反応 #2286365

ord-f2b0faecd68b41378f4c152faed9aff0

反応方程式

CCOc1ccccc1C(=O)C#Cc1csc(C2CCN(C(=O)Cn3nc(C(F)(F)F)cc3C)CC2)n1
1-(2-Ethoxyphenyl)-3-[2-(1-{[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]acetyl}piperidin-4-yl)-1,3-thiazol-4-yl]prop-2-yn-1-one
CCOc1ccccc1C(=O)CCc1csc(C2CCN(C(=O)Cn3nc(C(F)(F)F)cc3C)CC2)n1
1-(2-Ethoxyphenyl)-3-[2-(1-{[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]acetyl}piperidin-4-yl)-1,3-thiazol-4-yl]propan-1-one

溶媒

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    ろ過This gave, after filtration and removal of the solvent under reduced pressure, 1-(2-ethoxyphenyl)-3-[2-(1-{[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]acetyl}piperidin-4-yl)-1,3-thiazol-4-yl]propan-1-one (40 mg)

実験手順

1-(2-Ethoxyphenyl)-3-[2-(1-{[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]acetyl}piperidin-4-yl)-1,3-thiazol-4-yl]prop-2-yn-1-one (130 mg) was dissolved in methanol and hydrogenated at 40° C. and an H2 pressure of 10 bar and in the presence of Pd/C (10%). This gave, after filtration and removal of the solvent under reduced pressure, 1-(2-ethoxyphenyl)-3-[2-(1-{[5-methyl-3-(trifluoromethyl)-1H-pyrazol-1-yl]acetyl}piperidin-4-yl)-1,3-thiazol-4-yl]propan-1-one (40 mg).

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US09357779B2uspto-grants-2016_06