TAILIEUCHUNG - Pharmaceutical Substances Syntheses, Patents, Applications - Part 141

Pharmaceutical Substances Syntheses, Patents, Applications - Part 141. 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 | Naproxen N 1401 Br S -2- 5-bromo-6-methoxy-2-nophthyl -propanoic acid XII H2 Pd-C Noproxen Stereospecific Syntex process 0 h3cY o xch3 OH Ms CI N C2H5 3 --------- 1. NaOH 0 2. SOCL 0 h3cV o xch3 h3cy ci CL o. Ms Ms mesyl Chloride XIII ethyl S -Ioctate 0 ll Ms S CH- 0 IRC-50S resin 115-120 C ------------------------- CH3H C u r I T T Î CH3 XVI XVI H30 Noproxen Reference s process review Harrington . Lodewijk E. Organic Process Res. Dev. 1 72 1997 . Harrison . et al. J. Med. Chem. JMCMAR 13 203 1970 . a US 3 896 157 Syntex prior. . US 3 904 682 Syntex prior. . US 3 978 116 Syntex prior. . US 3 978 124 Syntex prior. . US 3 998 966 Syntex prior. . US 4 001 301 Syntex prior. . US 4 009 197 Syntex prior. . DAS 1 668 654 Syntex appl. USA-prior. . improved racemate resolution with cinchonidine DAS 2 319 245 Syntex appl. USA-prior. . 1402 N Naproxen racemization DAS 2 008 272 Syntex appl. USA-prior. . b US 3 663 584 Syntex appl. . similar process with Cu-compound US 3 658 863 Syntex appl. . similar process with Cd-compound US 3 694 476 Syntex appl. . c DOS 2 805 488 Syntex appl. USA-prior. . resolution with N-alkyl-D-glucamines US 4 515 811 Syntex USA-prior. . EP 7 116 Syntex appl. CH-prior. . DOS 3 025 448 Syntex appl. USA-prior. . d Ohta T. et al. J. Org. Chem. JOCEAH 52 3174 1987 . DOS 2 919 919 Montedison appl. I-prior. . US 4 239 914 Montedison I-prior. . electrocarboxylation o 2-acetyl-6-methoxynaphthalene Chan . et al. J. Org. Chem. JOCEAH 60 742 1995

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