反应 #1178453

ord-ee2df718879c496b86a46e4e026ea7f7

反应方程式

CN1CCOCC1
4-methylmorpholine
CCN=C=NCCCN(C)C.Cl
N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride
O=C(Nc1ccc(Cl)cc1)[C@H]1CCC[NH2+]1.[Cl-]
(R)-2-(4-chlorophenyl-carbamoyl)pyrrolidinium chloride
O=C(O)Cc1ccc(N2CCOCC2=O)cc1
4-(3-oxomorpholin-4-yl)phenylacetic acid
O=C(Nc1ccc(Cl)cc1)[C@H]1CCCN1C(=O)Cc1ccc(N2CCOCC2=O)cc1
N-(4-chlorophenyl)-(R)-1-{2-[4-(3-oxomorpholin-4-yl)phenyl]acetyl}pyrrolidine-2-carboxamide

溶剂

反应条件

详细条件
See reaction.notes.procedure_details.

后处理

  1. 1
    其他the precipitate formed
  2. 2
    过滤is filtered off

实验过程

0.26 ml (2.4 mmol) of 4-methylmorpholine and 230 mg (1.2 mmol) of N-(3-dimethylaminopropyl)-N′-ethylcarbodiimide hydrochloride (DAPECI) are added to a solution of 261 mg (1.00 mmol) of (R)-2-(4-chlorophenyl-carbamoyl)pyrrolidinium chloride and 235 mg (1.00 mmol) of 4-(3-oxomorpholin-4-yl)phenylacetic acid in 2 ml of DMF, and the mixture is stirred at room temperature for 18 hours. The reaction mixture is introduced into water, and the precipitate formed is filtered off, giving N-(4-chlorophenyl)-(R)-1-{2-[4-(3-oxomorpholin-4-yl)phenyl]acetyl}pyrrolidine-2-carboxamide as a slightly brownish solid; ESI 442.

来源

DOI: 10.6084/m9.figshare.5104873.v1专利: US08129373B2uspto-grants-2012_03