1416134-60-5Relevant articles and documents
Method of preparing 5R-[(benzyloxy) amino] piperidine-2S-carboxylic acid or a derivative thereof
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, (2021/10/13)
The present application relates to methods of preparing 5R-[(benzyloxy) amino] piperidine-2S-carboxylic acid or its derivatives in an environment-friendly way. The method uses L-glutamic acid as a starting material, which is first subjected to esterification reaction in the presence of an acidic reagent, and then reacted successively with 2-haloacetate and N-protecting agent, or with N-protecting agent and 2-haloacetate under a basic condition to obtain compound IV; then, the obtained compound IV is subjected to intramolecular condensation into a ring under the action of a strong base to obtain N-protecting group piperidine-5-one-2S-carboxylate (V).
Convenient preparing methods for 5R-benzyloxyaminopiperidine-2S-formate and oxalate thereof
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, (2018/04/01)
The invention relates to convenient preparing methods for 5R-benzyloxyaminopiperidine-2S-formate and oxalate thereof. L-glutamic acid is adopted as an initial raw material and esterified under the existence of an acidic agent to prepare a compound III; the compound III and 2-halogen-acetate are reacted under an alkaline condition to obtain a compound IV; the compound IV is subjected to intramolecular condensation and cyclization under functions of a strong alkali to obtain piperidin-5-one-2S-formate; the piperidin-5-one-2S-formate and benzylhydroxylamine hydrochloride are subjected to a condensation reaction under the existence of an alkali to obtain 5-benzyloxy imino piperidine-2S-formate; the 5-benzyloxy imino piperidine-2S-formate is subjected to reduction and chiral resolution to obtain the 5R-benzyloxyaminopiperidine-2S-formate oxalate; and the 5R-benzyloxyaminopiperidine-2S-formate oxalate is neutralized to obtain the 5R-benzyloxyaminopiperidine-2S-formate. The invention also provides a method for preparing avibactam. Raw materials of the methods are easily available, the methods are simple to operate, a production process is environmentally friendly, yields are high, and a production cost of the avibactam can be reduced.