Nitrogen-substituted heterocyclic derivatives and application thereof
A technology of heterocyclyl and heterocyclylalkyl, applied in a class of substituted nitrogen heterocyclic derivatives and its application field, can solve the problems of insignificant blood lipid-lowering effect, adverse reactions, and only injection preparations, etc.
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[0250] The general method of the present invention is further explained below, the compound of the present invention can be prepared by methods known in the art, and the preparation method of the preferred compound of the present invention is used as an example to illustrate in detail below, but the preparation method of the compound of the present invention is not limited thereto .
[0251] The preparation of the general formula compound (V) disclosed by the present invention is mainly prepared with reference to the following scheme:
[0252]
[0253] The above preparation route is described as follows: X1 and X2 are the starting materials of this scheme, which can be obtained from commercially available products, or prepared according to methods reported in literature. Compound V is obtained by coupling X1 and X2 under certain reaction temperature conditions and in the presence of certain basic reagents.
[0254] Taking the representative synthetic preparation process in...
Embodiment 1
[0301]
[0302] 1A (332mg, 1mmol) and dichloromethane were added to a 25ml round-bottomed flask, stirred and dissolved, and then 2B (229mg, 1.2mmol) and triethylamine (180μl, 1.3mmol) were added, stirred overnight, TLC detected that the reaction was complete, washed with water, The aqueous layer was extracted twice with ethyl acetate, the organic phases were combined, washed with saturated brine, dried over anhydrous sodium sulfate, concentrated and subjected to silica gel column chromatography to obtain the product compound 1 (412 mg, 90%). 1 HNMR (400MHz, CDCl 3)δ7.68 (dd, J=8.1, 4.1Hz, 4H), 7.40–7.28 (m, 4H), 6.79 (dd, J=46.0, 9.1Hz, 4H), 3.17 (ddd, J=9.4, 6.8, 4.0Hz,8H),2.45(s,6H); MS(ESI)m / z[M+H] + : 486.98.
Embodiment 2
[0304]
[0305] Add 2A (332 mg, 1 mmol) and dichloromethane into a 25 ml round bottom flask, stir and dissolve, add 2B (140 μl, 1.2 mmol) and triethylamine (180 μl, 1.3 mmol), stir overnight, TLC detects that the reaction is complete, wash with water, The aqueous layer was extracted twice with ethyl acetate, and the organic phases were combined, washed with saturated brine, dried over anhydrous sodium sulfate, concentrated and subjected to silica gel column chromatography to obtain the product Compound 2 (331 mg, 92%). 1 HNMR (400MHz, CDCl 3 )δ7.70(dd, J=8.3,1.7Hz,2H),7.43(d,J=1.0Hz,5H),7.31(d,J=7.8Hz,2H),6.92–6.83(m,2H), 6.82–6.74(m,2H),3.45(dd,J=238.2,77.4Hz,8H),2.45(s,3H); MS(ESI)m / z[M+H] + : 375.22.
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