4-Methylmorpholine → (S)-2-[(S)-4-(3-Chloro-4-trifluoromethoxy-phenylcarbamoyl)-3-methyl-2-oxo-piperazin-1-yl]-5-((S)-4-hydroxy-6-aza-spiro[2.5]oct-6-yl)-5-oxo-pentanoic acid methyl ester

Participants

Reaction Steps

In analogy to the procedure described in Example 30, (S)-5-((S)-4-hydroxy-6-aza-spiro[2.5]oct-6-yl)-2-((S)-3-methyl-2-oxo-piperazin-1-yl)-5-oxo-pentanoic acid methyl ester (intermediate 29) with 3 eq. of 4-methylmorpholine and 1.2 eq. of 2-chloro-4-isocyanato-1-trifluoromethoxy-benzene (intermediate 17) gave the titled compound in 67% yield as white foam. MS: 605.20 (MH+, Cl).

Provenance & Evidence