Synthesis
Step 1 (MZ-S1): trans-3-fluorocinnamic acid (20 g, 121.9 mmol) was hydrogenated in ethanol for 2 h under hydrogen atmosphere (7 psi) with 10% Pd/C (2 g) as catalyst. After completion of the reaction, the mixture was filtered through diatomaceous earth and washed with ethanol. The filtrate was concentrated under reduced pressure to give 19.5 g (97% yield) of MZ-S1 as an off-white solid, which could be used in subsequent steps without further purification.
References
[1] Patent: WO2014/140279, 2014, A1. Location in patent: Page/Page column 91; 177
[2] Patent: US2004/39014, 2004, A1
[3] Bioorganic and Medicinal Chemistry Letters, 2000, vol. 10, # 14, p. 1519 - 1522
[4] Patent: US5486541, 1996, A
[5] Patent: WO2008/85505, 2008, A1. Location in patent: Page/Page column 83-84