morpholine_methylmorpholine_morpholine information network Knowledge preparation method of 4-(3-bromophenyl)piperidine hydrochloride_kain industrial additive

preparation method of 4-(3-bromophenyl)piperidine hydrochloride_kain industrial additive

background and overview[1]

4-(3-bromophenyl)piperidine hydrochloride can be used as a pharmaceutical synthesis intermediate. if 4-(3-bromophenyl)piperidine hydrochloride is inhaled, move the patient to fresh air; if skin contact occurs, remove contaminated clothing and rinse skin thoroughly with soap and water. if discomfort occurs , seek medical attention; if eye contact occurs, separate eyelids, rinse with running water or saline, and seek medical attention immediately; if ingested, rinse mouth immediately, do not induce vomiting, and seek medical attention immediately.

preparation[1]

the preparation of 4-(3-bromophenyl)piperidine hydrochloride is as follows: 4-(3-bromo-phenyl)-piperidine (1.0g, 3.6mmol) is added to hydrochloride, and the reaction product is isolated. 4-(3-bromophenyl)piperidine hydrochloride, a white solid (0.43 g, 41%), was used without further purification. 1hnmr (400mhz, (d3c)2so, δ, ppm): 10.52 (s, 1h), 7.47-7.41 (m, 2h), 7.37-7.21 (m, 2h), 3.52-3.41 (m, 2h), 3.10- 2.95 (m, 2h), 2.85-2.78 (m, 1h), 2.75 (s, 3h), 2.15-2.78 (m, 4h).

apply[1]

4-(3-bromophenyl)piperidine hydrochloride can be used as a pharmaceutical synthesis intermediate. as prepared:

composed of 8-(4-methanesulfonyl-phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-ylamine (75.0mg, 0.260mmol) and 4- (3-bromophenyl)piperidine hydrochloride was used as the reactant, and 2,2′-bis-dicyclohexylphosphoryl-biphenyl (30.0 mg, 0.0549mmol) was used as the ligand. hydrochloride (90.0 mg ,0.310mmol). the title compound was isolated as a brown solid (0.031 g, 26%). mp=208-210℃. 1hnmr (400mhz, cdcl3, δ, ppm): 8.51 (d, j=6.5hz, 1h), 8.08 (d, j=8.3hz, 2h), 8.10 (d, j=7.3hz, 2h), 7.66 (d , j=6.6hz, 1h), 7.55 (s, 1h), 7.38 (d, j=8.7hz, 1h), 7.31-7.25 (m, 1h), 7.02 (t, j=7.4hz, 1h), 6.91 -6.85 (m, 2h), 3.10 (s, 3h), 3.01 (d, j=10.9hz, 2h), 2.57-2.45 (m, ih), 2.35 (s, 3h), 2.11-2.03 (m, 2h ), 1.92-1.83 (m, 4h). ms=462(mh)+.

main reference materials

[1] (wo2010141796)preparationandusesof1,2,4-triazolo[1,5a]pyridinederivatives

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