Hydrochloric Acid → 3-[2-(4-Bromo-phenyl)-2-oxo-ethylcarbamoyl]-pyrrolidine-1-carboxylic acid tert-butyl ester

참여 물질

역할	이름	HCID	투입량
반응물	Hydrochloric Acid	HCID 313	—
반응물	2-Amino-1-(4-bromophenyl)ethanone	HCID 21639	—
반응물	Diisopropylethylamine	HCID 81531	—
반응물	1-((Tert-butoxy)carbonyl)pyrrolidine-3-carboxylic acid	HCID 2760529	—
반응물	Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1)	HCID 9886157	—
용매	Dimethylformamide	HCID 6228	—
생성물	3-[2-(4-Bromo-phenyl)-2-oxo-ethylcarbamoyl]-pyrrolidine-1-carboxylic acid tert-butyl ester	HCID 59611512	—

반응 단계

N,N-diisopropylethylamine (5.3 mL, 30.6 mmol) was added dropwise to a mixture of pyrrolidine-1,3-dicarboxylic acid 1-tert-butyl ester (2.2 g, 10.1 mmol), HATU (4.0 g, 10.5 mmol), the HCl salt of 2-amino-1-(4-bromophenyl)ethanone (2.4 g, 9.6 mmol), and DMF (40 mL), and stirred at ambient condition for 1 hour. Most of the volatile component was removed in vacuo, and the resulting residue was dissolved in ethyl acetate (150 mL), washed with water and brine, dried over Na2SO4, filtered and concentrated in vacuo. The obtained residue was purified by flash chromatography to provide the desired product as a white foam-like solid (3.5 g, 90%). m/z 432.9, 434.9 (M+Na)+.

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US08822430B2
출처 데이터셋	uspto-grants-2014_09
ORD ID	ord-7bfed5c16a1946e6bda0d13963b1db3f
출처 메모	uspto-grants-2014_09