethylpyruvic acid N-acetyl-amide 
• 38941-46-7 methyl trimethylpyruvate 
• 130231-67-3 2,5-dihydrazino-1,3,4-thiadiazole dihydrochloride 
• 815-17-8 trimethylpyruvic acid 
• 43165-46-4 sodium 3,3-dimethyl-2-oxobutyrate 
• 21087-64-9 4-amino-6-tert-butyl-3-methylthio-1,2,4-triazin-5(4H)-one 
• 60166-88-3 2-(1-Carboxy-2,2-dimethylpropylidene)carbonothioic dihydrazide 
• 75-97-8 3,3-dimethyl-butan-2-one 
• 13547-70-1 1-chloro-3,3-dimethyl-butan-2-one 
• 22591-21-5 1,1-dichloro-3,3-dimethylbutan-2-one 
• 110-91-8 morpholine 
• 59742-88-0 pyridinium 2,2-dibromo-3,3-dimethyl butyrate 

Downstream Products

• 21087-64-9 4-amino-6-tert-butyl-3-methylthio-1,2,4-triazin-5(4H)-one 
• 85485-26-3 3-tert-Butyl-7-phenyl-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one 
• 1621091-11-9 3-tert-butyl-7-[(4-chlorophenoxy)methyl]-4H-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one 
• 1621091-12-0 3-tert-butyl-7-[(2,4-dichlorophenoxy)methyl]-4H-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one 
• 1621091-13-1 3-tert-butyl-7-[(2,3,5-trimethylphenoxy)methyl]-4H-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one 
• 1621091-14-2 3-tert-butyl-7-[(2,6-dimethylphenoxy)methyl]-4H-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one 
• 1621091-15-3 3-tert-butyl-7-[(2-nitrophenoxy)methyl]-4H-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one 
• 1621091-16-4 3-tert-butyl-7-[(4-hydroxyphenoxy)methyl]-4H-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one 
• 1621091-17-5 3-tert-butyl-7-[(2-methoxyphenoxy)methyl]-4H-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one 
• 1621091-18-6 3-tert-butyl-7-(phenoxymethyl)-4H-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one 
• 1621091-19-7 3-tert-butyl-7-[2-(4-chlorophenoxy)propan-2yl]-4H-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one 
• 1621091-20-0 3-tert-butyl-7-[(2-chlorophenoxy)methyl]-4H-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one 
• 1621091-21-1 3-tert-butyl-7-[(2,4,5-trichlorophenoxy)methyl]-4H-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one 
• 1621091-22-2 3-tert-butyl-7-[(4-iodophenoxy)methyl]-4H-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one 

Relevant articles and documents

Crystal structure, mosquito larvicidal & antifungal activity of 3?tert?butyl?7-(2,3,4-trimethoxyphenyl)-4H-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one

The title compound 3?tert?butyl?7-(2,3,4-trimethoxyphenyl)-4H-[1,3,4]thiadiazolo[2,3-c][1,2,4]triazin-4-one was prepared and characterized using single crystal X-ray diffraction, thermal & Uv-Vis analysis, FTIR, NMR (1H, 13C) and Mas

Triazinone preparation method

The invention relates to a triazinone preparation method, which comprises: carrying out a hydrolysis reaction on 1-chloropinacolone at a temperature of 80-140 DEG C under the actions of a solvent andan alkali to obtain a compound I, wherein the solvent is water; carrying out an oxidation reaction on the compound I in the presence of oxygen by using Pt as a catalyst under a neutral or weakly basiccondition to obtain a compound II; and carrying out a ring closure reaction on the compound II and thiocarbohydrazide under the catalysis of an acid to obtain triazinone, wherein the structure formula of the compound I is defined in the specification, and the structure formula of the compound II is defined in the specification. According to the present invention, 1-chloropinacolone is used as theraw material, and the water is used as the solvent, such that the generation of high salt wastewater can be avoided; Pt is used as the catalyst, and oxygen is used as the oxidant, such that the use of hydrogen peroxide can be avoided, and the catalyst can be recycled so as to reduce the raw material cost; and the production method is simple, meets the environmentally friendly requirement, and issuitable for industrial production, and the yield and the content of the final product are high.

Synthesis of novel thiadiazolotriazin-4-ones and study of their mosquito-larvicidal and antibacterial properties

A series of novel 3-tert-butyl-7-(aryloxymethyl)-4H-[1,3,4]thiadiazolo[2,3- c][1,2,4]triazin-4-ones (5a-5n) were synthesized by refluxing 3,3-dimethyl-2-oxobutanoic acid (trimethyl pyruvic acid) (1) and thiocarbohydrazide (2) in ethanol as solvent for 12 h, to yield 3-mercapto-4-amino-6-tert-butyl-1,2,4-triazine-5(4H)-one (3) (Scheme 1), then the compound (3) was condensed with different substituted aryloxyacetic acids (4) in POCl3 at 90 °C for 8 h (Scheme 2). The structures of the newly synthesized compounds were confirmed by IR, 1H NMR, 13C NMR, elemental analyses and mass spectroscopic studies. Few of the synthesized compounds exhibited moderate mosquito-larvicidal and antibacterial activities. Among the novel derivatives, the compound (5f) showed relatively high larvicidal activity against a malaria vector. Compounds (5i) and (5m) exhibited a broad spectrum antibacterial activity against Gram positive and Gram negative species and hence they may be considered as drug candidates for bacterial pathogens.