Hydrochloric Acid → HCID 178424980, compound

Participants

Reaction Conditions

Reaction Steps

To a solution of 1-[2-(3,5-dimethyl-phenyl)-acetyl]-2-methyl-azetidine-2-carboxylic acid (4-chloro-benzyl)-cyanomethyl-amide, Compound 68 (1 eq.) in toluene was added Bu3SnN3 (10 eq.). The reaction was refluxed for 6 h and cooled to 20° C. then HCl 2N in Et2O was added. After 15 h of stirring, the solid was filtered, dissolved in DCM and precipitated with iPr2O. The solid was purified by chromatography on silica gel (elution with DCM/MeOH: 1/0 to 95/5) to afford 1-[2-(3,5-dimethyl-phenyl)-acetyl]-2-methyl-azetidine-2-carboxylic acid (4-chloro-benzyl)-(1H-tetrazol-5-ylmethyl)-amide.

Provenance & Evidence