反応 #1136

ord-78d0ff9eaef04c19a3803165f28b1df6

反応方程式

c1ccncc1
pyridine
O=C(O)/C=C/C(=O)O
fumaric acid
Fc1ccc(-c2cncc(C3CCCCN3)c2)cc1
amine
Fc1ccc(-c2cncc(C3CCCCN3)c2)cc1
5-(4-fluorophenyl)-3-(2-piperidinyl)pyridine
Fc1ccc(-c2cncc(C3CCCCN3)c2)cc1.O=C(O)/C=C/C(=O)O
5-(4-fluorophenyl)-3-(2-piperidinyl)pyridine fumarate
収率 70.0%

溶媒

反応条件

詳細条件
See reaction.notes.procedure_details.

後処理

  1. 1
    その他After 30 minutes the solvent was removed in vacuo

実験手順

The above described pyridine derivative was converted into invention compound of Formula I by the addition of one equivalent of fumaric acid to a methanol (15 mL) solution of the free amine at 25° C. After 30 minutes the solvent was removed in vacuo and the residue pumped under high vacuum. Trituration with diethyl ether resulted in the formation of 5-(4-fluorophenyl)-3-(2-piperidinyl)pyridine fumarate (70%) as a colorless solid.

出典

DOI: 10.6084/m9.figshare.5104873.v1特許: US05723477uspto-grants-1998_03