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A technology of docetaxel and compounds, which is applied in the field of preparation of anti-cancer raw material drug docetaxel, can solve the problems of high cost, difficult reduction of product price, and low yield of docetaxel technology
Active Publication Date: 2012-03-21
JIANGSU HAICI BIOLOGICAL PHARMA CO LTD OF YANGTZE RIVER PHARMA GRP +1
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The technical yield of the existing semi-synthetic method for preparing docetaxel is...
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Embodiment 1
[0036] Dissolve 2.0 g of 10-DABIII in 20 mL of pyridine, add 1.56 mL of trichloroethyl chloroformate, react at zero temperature for 1 hour after the addition, and the reaction is complete. The reaction was quenched with ice-water mixture and extracted with dichloromethane. Dry over anhydrous sodium sulfate and concentrate. Compound 1 was obtained.
[0037] Dissolve 3 grams of side chains in 15 mL of dichloromethane, add dropwise 2.4 mL of 1,1-dimethoxycyclohexane, add 0.3 mL of boron trifluoride ether, and react at room temperature. After the reaction was complete, the solvent was drained, added with saturated sodium bicarbonate solution, extracted with ethyl acetate, washed with saturated brine, dried over anhydrous sodium sulfate, concentrated and then column chromatographed. 1.0 g of the obtained compound was dissolved in 10 mL of tetrahydrofuran, and 5.3 mL of 1.0 N lithium hydroxide solution was slowly added dropwise. After the addition was complete, the reaction was co...
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Abstract
The invention provides a preparation method of docetaxel. The method comprises the following steps: 1) dissolving 10-deacetylbaccatin III in an solvent, and reacting with a protective agent to selectively protect the 7-hydroxyl group and 10-hydroxyl group in the 10-deacetylbaccatin III; 2) preparing a side chain intermediate; 3) performing an esterification reaction on the products obtained in the step 1) and the step 2); 4) removing the protective groups on the side chain of the esterification product under the acidic condition; 5) protecting amino on the side chain with the protective group under the alkaline condition; and 6) removing the protective groups on the hydroxyl groups to produce docetaxel. The invention provides the new preparation method of docetaxel, wherein the new related side chains are synthesized to prepare docetaxel; and the method has significances to utilize various taxanes which are extracted and separated from natural products and have similar structures with the target compound, optimize the technological process, increase the yield, reduce the cost, reduce the product price, comprehensively utilize resources and the like.
Description
technical field [0001] The invention relates to a preparation method of an anticancer crude drug docetaxel, which belongs to the technical field of drug synthesis. Background technique [0002] Docetaxel chemical name: [2aR-(2aα, 4β, 4aβ, 6β, 9α, (aR * , βS * ), 11α, 12α, 12aα, 12bα)]-β-[[(1,1-dimethylethoxy)carbonyl]amino]-α-hydroxyphenylpropanoic acid [12b-acetoxy-12-benzoyl Oxy-2a, 3, 4, 4a, 5, 6, 9, 10, 11, 12, 12a, 12b-dodecahydro-4, 6, 11-trihydroxy-4a, 8, 13, 13-tetramethyl -5-Oxo-7,11-methylene-1H-cyclodecapenta-[3,4]benzo[1,2-b]oxetan-9-yl]ester. Molecular weight 807.89, CAS No.: 114977-28-5, molecular formula: C 43 h 53 N 14 , the structural formula is: [0003] [0004] Docetaxel is a new anti-tumor drug obtained after artificial structure modification on the basis of the structure of the natural anti-tumor drug paclitaxel. Docetaxel is a paclitaxel anti-tumor drug, which plays an anti-tumor effect by interfering with the microtubule network necessary f...
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IPC IPC(8): C07D305/14
CPCY02P20/55
Inventor 胡玉玺路显峰冯建鹏张薇樊苗苗陆良喆程瑞玲
Owner JIANGSU HAICI BIOLOGICAL PHARMA CO LTD OF YANGTZE RIVER PHARMA GRP
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