An efficient preparation of beta-aryl-beta-ketophosphonates by the TFAA/H3PO4-mediated acylation of arenes with phosphonoacetic acids.
Beta-aryl-beta-ketophosphonates can be efficiently prepared in good yield by using a TFAA/85% H 3PO 4-mediated acylation of electron-rich arenes with phosphonoacetic acids. The conditions offer advantages over existing methods of preparing these useful compounds by not requiring the use of strong base, cryogenics, or an anhydrous and inert atmosphere. Furthermore, some functional groups not tolerated with the reaction conditions used in existing methods are compatible with the herein described conditions.
Luke
George P
GP
Process Chemistry, Neurogen Corporation, Branford, Connecticut 06405, USA. gluke@nrgn.com
Seekamp
Christopher K
CK
Wang
Zhe-Qing
ZQ
Chenard
Bertrand L
BL