Process for the preparation of benzohetero[1,3]oxadiazole compounds disubstituted with heteroaryl groups
An azole compound, disubstituted technology, applied in organic chemistry, photovoltaic power generation, etc., can solve the problems of long temperature and reaction time, long process time, high processing cost, etc., and achieve short temperature and reaction time, short process time, low cost. The effect of energy cost
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example 1
[0094] Preparation of 4,7-di-2-thienyl-2,1,3-benzothiadiazoles of formula (a)
[0095]
[0096] 4,7-dibromo-2,1,3-benzothiadiazole (0.294g, 1.0mmol), potassium acetate (0.295g, 3.0mmol), N,N-dimethylacetamide (5ml ), thiophene (0.842g, 10mmol) and palladium(II) acetate [Pd(OAc) 2 ] (1.2 mg, 0.005 mmol) was charged to a 10 ml Pyrex glass reactor fitted with a screw cap.
[0097] The reactor was preheated to 130°C in an oil bath and stirred vigorously for 4 hours. After cooling to room temperature (25°C), the reaction mixture was put into a saturated solution of sodium chloride (25ml) and extracted with ethyl acetate (3x25ml). The organic base obtained was dried over anhydrous sodium sulfate and evaporated. The obtained residue (brown solid) was purified by flash chromatography on silica gel using a mixture of n-heptane / ethyl acetate (1 / 1, v / v) as eluent to obtain 240 mg of pure 4,7-di-2-thienyl-2,1,3-benzothiadiazole (yield 80%).
[0098] The 4,7-di-2-thienyl-2,1,3-be...
example 2
[0101] Preparation of 4,7-bis-(5'-acetylthienyl)-2,1,3-benzothiadiazole having formula (b)
[0102]
[0103] 4,7-dibromo-2,1,3-benzothiadiazole (0.294g, 1.0mmol), potassium acetate (0.295g, 3.0mmol), N,N-dimethylacetamide (5ml ), 1-(thiophen-2-yl)ethanone (0.631g, 5mmol) and palladium(II) acetate [Pd(OAc) 2 ] (1.2 mg, 0.005 mmol) was charged to a 10 ml Pyrex glass reactor fitted with a screw cap.
[0104] The reactor was preheated to 120°C in an oil bath and stirred vigorously for 18 hours. Subsequent work-up as described in Example 1 afforded 339 mg of pure 4,7-bis-(5'-acetylthienyl)-2,1,3-benzothiadiazole as a red solid (88% yield) .
[0105] The 4,7-bis-(5'-acetylthienyl)-2,1,3-benzothiadiazole is passed 1 H-NMR (400MHz, CDCl 3 ), the following spectra were obtained: δ=8.13(d, J=4.0Hz, 2H), 7.96(s, 2H), 7.76(d, J=4.0Hz, 2H), 2.62(s, 6H).
[0106] The 4,7-bis-(5'-acetylthienyl)-2,1,3-benzothiadiazole was also characterized by MS mass analysis to obtain the followi...
example 3
[0108] Preparation of 4,7-bis-(5'-hexyl-2,2'-dithienyl)-2,1,3-benzothiadiazole having formula (c)
[0109]
[0110] 4,7-dibromo-2,1,3-benzothiadiazole (0.294g, 1.0mmol), potassium acetate (0.295g, 3.0mmol), N,N-dimethylacetamide (5ml), 5-hexyl-2,2'-dithiophene (1.252g, 5mmol) and palladium(II) acetate [Pd(OAc) 2 ] (1.2 mg, 0.005 mmol) was charged to a 10 ml Pyrex glass reactor fitted with a screw cap.
[0111] The reactor was preheated to 10°C in an oil bath and stirred vigorously for 18 hours. Subsequent work-up as described in Example 1 afforded 512 mg of pure 4,7-bis-(5'-hexyl-2,2'-bithienyl)-2,1,3-benzothiadiazole as a red solid (Yield 81%).
[0112] The 4,7-bis-(5'-hexyl-2,2'-dithienyl)-2,1,3-benzothiadiazole is passed 1 H-NMR (400MHz, CDCl 3 ) characterization, the following spectra were obtained: δ=8.03(d, J=4.0Hz, 2H), 7.83(s, 2H), 7.19(d, J=4.0Hz, 2H), 7.11(d, J=3.6Hz, 2H ), 6.73(d, J=3.6Hz, 2H), 2.82(t, J=7.6Hz, 4H), 1.73-1.69(m, 4H), 1.42-1.39(m, 4H), 1.3...
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