Roxatidine acetate hydrochloride

Roxatidine Acetate HCl is a specific and competitive histamin H2 receptor antagonist.Target: Histamin H2 ReceptorRoxatidine acetate is a histamine H2-receptor antagonist which, after almost complete oral absorption (greater than 95%), is rapidly converted to its active metabolite, roxatidine, by esterases in the small intestine, plasma and liver. Roxatidine is a potent inhibitor of basal and stimulated gastric acid secretion in animals and humans and, like most other H2-receptor antagoni

Roxatidine acetate hydrochloride is a member of piperidines. It contains a Roxane.

After dissolving 58 g (0.930 mol, according to 90percent content) of potassium hydroxide in 1160 g of water and cooling to 2025° C., 300 g (0.854 mol) of rosartan oxalate (compound 9, manufactured in Example 7) was added with stirring. Got)Then add ethyl acetate (600g+450g), combine the organic phases, dry over anhydrous sodium sulfate, and filter.The filtrate is concentrated, Product Roxaidine (Compound 8)251 g of the above-obtained 251 g of roctatin is dissolved with 500 g of glacial acetic acid, and then 170 g of acetic anhydride is added.Heat to refluxShould be 2hr; confirm the reaction is completed, the acetic acid is concentrated under reduced pressure, cooled to 15 ~ 20 °C, adding 600g of water, Then add 600g of ethyl acetate; under stirring, adjust pH=9~10 with aqueous solution containing 300g of potassium carbonate, liquid, waterThe phases were extracted with ethyl acetate (400 g + 300 g). The organic phases were combined, dried over anhydrous sodium sulfate, filtered, and the filtrate was concentrated to obtain 280 g of rosatilide acetate (Compound 10).280 g (0.804 mol) of roxamidine acetate obtained above was dissolved with 1400 g of acetone, After cooling to 0-5°C, an ethyl acetate solution containing 32 g of hydrogen chloride was added dropwise to precipitate solids.Stir and incubate at 05°C, crystallize 35hr, filter and dry it to get 295g of rozatidine acetate hydrochloride (theoretical amount: 328.58g; calculate with 300g compound 9); Yield: 89.8percent

antibacterial

Molecular Weight:384.9
Hydrogen Bond Donor Count:2
Hydrogen Bond Acceptor Count:5
Rotatable Bond Count:10
Exact Mass:384.1815851
Monoisotopic Mass:384.1815851
Topological Polar Surface Area:67.9
Heavy Atom Count:26
Complexity:410
Covalently-Bonded Unit Count:2
Compound Is Canonicalized:Yes