Preparation method of sulfydryl alkenyl ester compound

A technology of ester compounds and mercaptoalkenes, which is applied in the field of preparation of synthetic mercaptoalkene esters, can solve problems such as enlarged production risks and difficult safety control, so as to improve overall safety and environmental protection, solve industrialization problems, The effect of novel technology
CN113135848AInactive Publication Date: 2021-07-20SHENZHEN HUAXIAN PHARMA TECH CO LTD
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Patent Information

Authority / Receiving Office
CN · China
Patent Type
Applications(China)
Current Assignee / Owner
SHENZHEN HUAXIAN PHARMA TECH CO LTD
Publication Date
2021-07-20
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention relates to a preparation method of a sulfydryl alkenyl ester compound, belongs to the field of organic chemical synthesis, and aims to solve the problems of high risk of large-scale production and the like, and the synthesis route provided by the invention comprises the following three steps: (1) carrying out a reaction on a starting material ethyl 2-oxo carboxylate compound and Tf2O (trifluoromethanesulfonic anhydride) under the action of alkali and a solvent A, so as to generate an enol intermediate 1 protected by trifluoromethanesulfonyl; (2) carrying out substitution reaction with a sulfo reagent to obtain an intermediate 2; and (3) performing deprotection on the intermediate 2 under the action of a deprotection reagent to obtain a target product 3. The method for preparing the sulfydryl alkenyl ester compound has the beneficial effects that the process is novel, toxic gases such as hydrogen sulfide are prevented from being used, the overall safety and environmental protection property of the process are improved, and the method is more suitable for large-scale production and solves the industrialization problem.
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Description

technical field

[0001] The invention belongs to the field of organic chemical synthesis, in particular to a preparation method for synthesizing mercaptoalkenyl esters. Background technique

[0002] Mercaptoenol esters are key intermediates used in the preparation of innovative drugs such as sepsis. At present, the main route for the synthesis of this type of substance is shown in the following formula. In the reaction process, it is necessary to prepare a relatively high concentration of hydrogen sulfide methanol solution, and then introduce hydrogen chloride into the reaction solution. Although the synthesis scheme is simple, hydrogen sulfide has toxicity and foul smell, and there is a big safety hazard when used in large quantities. In addition, hydrogen chloride gas is also strongly irritating.

[0003]

[0004] In summary, the above-mentioned various defects make the safety control of this route difficult, and the risk of enlarged production is high. Therefore, ther...

Claims

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