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A kind of preparation method of 5r-benzyloxyaminopiperidine-2s-carboxylic acid or its derivative
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A kind of technology of benzyloxyamino piperidine, base piperidine
Active Publication Date: 2021-02-26
XINFA PHARMA
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The two reaction processes require protection and deprotection, the operation is extremely cumbersome, the amount of solvent used is large, the discharge of "three wastes" is large, and the utilization rate of atoms is low, which is not conducive to environmental protection
Simultaneously the product yield that above-mentioned prior art method obtains is low, is unfavorable for green industrialized production
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[0126] Add 300 grams of methanol, 14.7 grams (0.10 moles) of L-glutamic acid, 30.0 grams (0.25 moles) ) thionylchloride, heated, reacted at 60-63°C for 7 hours, cooled to 20-25°C, replaced hydrogenchloride gas in the system with nitrogen, and after 30 minutes of replacement, recovered excess thionylchloride and methanol by distillation, and then added to the remaining Add 300 grams of fresh methanol to the mixture. Then add 41.5 grams (0.30 moles) of potassiumcarbonate, 11.0 grams (0.10 moles) of methyl 2-chloroacetate, and stir at 40 to 45 ° C for 4 hours, then add 13.0 grams (0.10 moles) of benzyl chloride and stir at 40 to 45 ° C React for 4 hours, after the reaction is complete, filter while hot, wash the filter cake twice with methanol, 50 grams each time, combine the filtrate, and recover the methanol by atmospheric distillation, then distill under reduced pre...
[0128] Add 300 grams of ethanol, 14.7 grams (0.10 moles) of L-glutamic acid, 25.0 grams (0.08 moles) ) solidphosgene, heated, reacted at 70-75° C. for 5 hours, cooled to 20-25° C., replaced hydrogen chloride gas in the system with nitrogen, and replaced it for 30 minutes. Excessive triphosgene and ethanol were recovered by distillation, and then 300 g of fresh ethanol was added to the residue. Then add 41.5 grams (0.30 moles) of potassiumcarbonate, 17.5 grams (0.10 moles) of benzyl bromide, and stir at 30 to 35 ° C for 4 hours, then add 18.5 grams (0.11 moles) of ethyl 2-bromoacetate, and stir at 40 to 45 ° C React for 4 hours, after the reaction is complete, filter while it is hot, wash the filter cake twice with ethanol, 50 grams each time, combine the filtrate, and recover the ethanol by atmospheric distillation, then distill under reduced pressure to obtain 36.0 gra...
[0130] Add 280 grams of benzyl alcohol, 14.7 grams (0.10 moles) of L-glutamic acid, 36.0 grams (0.30 mol) thionyl chloride, heated, reacted at 80-85° C. for 5 hours, cooled to 20-25° C., and replaced the hydrogen chloride gas in the system with nitrogen for 30 minutes. Recover excessive thionyl chloride and benzyl alcohol by distillation, and then add 280 grams of fresh benzyl alcohol to the residue. Then add 41.5 grams (0.30 moles) of potassiumcarbonate, 19.5 grams (0.11 moles) of benzyl 2-chloroacetate, stir and react at 50-55 °C for 4 hours, then add 17.5 grams (0.10 moles) of benzyl bromide, and stir at 40-45 °C React for 4 hours, after the reaction is complete, filter while it is hot, wash the filter cake twice with benzyl alcohol, 80 grams each time, combine the filtrate, and recover the benzyl alcohol by atmospheric distillation, then distill under reduced pre...
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technical field [0001] The invention relates to a green preparation method of 5R-benzyloxyaminopiperidine-2S-carboxylic acid or its derivatives. The compound is a key intermediate for the preparation of Avibactam and Relebactam, belonging to Pharmaceutical biochemical industry. Background technique [0002] Avibactam and Relebactam are non-β-lactam inhibitors of novel diazabicyclooctamone compounds. Avibactam can inhibit type A (including ESBL and KPC) and C When avibactam is used in combination with various cephalosporins and carbapenemantibiotics, it has broad-spectrum antibacterial activity, especially against E. Pneumoniae primary, Escherichia coli containing excess AmpC enzyme, and Escherichia coli containing both AmpC and extended-spectrum β-lactamase had significant activity. The phase II clinical trials of relibactam and imipenem-cilastatin sodium combination drugs have shown good performance. The CAS number of Avibactam (Ia) is 1192491-61-4, and the chemical nam...
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