A kind of synthetic method of 2h-aziridine derivative

Abstract

The invention discloses a new method for synthesizing 2H-aziridine derivatives. In the Schlenk sealed tube reactor, add the alkyne compound shown in formula I successively, the sulfonic acid sodium salt shown in formula II, add tert-butyl nitrite (t-BuONO) and organic solvent again, under inert atmosphere protection condition Next, the oil bath was heated and stirred to react, and after the completion of the reaction was monitored by TLC or GC-MS, the 2H-aziridine derivative shown in formula III was obtained through post-processing. The method has the advantages of easy source of raw materials, simple process route, mild reaction conditions, low process cost, wide substrate adaptability and high yield.

Description

technical field [0001] The invention belongs to the technical field of organic synthesis, and in particular relates to a method for synthesizing 2H-azyridine derivatives. Background technique [0002] 2H-Aziridine is the smallest unsaturated azathree-membered ring structure existing in nature, and they widely exist in natural products, medicines, agricultural chemicals and organic materials, for example, the prior art has reported that ampicillin Azirinomycin and other compounds with the structures shown in the following formulas I-VI. [0003] [0004] Due to the widespread occurrence of 2H-aziridine derivatives in nature and their great potential in the construction of amino derivatives and nitrogen-containing heterocycles, chemists have conducted intensive research on this class of molecules. 2H-Aziridine derivatives have been widely used in the synthesis of complex nitrogen-containing acyclic molecules and various nitrogen heterocyclic compounds, such as pyrroles, in...

AI Technical Summary

Problems solved by technology

Such a synthetic strategy has the disadvantages of multi-step reaction steps, complicated operation, harsh conditions, high cost, and limited adaptability of reaction substrates.

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