336882-06-5

Upstream product

• 927-68-4 bromoethyl acetate 
• 336881-92-6 N,N-dimethyl-2,2-diphenyl-4-[4-hydroxy-4-(3-hydroxyphenyl)piperidin-1-yl]butanamide 
• 188863-55-0 1-benzyl-4-[3-(benzyloxy)phenyl]-4-hydroxypiperidine 
• 325808-14-8 4-hydroxy-4-(3-hydroxyphenyl)piperidine 
• 36281-96-6 <3-(benzyloxy)phenyl>magnesium bromide 
• 3612-20-2 1-phenylmethyl-4-piperidone 

Downstream Products

• 336882-18-9 4-{4-hydroxy-4-[3-(2-hydroxy-ethoxy)-phenyl]-piperidin-1-yl}-N,N-dimethyl-2,2-diphenyl-butyramide 

Relevant academic research and scientific papers

4-hydroxy-4-phenylpiperidine derivatives and pharmaceuticals containing the same

Described is a 4-hydroxy-4-phenylpiperidine derivative represented by the following formula (1): [wherein, R1and R2are the same or different and each independently represents a hydrogen atom, a lower alkyl, or the like, R3represents a hydrogen atom or a group —(CR4R5)n—Y (in which, R4and R5each represents a hydrogen atom or a lower alkyl group, Y represents a group —COOR6, —CONR7R8, —OR9or —OCOR10(in which R6, R9and R10each independently represents a hydrogen atom, a lower alkyl group, or the like, R7and R8are the same or different and each independently represents a hydrogen atom, a lower alkyl group, or the like), and n stands for 1 to 6)], or salt thereof. The compound exhibits excellent peripheral analgesic action.

New μ-opioid receptor agonists with phenoxyacetic acid moiety

New μ-opioid receptor (MOR) agonists containing 4-hydroxypiperidine, piperidine and piperazine moieties were synthesized and evaluated to find a peripheral opioid analgesic. Among the synthesized compounds, [2-[1-[3-(N,N-dimethylcarbamoyl)-3,3-diphenylpropyl]-4-hydroxypiperidin-4-yl] phenoxy]acetic acid (8: SS620) having phenoxyacetic acid and 4-hydroxypiperidine moieties showed the highest agonist potency on the MOR in an isolated guinea-pig ileum preparation, and it also had selectivity to the human MOR expressed in Chinese hamster ovary (CHO)-K1 cells compared with the same types of δ- and κ-opioid receptors (DOR and KOR). In addition, compound 8 showed a 10 times more potent MOR agonist activity than loperamide. Furthermore, compound 8 showed a peripheral analgesic activity in vivo screening on rat.