The compound was first prepared by Leonidas Zervas in the early 1930s who used it for the introduction of the benzyloxycarbonyl protecting group, which became the basis of the Bergmann-Zervas carboxybenzyl method of peptide synthesis he developed with Max Bergmann.

[3] The use of phosgene gas in the lab preparation carries a very large health hazard, and has been implicated in the chronic pulmonary disease of pioneers in the usage of the compound such as Zervas.

[4] Benzyl chloroformate is commonly used in organic synthesis for the introduction of the benzyloxycarbonyl (formerly called carboxybenzyl) protecting group for amines.

The protecting group is abbreviated Cbz or Z (in honor of discoverer Zervas), hence the alternative shorthand designation for benzyl chloroformate as Cbz-Cl or Z-Cl.

This "reactivity masking" property, along with the ability to prevent racemization of Z-protected amines, made the Z group the basis of the Begmann-Zervas synthesis of oligopeptides (1932) where the following general reaction is performed to protect the N-terminus of a serially growing oligopeptide chain:[1][2] This reaction was hailed as a "revolution" and essentially started the distinct field of synthetic peptide chemistry.