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药物详细合成路线

Name Famotidine;MK-208;YM-11170;Quamatel;Pepdine;Famodil;Gastridin;Pepcid RPD;Pepcid AC;Pepcid;Pepdul;Pepcidine;Gaster
Chemical Name 3-(2-Guanidinothiazol-4-ylmethylthio)-N-sulfamoylpropanamidine
CAS 76824-35-6
Related CAS
Formula C8H15N7O2S3
Structure
Formula Weight 337.44645
Stage 上市-1985
Company Merck & Co. (Originator), Yamanouchi (Originator), Sigma-Tau (Not Determined), Merck Sharp & Dohme (Licensee)
Activity/Mechanism Antiulcer Drugs, Esophageal Diseases, Treatment of, Gastric Antisecretory Drugs, Gastroesophageal Reflux Disease, Agents for, GASTROINTESTINAL DRUGS, Histamine H2 Receptor Antagonists
Syn. Route 1
Route 1
the reaction ot s-(2-aminothiazol-4-ylmethyl)isothiourea (i) with 3-chloropropionitrile (ii) by means of naoh in ethanol - water gives 3-(2-aminothiazol-4-ylmethylthio)propionitrile (iii), which is condensed with benzoyl isothiocyanate (iv) in refluxing acetone to afford 3-[2-(3-benzoylthioureido)thiazol-4-ylmethylthio]propionitrile (v). the hydrolysis of (v) with k2co3 in acetone - methanol - water yields 3-(2-thioureidothiazonl-4-ylmethylthio)propionitrile (vi), which by methylation with methyl iodide in refluxing ethanol is converted into 3-[2-(s-methylisothioureido)thiazol-4-ylmethylthio]propionitrile hydroiodide (vii). the reaction of (vii) with nh3 and nh4cl in methanol at 90 c in a pressure vessel affords 3-(2-guanidinothiazol-4-ylmethylthio)propionitrile (viii), which by partial alcoholysis with methanol by means of dry hcl in chcl3 is converted into methyl 3-(2-guanidinothiazol-4-ylmethylthio)propionimidate (ix). finally, this compound is treated with sulfamide in refluxing methanol.
List of intermediates No.
2-([4-(2-benzoyl-4-chlorophenyl)-5-[(dimethylamino)methyl]-4h-1,2,4-triazol-3-yl]methyl)-1h-isoindole-1,3(2h)-dione (iv)
sodium (z)-1-(cyclopropylamino)-3-ethoxy-3-oxo-2-(2,4,5-trifluorobenzoyl)-1-propene-1-thiolate (i)
sodium (e)-1-(cyclopropylamino)-3-ethoxy-3-oxo-2-(2,4,5-trifluorobenzoyl)-1-propene-1-thiolate (ii)
ethyl (z)-3-(cyclopropylamino)-3-(methylsulfanyl)-2-(2,4,5-trifluorobenzoyl)-2-propenoate (iii)
ethyl (e)-3-(cyclopropylamino)-3-(methylsulfanyl)-2-(2,4,5-trifluorobenzoyl)-2-propenoate (v)
ethyl 1-cyclopropyl-6,7-difluoro-2-(methylsulfanyl)-4-oxo-1,4-dihydro-3-quinolinecarboxylate (vi)
ethyl 1-cyclopropyl-6,7-difluoro-2-(methylsulfinyl)-4-oxo-1,4-dihydro-3-quinolinecarboxylate (vii)
ethyl 1-cyclopropyl-6,7-difluoro-4-oxo-2-sulfanyl-1,4-dihydro-3-quinolinecarboxylate (viii)
ethyl 2-(aminosulfanyl)-1-cyclopropyl-6,7-difluoro-4-oxo-1,4-dihydro-3-quinolinecarboxylate (ix)
Reference 1:
    isomura, y.; ishii, y.; ito, n.; takeda, m.; yanagisawa, i.; hirata, y.; tsukamoto, s. (yamanouchi pharmaceutical co., ltd.); guanidinothiazole cpds., process for preparation and gastric inhibiting compsns. containing them. us 4283408 .
Reference 2:
    hirata y.; et al. (yamanouchi pharmaceutical co., ltd.); novel amidine derivative and its preparation. be 0882071; de 2951675; de 3008056; fr 2450827; gb 2052478; gb 2055800; jp 55118476; nl 7909321; nl 8001361 .
Reference 3:
    blancafort, p.; castaner, j.; hillier, k.; serradell, m.n.; famotidine. drugs fut 1983, 8, 1, 14.

来源:药化网

作者:药化小编

摘要:本文合成路线介绍的是药物中文名法莫替丁;英文名Famotidine;MK-208;YM-11170;Quamatel;Pepdine;Famodil;Gastridin;Pepcid RPD;Pepcid AC;Pepcid;Pepdul;Pepcidine;Gaster;CAS[76824-35-6]

 
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