Реакция #1726727

ord-2c81092a3a8647728fc777a5db2d32c1

Уравнение реакции

O=C=Nc1cccc(C(F)(F)F)c1
3-(trifluoromethyl)phenyl isocyanate
CC(C)(C)OC(=O)N1CCC(NCCC(c2ccccc2)c2ccccc2)CC1
tert-butyl 4-[(3,3-diphenylpropyl)amino]-1-piperidine carboxylate
CC(C)(C)OC(=O)N1CCC(N(CCC(c2ccccc2)c2ccccc2)C(=O)Nc2cccc(C(F)(F)F)c2)CC1
white foam
Выход 87.4%
CC(C)(C)OC(=O)N1CCC(N(CCC(c2ccccc2)c2ccccc2)C(=O)Nc2cccc(C(F)(F)F)c2)CC1
tert-butyl-4-((3,3-diphenylpropyl){[3-(trifluoromethyl)anilino]carbonyl}amino)-1-piperidine carboxylate
Выход 87.4%

Растворители

Условия реакции

Подробные условия
See reaction.notes.procedure_details.

Обработка

  1. 1
    workup.WAITthe reaction medium is again placed on an orbital shaker for 45 minutes
  2. 2
    ФильтрацияThe resin is filtered
  3. 3
    Промывкаwashed with dichloromethane
  4. 4
    КонцентрированиеThe filtrate is concentrated in vacuo in order

Методика

246 mg (1.32 mmol) of 3-(trifluoromethyl)phenyl isocyanate is added to a solution of tert-butyl 4-[(3,3-diphenylpropyl)amino]-1-piperidine carboxylate (470 mg, 1.2 mmol) in 5 ml of dichloromethane. The solution is agitated for 45 minutes, and the aminomethyl resin (180 mg, 0.36 mmol) is added and the reaction medium is again placed on an orbital shaker for 45 minutes. The resin is filtered and washed with dichloromethane. The filtrate is concentrated in vacuo in order to produce 610 mg (yield=87%) of a white foam.

Источник

DOI: 10.6084/m9.figshare.5104873.v1Патент: US08110574B2uspto-grants-2012_02