반응 #85841

ord-be7039892c9b4440990e7bc0b5df7e29

반응 방정식

CC1(C)OB(c2ccc(N3CCNCC3)cc2)OC1(C)C.Cl
1-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)piperazine hydrochloride
O=C([O-])[O-].[K+].[K+]
potassium carbonate
OCCBr
2-bromoethanol
CC1(C)OB(c2ccc(N3CCN(CCO)CC3)cc2)OC1(C)C
2-(4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)piperazin-1-yl)ethanol

반응 조건

온도
60°CELSIUS
상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    여과Then the mixture was filtered over celite
  2. 2
    세척washed with DCM
  3. 3
    농축concentrated
  4. 4
    기타to give product as a light brown solid

실험 절차

To a solution of 1-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)piperazine hydrochloride (500 mg, 1.54 mmol) and potassium carbonate (430 mg, 3.1 mmol) in acetonitrile (20 mL) was added 2-bromoethanol (388 mg, 3.1 mmol), then the mixture was heated at 60° C. overnight under an atmosphere of nitrogen. Then the mixture was filtered over celite and washed with DCM, concentrated to give product as a light brown solid. MS (m/z): 333 (M+H)+.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US09434726B2uspto-grants-2016_09