Preparation method of 1,7-m-carborane dihydroxyl substituted derivatives
A carborane and dihydroxyl technology, which is applied in the field of preparation of 1,7-m-carborane dihydroxyl substituted derivatives, can solve problems such as expensive raw materials, difficult post-processing, incomplete reaction, etc.
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Embodiment 1
[0033] The preparation method of the 1,7-bishydroxymethyl-m-carborane of the present embodiment comprises the following steps:
[0034]
[0035] (1) Add 12.2 g of decaborane and 25 g of acetonitrile into a reactor with a reflux device, stir and raise the temperature, and under reflux conditions, add 18.3 g of 1,4-diacetoxy-2-butyne shown in formula VIa , the reaction was carried out at 80°C, and the end point of the reaction was determined by thin-layer chromatography (developing agent: PE (petroleum ether): EA (ethyl acetate) = 5:1, Rf was 0.4), and the reaction was completed after 4 hours. Petroleum ether was extracted three times, and the compound represented by formula IIIa (26.5 g, yield 92.0%) was obtained after recovering petroleum ether.
[0036]
[0037] (2) In an inert environment, 26.5 g of the compound represented by formula IIIa was added into the rearrangement reactor at a constant rate, and the reaction was completed after reacting at 200° C. for 5 hours, ...
Embodiment 2
[0046]The preparation method of the 1,7-bishydroxymethyl-m-carborane of the present embodiment comprises the following steps:
[0047]
[0048] (1) Add 122.3 g of decaborane and 245 g of acetonitrile into a reactor with a reflux device, stir and raise the temperature, and under reflux conditions, add 367 g of 1,4-diacetoxy-2-butyne shown in formula VI, The reaction was carried out at 50°C, and the end point of the reaction was determined by thin-layer chromatography (developing agent: PE: EA = 5: 1, Rf 0.4). After 8 hours of reaction, the reaction was terminated, extracted three times with 150 mL of petroleum ether, and the solvent was recovered to obtain the formula Compound indicated by III (269.5 g, yield 93.5%).
[0049]
[0050] (2) In an inert environment, 269.5 g of the compound represented by formula III was heated to 270° C., and the reaction was completed after 4 hours of reaction, and separated by column chromatography.
[0051] The separation conditions of t...
Embodiment 3
[0058] The preparation method of the 1,7-bishydroxymethyl-m-carborane of the present embodiment comprises the following steps:
[0059]
[0060] (1) Add 122.3 g of decaborane and 611.5 g of dimethyl sulfide into a reactor with a reflux device, stir and raise the temperature, and under reflux conditions, add 1,4-diacetoxy-2- Butyne 611.5g, reacted at 60°C, determined the end point of the reaction by thin-layer chromatography (developer: PE:EA=5:1, Rf 0.4), ended the reaction after 10 hours, extracted 300mL*3 with petroleum ether , after recovering the solvent, the compound represented by formula III (270.9 g, yield 94.0%) was obtained.
[0061]
[0062] (2) In an inert environment, heat up 270.9 g of the compound shown in formula III to 300° C., finish the reaction after 1.5 hours of reaction, and separate by column chromatography (the conditions for column chromatography separation are the same as in Example 2) to obtain the compound obtained by formula IIa. For the com...
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