Trifluoroacetic acid → {2-[9-(1H-pyrazol-1-yl)-6-oxaspiro[4.5]decan-9-yl]ethyl}(thiophen-2-ylmethyl)amine
反応式
[N:1]1([C:6]2([CH2:16][CH:17]=O)[CH2:15][C:10]3([CH2:14][CH2:13][CH2:12][CH2:11]3)[O:9][CH2:8][CH2:7]2)[CH:5]=[CH:4][CH:3]=[N:2]1.[S:19]1[CH:23]=[CH:22][CH:21]=[C:20]1[CH2:24][NH2:25].[BH-](OC(C)=O)(OC(C)=O)OC(C)=O.[Na+].C(O)(C(F)(F)F)=O>>[N:1]1([C:6]2([CH2:16][CH2:17][NH:25][CH2:24][C:20]3[S:19][CH:23]=[CH:22][CH:21]=3)[CH2:15][C:10]3([CH2:14][CH2:13][CH2:12][CH2:11]3)[O:9][CH2:8][CH2:7]2)[CH:5]=[CH:4][CH:3]=[N:2]1参加物
5
実験手順
To a mixture of 2-[9-(1H-pyrazol-1-yl)-6-oxaspiro[4.5]decan-9-yl]acetaldehyde (15 mg, 0.06 mmol) and thiophen-2-ylmethanamine (19 uL, 0.18 mmol) was stirred at rt for 1 h before NaBH(OAc)3 (25.4 mg, 0.12 mmol) was added. The solution stirred overnight. After removal of solvent, the residue was purified by HPLC to provide {2-[9-(1H-pyrazol-1-yl)-6-oxaspiro[4.5]decan-9-yl]ethyl}(thiophen-2-ylmethyl)amine (17 mg, 61% yield) as a TFA salt. LCMS m/z 346 (M+1) observed.