2-Morpholinoethylamine → HCID 178472024, compound

HRID 2243052Notes

Reaction equation

C[N:2]([CH3:20])/[CH:3]=[C:4](/[C:10](=[O:19])[C:11]1[CH:16]=[C:15]([I:17])[CH:14]=[CH:13][C:12]=1[F:18])\[C:5]([O:7][CH2:8][CH3:9])=[O:6].NC[CH2:23][N:24]1[CH2:29][CH2:28][O:27][CH2:26][CH2:25]1>C(O)C.C(OCC)C>[F:18][C:12]1[CH:13]=[CH:14][C:15]([I:17])=[CH:16][C:11]=1[C:10]([C:4](=[CH:3][NH:2][CH2:20][CH2:23][N:24]1[CH2:29][CH2:28][O:27][CH2:26][CH2:25]1)[C:5]([O:7][CH2:8][CH3:9])=[O:6])=[O:19]

Participants

Conditions

Temperature: 0 °C

Procedure

A suspension of ethyl 3-(dimethylamino)-2-(2-fluoro-5-iodobenzoyl)acrylate (WO2006/010733, 294 mg, 0.75 mmol) in ethanol (2.500 mL) and diethyl ether (5 mL) was cooled 0° C. and 4-(2-aminoethyl)morpholine (103 mg, 0.79 mmol) was added dropwise. The reaction mixture was stirred for 3 h, then concentrated under reduced pressure to give the desired product (358 mg). MS (ESP): 477 (M+H+) for C18H22FIN2O4.

Workup

concentrationconcentrated under reduced pressure

Sources & evidence

ORD record: ord-b56b8fa601a249d98d6fa7ebb5a48de8
Source dataset: uspto-grants-2010_03
DOI: 10.6084/m9.figshare.5104873.v1
Patent number: US07674801B2

Reaction notes

Loading…