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With N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In N,N-dimethyl-formamide at 20℃;
12 tert-butyl N-[(2R)-3-(2,4-dichlorophenyl)-l-oxo-l-[3-(lH-pyrazol-l-yl)azetidin-l- yl]propan-2-yl] carbamate
A solution of l-(azetidin-3-yl)-lH-pyrazole hydrochloride (1 eq.), (R)-2-((tert- Butoxycarbonyl)amino)-3-(2,4-dichlorophenyl)propanoic acid (1 eq.), HATU (1.3 eq.), and DIPEA (3 eq.) in DMF (5 mL) was stirred overnight at room temperature. Then the mixture was diluted with ethyl acetate, washed twice with water and once with brine, dried over Na2SC>4, filtered, concentrated in vacuo and purified by HPLC to afford tert-butyl N-[(2R)-3- (2,4-dichlorophenyl)-l-oxo-l-[3-(lH-pyrazol-l-yl)azetidin-l-yl]propan-2-yl]carbamate (0.35 g, 50% yield).
50%
With N-ethyl-N,N-diisopropylamine; N-[(dimethylamino)-3-oxo-1H-1,2,3-triazolo[4,5-b]pyridin-1-yl-methylene]-N-methylmethanaminium hexafluorophosphate In N,N-dimethyl-formamide at 20℃;
12 tert-butyl N-[(2R)-3-(2,4-dichlorophenyl)-l-oxo-l-[3-(lH-pyrazol-l-yl)azetidin-l- yl]propan-2-yl] carbamate
A solution of l-(azetidin-3-yl)-lH-pyrazole hydrochloride (1 eq.), (R)-2-((tert- Butoxycarbonyl)amino)-3-(2,4-dichlorophenyl)propanoic acid (1 eq.), HATU (1.3 eq.), and DIPEA (3 eq.) in DMF (5 mL) was stirred overnight at room temperature. Then the mixture was diluted with ethyl acetate, washed twice with water and once with brine, dried over Na2SC>4, filtered, concentrated in vacuo and purified by HPLC to afford tert-butyl N-[(2R)-3- (2,4-dichlorophenyl)-l-oxo-l-[3-(lH-pyrazol-l-yl)azetidin-l-yl]propan-2-yl]carbamate (0.35 g, 50% yield).
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