Access to Unprotected β‑Fluoroalkyl β‑Amino Acids and Their α‑Hydroxy Derivatives

Published on 2019-03-15T11:19:02Z (GMT) by
Unprotected β-(het)­aryl-β-fluoroalkyl β-amino acids and their α-hydroxy derivatives can be readily obtained using a decarboxylative Mannich-type reaction without protection/deprotection steps. This protocol utilizes lithium hexamethyldisilazide and (het)­arylfluoroalkyl ketones to generate NH-ketimine intermediates. The mild reaction conditions allow the preparation of original fluorinated β-amino acids as useful building blocks in a practical and scalable manner.

Cite this collection

Sukach, Volodymyr; Melnykov, Serhii; Bertho, Sylvain; Diachenko, Iryna; Retailleau, Pascal; Vovk, Mykhailo; et al. (2019): Access to Unprotected β‑Fluoroalkyl β‑Amino Acids and Their α‑Hydroxy Derivatives. ACS Publications. Collection.