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The important synthetic precursor(Ⅲ), 1-(prop-2-yn-1-yl)-7,8-dihydro-1Hbenzo[d][1,3]thiazine-2,5(4H,6H)-dione(C_(11)H_(11)NO_2S), was prepared through a three-component reaction, which was further transferred into cytotoxic triazoles by alkylation and “click” synthesis in satisfactory yields of 87%~95%. Their structures were characterized by IR, H-RESI-MS and NMR analysis. Meanwhile, the crystal of Ⅲ was obtained and determined by X-ray single-crystal diffraction. Crystal data: orthorhombic system, space group P2_12_12_1, a = 5.189(4), b = 8.661(6), c = 23.498(17) ?, V = 1056.2(13) ?~3, Z = 4, F(000) = 464, D_c = 1.392 g/cm~3, μ =0.284 mm~(-1), R = 0.0637 and wR = 0.1668 for 8182 independent reflections(R_(int) = 0.1580) and 2166 observed ones(I > 2σ(I)).
The significant synthetic precursor (III) was synthesized using the same method as described in Example 1 except that 1- (prop-2-yn-1-yl) -7,8-dihydro- 1Hbenzo [d] [1,3] thiazine- C 11 H 11 NO 2 S), was prepared through a three-component reaction, which was further transferred into cytotoxic triazoles by alkylation and “click” synthesis in a satisfactory result of 87% -95%. Crystal data: orthorhombic system, space group P2_12_12_1, a = 5.189 (4), b = 8.661 (6), c = 23.498 (17) ?, V = 1056.2 (13)? 3, Z = 4, F = 0004 = 464, Dc = 1.392 g / 1), R = 0.0637 and wR = 0.1668 for 8182 independent reflections (R_ (int) = 0.1580) and 2166 observed ones (I> 2σ (I)).