تفاعل #2045114

ord-8e2de5afb87642b8bc5effe46660d0c9

معادلة التفاعل

Cn1cc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1C(=O)O
1-methyl-4[({[4-(trifluoromethoxy)phenyl]amino}carbonyl)amino]-1H-pyrrole-2-carboxylic acid
Cn1cc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1C(=O)O
1-Methyl-4-[({[4-(trifluoromethoxy)phenyl)amino}carbonyl)amino]-1H-pyrrole-2-carboxylic acid
CN(C)C(On1nnc2ccccc21)=[N+](C)C.F[B-](F)(F)F
O-(benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium tetrafluoroborate
c1ccc(N2CCNCC2)nc1
1-(2-pyridyl)piperazine
Cn1cc(NC(=O)Nc2ccc(OC(F)(F)F)cc2)cc1C(=O)N1CCN(c2ccccn2)CC1
N-{1-Methyl-5-[(4-pyridin-2-ylpiperazin-1-yl)carbonyl]-1H-pyrrol-3-yl}-N′-[4-(trifluoromethoxy)-phenyl]urea

المذيبات

ظروف التفاعل

الظروف التفصيلية
See reaction.notes.procedure_details.

المعالجة

  1. 1
    أخرىThe reaction solution is purified by RP-HPLC (acetonitrile/water)
  2. 2
    أخرىThis gives a solid

الإجراء التجريبي

50 mg (0.15 mmol) of 1-methyl-4[({[4-(trifluoromethoxy)phenyl]amino}carbonyl)amino]-1H-pyrrole-2-carboxylic acid (Example 5A) are initially charged in 1 ml of DMF, and 56 mg (0.18 mmol) of O-(benzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium tetrafluoroborate (TBTU) and 8.9 mg (0.07 mmol) of 4-(dimethylamino)pyridine (DMAP) are added. 29 mg (0.18 mmol) of 1-(2-pyridyl)piperazine are then added, and the mixture is stirred at RT for 8 h. The reaction solution is purified by RP-HPLC (acetonitrile/water). This gives a solid.

المصدر

DOI: 10.6084/m9.figshare.5104873.v1براءة الاختراع: US08410090B2uspto-grants-2013_04