187795-95-5Relevant articles and documents
Oxazole (oxathiazole) oxide synthesis method
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Paragraph 0016; 0024; 0028-0029; 0030; 0034-0035; 0036-0041, (2019/10/04)
The invention provides an oxazole (oxathiazole) oxide synthesis method, which comprises: S1, adding dichloromethane to a reactor, adding 2-aminopyridine to the reactor to dissolve the 2-aminopyridine in the dichloromethane, adding triethylamine, slowly adding dimethyl sulfate in a dropwise manner at a room temperature, cooling to a temperature of 0 DEG C after the adding, and carrying out a reaction; S2, adding triethylamine to the reactor, adding propylene oxide in a dropwise manner at a room temperature, and carrying out a reaction for 12-15 h at a room temperature; S3, heating to a temperature of 45-55 DEG C, and carrying out a cyclization reaction; and S4, after completing the reaction, carrying out rotary removing on the solvent, and re-crystallizing the crude product to obtain the target product. According to the present invention, the starting raw material is cheap, the route can adopt the one-pot method, the intermediate product does not need to be separated, the safety is high, the magnification production can be performed, and the purity of the final product can reach 99%.
Processes and intermediates for the preparation of piperazine derivatives
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, (2008/06/13)
Compounds having the formulaR5O-A-NR4-R2(V)where R2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R4 and R5 are both hydrogen atoms or together represent -SO- or -SO2- and A is C2-C4 alkylene