N-(2,2,2-trifluoroethyl)morpholine-4-carbothioamide

Conditions: temp:0.00; pressure:0.00; stir:

Conditions: temp:0.00; pressure:0.00; stir:

Conditions: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: Proceeding as described in Example 5 above, but substituting (morpholin-4-yl-carbothioyl)carbamic acid ethyl ester with morpholine-4-carbothioic acid (2,2,2-trifluoroethyl)amide and 2-amino-4-methylpentanoic acid [1-(benzoxazol-2-ylhydroxymethyl)propyl]amide hydrochloride with 2-amino-3-cyclohexylpropionic acid [1-(benzoxazol-2-ylhydroxymethyl)propyl]amide hydrochloride (prepared by reacting L-cyclohexyalanine with 2RS-amino-1-benzoxazol-2-yl-1-butanol as described in Example 1, step 2 above) provided N-[1-(benzoxazol-2-yl-hydroxy-methyl)-propyl]-3-cyclohexyl-2-{[N-(2,2,2-trifluoroethyl)-morpholine-4-carboximidoyl]-amino}-propionamide, Mol. Wt.: 553.62. MS: 552.5 (M−1), 554.7 (M+1).

Conditions: temp:0.00; pressure:0.00; stir:; See reaction.notes.procedure_details.

Procedure: Proceeding as described in Example 5 above, but substituting (morpholin-4-yl-carbothioyl)carbamic acid ethyl ester with morpholine-4-carbothioic acid (2,2,2-trifluoroethyl)amide and 2-amino-4-methylpentanoic acid [1-(benzoxazol-2-ylhydroxymethyl)propyl]amide hydrochloride with 2-amino-3-cyclohexylpropionic acid [1-(benzoxazol-2-ylhydroxymethyl)propyl]amide hydrochloride (prepared by reacting L-cyclohexyalanine with 2RS-amino-1-benzoxazol-2-yl-1-butanol as described in Example 1, step 2 above) provided N-[1-(benzoxazol-2-yl-hydroxy-methyl)-propyl]-3-cyclohexyl-2-{[N-(2,2,2-trifluoroethyl)-morpholine-4-carboximidoyl]-amino}-propionamide, Mol. Wt.: 553.62. MS: 552.5 (M−1), 554.7 (M+1).