Preparation method of ethyl 2-[[(bezyloxy)carbonyl]amido]-4-thiazolyl acetate
A technology of thiazolyl acetate and benzyloxy, applied in the field of pharmaceutical intermediates, can solve problems such as increased difficulty, high cost, unrealistic industrialized production, etc., and achieves the effects of easy operation, few reaction procedures, and reduced production costs
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[0023] Example 1 Preparation of ethyl 2-[[(benzyloxy)carbonyl]amino]-4-thiazolylacetate
[0024] In a 500ml reaction flask, add 200g ethanol, 0.5g (4mmol) 4-dimethylaminopyridine, 8.3g (105mmol) pyridine and stir, cool to -5°C, add 17.9g (105mmol) benzyl chloroformate, continue React for 2h, then heat to 10°C, react for 8h, and filter. The filtrate was poured into 18.6g (100mmol) ethyl 2-amino-4-thiazolyl, and the reaction was stirred at this temperature for 18h to obtain 14.2g of 2-[[(benzyloxy)carbonyl]amino]-4-thiazolyl Ethyl acetate, the yield was 44.4% (calculated as ethyl 2-amino-4-thiazolyl).
Example Embodiment
[0025] Example 22 Preparation of methyl-[[(benzyloxy)carbonyl]amino]-4-thiazolyl acetate
[0026] In a 500ml reaction flask, add 86g methanol, 1.2g (10mmol) 4-dimethylaminopyridine, 10.1g (100mmol) triethylamine and stir, cool to -10°C, add 17.1g (100mmol) benzyl chloroformate , Continue to react for 2h, then heat to 15°C for 6h, and filter. The filtrate was poured into 17.2g (100mmol) methyl 2-amino-4-thiazolyl acetate, stirred at this temperature for 18h to obtain 10.7g of 2-[[(benzyloxy)carbonyl]amino]-4-thiazolyl Methyl acetate, the yield is 35.0% (based on 2-amino-4-thiazolyl methyl acetate).
Example Embodiment
[0027] Example 32 Preparation of ethyl-[[(benzyloxy)carbonyl]amino]-4-thiazolylacetate
[0028] In a 500ml reaction flask, add 280g isopropanol, 0.1g (1mmol) 4-dimethylaminopyridine, 15.9g (150mmol) Na 2 CO 3 Stir, lower the temperature to 0°C, add 25.6 (150mmol) benzyl chloroformate, continue the reaction for 1h, then increase the temperature to 15°C to react for 4h, and filter. The filtrate was poured into 18.6g (100mmol) ethyl 2-amino-4-thiazolyl, and the reaction was stirred at this temperature for 12h to obtain 10.4g of 2-[[(benzyloxy)carbonyl]amino]-4-thiazolyl Ethyl acetate, the yield was 32.7% (calculated as ethyl 2-amino-4-thiazolyl).
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