반응 #58481

ord-9b02042daf3a4b20971170c5f1a9a16c

반응 방정식

Cl
hydrochloric acid
O=C(N1CCCCC1)C1(Cl)C=CC=CN1
2-chloropyridinoyl-piperidine
N=C(c1ccccc1)c1ccccc1
benzophenone imine
c1ccc(P(c2ccccc2)c2ccc3ccccc3c2-c2c(P(c3ccccc3)c3ccccc3)ccc3ccccc23)cc1
2,2′-bis(diphenylphosphino)-1,1′-binaphthyl
CC(C)(C)[O-].[Na+]
sodium t-butoxide
NC1(C(=O)N2CCCCC2)C=CC=CN1
2-aminopyridinoyl-piperidine

반응 조건

상세 조건
See reaction.notes.procedure_details.

후처리

  1. 1
    기타purified

실험 절차

Next, the 2-chloropyridinoyl-piperidine intermediate is reacted with benzophenone imine in the presence of tris(dibenzylidineacetone)-dipalladium(0) Pd2(dba)3) as a catalyst, and 2,2′-bis(diphenylphosphino)-1,1′-binaphthyl (BINAP) and sodium t-butoxide in a suitable solvent, such as toluene, at reflux, to substitute the halo group with the benzophenone imino group. After work-up, this intermediate is typically reacted with hydrochloric acid in a suitable solvent, such as tetrahydrofuran, and then purified to give the corresponding 2-aminopyridinoyl-piperidine intermediate.

출처

DOI: 10.6084/m9.figshare.5104873.v1특허: US07423050B2uspto-grants-2008_09