A series of novel 6-substituted quinazoline derivatives were synthesised as epidermal growth factor receptor(EGFR) and Human epidermal growth factor receptor 2 (HER2)inhibitors in our lab. The novel compounds were measured for their dual enzyme inhibition as well as their cytotoxic activity on MCF7 cell line. The results revealed that all the compounds showed inhibition of both enzymes. Compound 5c showed the best inhibitory activity against both enzymes and IC50 of its was 2.6 nM against EGFR kinases and 4.3 nM against HER2 kinases, respectively. Most of the measured compounds showed to antitumor activity on MCF7.

The target compound Febuxostat was synthesized from the cheap material p-hydroxyl-benzoic acid by a ten-step reaction, including esterification, halogeno, ammonolysis, thio, Hantzsch reaction, Duff reaction, etherification, and hydrolysis. The total yield was 10. 87%. The structure of Febuxostat was confirmed by IR, MS, 1 H-NMR and 13 C -NMR. The research results indicated that the toxicity and the cost of this synthetic route were reduced, the operation was simple. This method was suitable for industrial manufacture.

AbstractThe reaction works with 1,1′‐biphenyl‐2‐carboxylic acids only.

The key intermediate, ethyl 3-[2-{[(4-cyanophenyl) amino] methyl}-1-methyl-N-(pyri-din-2-yl)-1H-benzo[d] imidazole-5-carboxamido]propanoate, in total yield of 79.6%, was synthe-sized by ammoniation reaction of 4-aminobenzonitrile, then amidation with ethyl 3-{[ 3-amino-4-(methylamino) benzoyl]-pyridin-2-ylamino}propanoate and ring-formation.The structure was con-firmed by 1 H NMR and ESI-MS.

Dabigatran etexilate tetrahydrate, C 34 H 49 N 7 O 9 , has been crystallised at ambient conditions. The colourless crystal was investigated using X-ray crystallography with single crystals and powder techniques, and was characterised by thermogravimetric-differential thermal analysis (TG-DTA) and infrared spectroscopy (IR). The compound was shown to be a tetrahydrate. A dabigatran etexilate molecule and four water molecules form a large ring structure, and intra-molecular hydrogen bonds contribute to the formation of a stable molecule in the unit cell.

A one-pot palladium-catalyzed synthesis of fluoronones via decarboxylative cyclization is reported. This protocol offers good yields and tolerates a broad range of functional groups. Based on the extensive experimental data, we propose a plausible decarboxylative insertion mechanism.

A new 4,5-diaryl-1H-imidazole was synthesized and characterized by H-1 NMR, ESI-MS, elemental analysis and FT-IR. The crystal structure of the title compound (C19H16Cl2N2O2, M-r = 375.24) has been determined by single-crystal X-ray diffraction. Crystal parameters: monoclinic system, space group P2(1)/n, a = 14.349(3), b = 8.7918(18), c = 15.352(3) angstrom, beta= 108.56(3)degrees, V = 1836.1(6) angstrom(3), Z = 4, F(000) = 776, D-c = 1.357 g/cm(3), mu = 0.368 mm(-1), the final R = 0.0502 and wR = 0.1066 for 2324 observed reflections with I > 2 sigma(I). A total of 16117 reflections were collected, of which 3615 were independent (R-int = 0.0595). The preliminary bioassay suggested that the title compound exhibits distinct effective inhibition on the proliferation of cancer cell lines.

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本文按照"卓越计划",在高校有机化学实验教学中,从精心选择实验内容,改变教学方式,丰富教学手段等方面,探讨了应如何充分培养学生的工程素质,使其成为合格的工程技术人才。

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