Synthesis method of phosphorothioate compounds and application thereof to synthesis of various medicines

A technology of phosphorothioate and phosphorothioate, which is applied in the field of synthesis of phosphorothioate compounds, can solve the problems of poor functional group compatibility, large substrate limitations, and difficulty in putting into use, and achieve mild and simple reaction conditions, Effect of less waste discharge and lower cost
CN106905361AInactive Publication Date: 2017-06-30PEKING UNIV
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Patent Information

Authority / Receiving Office
CN · China
Current Assignee / Owner
PEKING UNIV
Publication Date
2017-06-30
Estimated Expiration
Not applicable · inactive patent

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Abstract

The invention discloses a synthesis method of phosphorothioate compounds with general formula (III), and aims to provide a novel synthesis method of phosphorothioate compounds with simple conditions and easy industrial production. The method is to mix the organophosphorus oxygen compound having the general formula (I) with the mercaptan or thiophenol compound having the general formula (II), and react under the action of a catalyst to prepare the compound of the general formula (III). Phosphorothioate compounds. By adopting the method of the invention, phosphorothioate compounds can be synthesized cheaply and efficiently, and will have wide application prospects in actual production.
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Description

technical field

[0001] The invention relates to a method for synthesizing phosphorothioate compounds, belonging to the field of organic synthesis chemistry. Background technique

[0002] Phosphorothioate compounds, especially alkyl phosphorothioate compounds, have significant biological activity and are widely present in the skeleton structures of drugs (treatment of glaucoma, cancer chemotherapy, etc.) and pesticides (insecticides). , which has important scientific significance and application value for the efficient synthesis of phosphorothioate compounds.

[0003] However, the existing synthetic methodologies are limited to the preparation of aryl phosphorothioate compounds, while the synthesis of alkyl phosphorothioate compounds is difficult and rarely reported. Existing strategies are mainly divided into three categories, one, Atherton-Todd type reaction, first halogenation and then coupling reaction [a) F.R.Atherton, A.R.Todd, J.Chem.Soc.1947,674; b) E.M.Georgiev, J ...

Claims

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