The application of stop-flow microwave technology to scaling-out SNAr reactions using a soluble organic base.
A model S(N)Ar reaction which gives a range of substituted diaryl ethers has been re-developed to function with the soluble organic base DBU in the place of insoluble potassium carbonate. Manufacture of these diaryl ethers has then been achieved by scaling-out in an automated stop-flow microwave reactor to give productivities of >0.5 kg per day. Analogous reaction partners have also been scaled up in this reactor to extend the scope of the study. Brief comparison in a scale-up batch microwave reactor is also made. Lastly, continuous 24 h processing is reported in this small microwave stop-flow reactor, which requires no manual intervention once started.
Marafie
Jameel A
JA
AstraZeneca, PR&D, Avlon Works, Severn Road, Hallen, Bristol, United Kingdom BS10 7ZE.
Moseley
Jonathan D
JD
D002254:Carbonates / Q000737:chemistry; D004987:Ethers / Q000138:chemical synthesis* / Q000737:chemistry; D008872:Microwaves; D015394:Molecular Structure; D011188:Potassium / Q000737:chemistry; D012995:Solubility
D002254:Carbonates; D004987:Ethers; C037593:potassium carbonate; D011188:Potassium