Reaktion #315208

ord-4aa4d4af08e44c96bf2f3f26487d98c8

Reaktionsgleichung

N#C[C@@H]1C[C@H](F)CN1C(=O)CNC12CCC(C(=O)O)(CC1)CC2
(2S,4S)-1-[[N-(4-carboxybicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile
C#Cc1ccc(N)cc1
4-ethynylaniline
C#Cc1ccc(NC(=O)C23CCC(NCC(=O)N4C[C@@H](F)C[C@H]4C#N)(CC2)CC3)cc1
(2S,4S)-1-[[N-[4-[N-(4-ethynylphenyl)amino]carbonylbicyclo[2.2.2]oct-1-yl]amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile
Ausbeute 15.3%

Reaktionsbedingungen

Detaillierte Bedingungen
See reaction.notes.procedure_details.

Vorschrift

In a similar manner to Example 63, ((2S,4S)-1-[[N-(4-carboxybicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile (50.0 mg) and 4-ethynylaniline (40.0 mg) were used to obtain (2S,4S)-1-[[N-[4-[N-(4-ethynylphenyl)amino]carbonylbicyclo[2.2.2]oct-1-yl]amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile (10.0 mg).

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US07560569B2uspto-grants-2009_07