(S)-2-Hydroxybutyric acid → Pemafibrate

Participants

Reaction Steps

In the same manner as in Examples 1 and 2, a phenyl etherification reaction (step-1) and hydrolysis (step-2) were performed under the conditions indicated in the following Table 1. Also, phenethyl (S)-2-trifluoromethanesulfonyloxybutyrate (Example 11) and phenethyl (S)-2-para-toluenesulfonyloxybutyrate (Comparative Example 7) were produced using (S)-2-hydroxybutyric acid, n-butyl (S)-2-methanesulfonyloxybutrate (Comparative Examples 1 to 3) and n-butyl (S)-2-para-toluenesulfonyloxybutyrate (Comparative Examples 4 to 6) were produced using n-butyl (S)-2-hydroxybutrate, and methyl (S)-2-chlorobutyrate (Comparative Example 8) was produced using (S)-2-chlorobutyric acid, according to standard methods. The yields and optical purities are presented together in Table 1.

Provenance & Evidence