Regioselective and enantiospecific synthesis of the HSP co-inducer arimoclomol from chiral glycidyl derivativesElectronic supplementary information (ESI) available: Experimental procedures and data for all new compounds including traces of chiral SFC. See DOI: 10.1039/c7ob02578e

A new efficient chiral synthesis of enantiopure arimoclomol ( 2 ) is reported from ( R )-(−)-glycidyl nosylate ( 11 ) with complete retention of chiral integrity. Off-target pharmacology of arimoclomol ( 2 ) was evaluated against a representative set of drug targets and showed modest binding to a few kinases. Pharmacokinetic data was generated in vivo in mouse and showed a low brain : plasma ratio. These studies will be helpful towards a better understanding of the PK-PD relationship of 2 in disease models. A new efficient chiral synthesis of arimoclomol is reported from ( R )-(−)-glycidyl nosylate with complete retention of chiral integrity.