4-Piperidinecarboxylic acid → 1-(Benzocyclobuten-1-ylmethyl)-4-piperidinecarboxylic acid
Reaction equation
I[CH2:2][CH:3]1[C:6]2=[CH:7][CH:8]=[CH:9][CH:10]=[C:5]2[CH2:4]1.[NH:11]1[CH2:16][CH2:15][CH:14]([C:17]([OH:19])=[O:18])[CH2:13][CH2:12]1.C(N(CC)CC)C>CN(C)C=O>[C:3]1([CH2:2][N:11]2[CH2:16][CH2:15][CH:14]([C:17]([OH:19])=[O:18])[CH2:13][CH2:12]2)[C:6]2[CH:7]=[CH:8][CH:9]=[CH:10][C:5]=2[CH:4]=1Participants
5
Procedure
0.028 mole of 1-(iodomethyl)benzocyclobutene (Process 1, stage G), 0.028 mole of 4-piperidinecarboxylic acid and 0.028 mole of triethylamine are mixed in 95 ml of dimethylformamide. The mixture is brought to 60° C. for 6 hours. It is evaporated to dryness, the residue is taken up with ethyl acetate and water and settling is allowed to take place.