The invention discloses a synthetic method of an anesthetic analgesic drug. According to the synthetic method, 4-piperidinecarboxylic acid is used as a raw material and subjected to alkylation, bromination, methylation, acylation and the like to prepare the anesthetic analgesic drug. The method avoids the usage of highly toxic cyanide, so the safety and controllability of operation are improved; the method avoids an elimination reaction in reaction process, thereby accelerating reaction speed and shortening reaction time; and the method reduces reaction temperature, shortens the reaction time,and is more suitable for industrial production.
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(2019/12/29)
New method for synthesizing carfentanil
The invention belongs to the field of synthesis of organic matters and specifically relates to a method for synthesizing carfentanil. The synthesis method comprises the following steps of taking N-Bocprotective group piperidone as a raw material, and carrying out five steps of performing a Bargellini reaction, N-acylation, methylation, deprotection and N-alkylation to obtain a target product, namely the carfentanil. According to the invention, by adopting the new method for synthesizing the carfentanil, the use of a extremely-toxic substance, namely potassium cyanide, is avoided, so that theenvironment-friendly effect is achieved; the yield is high; a synthesis route is relatively simple; and the requirements of a modern high-efficiency and low-cost synthesis idea can be met.
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(2019/06/08)
Ugi reaction for the synthesis of 4-aminopiperidine-4-carboxylic acid derivatives. Application to the synthesis of carfentanil and remifentanil
A two-step sequence involving an Ugi four-component reaction was developed for the preparation of 4-aminopiperidine-4-carboxylic acid derivatives. This strategy has led to the successful preparation of two drugs carfentanil and remifentanil in shorter times and better yields than previously described methods.