The 14 selected MAGL inhibitor molecules were synthesized via a four-step procedure. The key step involved the alkylation of the benzoxazole building block (9) under Minisci-type conditions, which were pre-screened in silico and validated through HTE, yielding intermediates 9a -9i. These intermediates were subsequently coupled with four different head groups (13 -16) using classic amide coupling techniques. For this study, compound 17, consisting of non-alkylated 9 and head group 13, was synthesized freshly. All reactions were conducted under ambient conditions in glass reaction vessels equipped with pressure release caps and stirring bars. Purification was achieved via flash chromatography or reversedphase high-performance liquid chromatography (RP-HPLC). Structural elucidation was performed using nuclear magnetic resonance (NMR) spectroscopy and high-resolution mass spectrometry (HRMS). The complete experimental procedures, analytical results, and spectra for all compounds are provided in the SI (SI5 and SI6).