TAILIEUCHUNG - Pharmaceutical Substances Syntheses, Patents, Applications - Part 184

Pharmaceutical Substances Syntheses, Patents, Applications - Part 184. Reference containing a collection of 2267 active pharmaceutical ingredients, including those launched recently. Listed alphabetically according to their INNs and established a link between INNs, structure, synthesis and production processes, patent and literature situation, medical use, and trade names. For pharmacists and researchers. | Rofecoxib R 1831 H2o2 5 mois No2WO4 a Cl Cl hydrogen peroxide o-dichlorobenzene Sr2 CHjCOOH ------------- in bromine in acetic acid 4 - methylsulfonyl -acetophenone II IV 2-bromo-4 - methyl- phenylocetic acid sulfanyl acetophenone ni sodium sait H IjC NyCHj -----L2--------- G V -_ Mg2 yCO0 v CH2CI2. CHjOH Br2 AlCIj CHCI3 --------------------------------- ---------------------- magnesium monoperoxyphtholate MMPP III HOOC CHjCN N C2H5 3 Rofecoxib phenylocetic acid IV DBU 1 8-diozabicyclo- undec-7-ene Rh4 C0 12 THF H2O 10Û C 100 bar --------------------- Rofecoxib 1832 R Rofecoxib H3C Li . H3C O ch3. ch3 CuF 78 C fH3 2-H3C- i-CH3 CH3 ----------------------------- 1. tert-butyllithium 2. trimethylsilyl chloride 4-bromo- 2 5H - thioonisole V furanone H3C-S 4- 4- methylthio -phenyl -2 5H -furanone VI VI ---------------------------------k 1. palladium U acetate 2. iodine pyridine 3-iodo-4- 4- methylthio phenyl - 2 5H -furanone VII ethyl bromaacetote ethyl 2- pheny acetoxy -ocetate VIII VIII Rolitetracycline R 1833 B OH 2 Çj No2C03 Pd PPh3 H3C s or 1. LiBr or LiCI 2. X No2CO3 Pd PPh3 4 4- methylthio phenylboronic ocid X 2 KHSO5 KHS04 K2SO4 --------------------------- Rofecoxib synthesis of 4- methylthio phenylboronic acid CH3 -78 c V . O CHj 2- H2SO4. H2ũ - v . I 7. ---------------- X ÇH I CH . _ x _ I J 8 I 0 1. butyllithium HjC TD 0 CH3 triisopropyl borate Reference s a WO 9 800 416 Merck Co. appl. GB-prior. . b WO 9 613 483 Merck Frosst Canada appl. USA-prior. e WO 9 608 482 Merck Co. appl. USA-prior. . a-e WO 9 500 501 Merck Frosst Canada Inc. appl. USA-prior. . The discovery of rofecoxib Prasit P. et al. Bioorg. Med. Chem. Lett. BMCLE8 9 13 1773 1999 . alternative syntheses WO9636 623 Merck Frosst Canada appl. USA-prior. . GB 2 294 879 Merck Co. appl. USA-prior. . WO9 619469 Merck Frosst Canada appl. .

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