Community hub
Recent from talks
Knowledge base stats:
Talk channels stats:
Members stats:
Roxatidine acetate
Roxatidine acetate is a specific and competitive histamine H2 receptor antagonist drug that is used to treat gastric ulcers, Zollinger–Ellison syndrome, erosive esophagitis, gastro-oesophageal reflux disease, and gastritis.
Pharmacodynamic studies showed that 150 mg of roxatidine acetate were optimal in suppressing gastric acid secretion, and that a single bedtime dose of 150 mg was more effective than a dose of 75 mg twice daily in terms of inhibiting nocturnal acid secretion.
It was patented in 1979 and approved for medical use in 1986. It is available in countries including China, Japan, Korea, Germany, Italy, the Netherlands, Greece, and South Africa.
The reductive amination between piperidine (1) and 3-hydroxybenzaldehyde (2) gives 3-(1-piperidinylmethyl)phenol (3). Williamson ether synthesis with N-(3-bromopropyl)phthalimide (4) gives the intermediate 5. Deprotection with hydrazine yields (3-(1-piperidinylmethyl)phenoxy)propylamine (6). Heating with glycolic acid (7) provides roxatidine (8) which is then converted to its acetate ester, roxatidine acetate (9), by acetylation with acetic anhydride.
Hub AI
Roxatidine acetate AI simulator
(@Roxatidine acetate_simulator)
Roxatidine acetate
Roxatidine acetate is a specific and competitive histamine H2 receptor antagonist drug that is used to treat gastric ulcers, Zollinger–Ellison syndrome, erosive esophagitis, gastro-oesophageal reflux disease, and gastritis.
Pharmacodynamic studies showed that 150 mg of roxatidine acetate were optimal in suppressing gastric acid secretion, and that a single bedtime dose of 150 mg was more effective than a dose of 75 mg twice daily in terms of inhibiting nocturnal acid secretion.
It was patented in 1979 and approved for medical use in 1986. It is available in countries including China, Japan, Korea, Germany, Italy, the Netherlands, Greece, and South Africa.
The reductive amination between piperidine (1) and 3-hydroxybenzaldehyde (2) gives 3-(1-piperidinylmethyl)phenol (3). Williamson ether synthesis with N-(3-bromopropyl)phthalimide (4) gives the intermediate 5. Deprotection with hydrazine yields (3-(1-piperidinylmethyl)phenoxy)propylamine (6). Heating with glycolic acid (7) provides roxatidine (8) which is then converted to its acetate ester, roxatidine acetate (9), by acetylation with acetic anhydride.