Pharmaceutical Substances Syntheses, Patents, Applications - Part 183. 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. | Risperidone R 1821 o 0 CH3 3 1. Na C2H5OH 2. KOH H20 COOH SOCI2 ------- VI bis 2-chloro- diethyl molonate ethyl ether tetrahydropyron- 4-carboxylic acid OyCI 1 0 tetra hydropyran- 4-corbonyl chloride VI AICI3 2 4-difluorophenyl - tetrohydropyran- 4-yl methanone h2n-oh hci c2h5oh -------- ---- KOH. CH OH VI ------------5--- 0 1. U Nol. CH-zCN H3C CI 2. No2CO3 CH3OH VIII 6-fluoro-3- tet ra hyd ropyron -4-yl -1 2-benz-isoxazole CH3CN NaHCO3 ----------------- Risperidone VIII IX preparolion of intermediates V and IX 1. H2 Pd-C 2. SOCI2 2-amino-pyridine 2-ocetyl-butyrolactone 3- 2-hydroxyethyl - 2-methyl-4H-pyrido- 1 2-a pyrimidin-4-one 2. H2. Pd-C V ------------- 1. dibutylamine Reference s a EP 196 132 Janssen Pharmaceutica N. V. appl. USA-prior. . b ES 2 074 966 Vita-invest S. A. appl. E-prior. . 1822 R Ritodrine preparation of l-acetyl-4-piperidinecarbonylchloride Strupczewski . Allen . Gardner . Schmid . Stäche U. J. Med. Chem. JMCMAR 28 6 761 1985 . preparation o tetrahydropyran-4-carboxylìc acid Radiszewski . Kaszynski P Littmann D. Balaji V Hess . Michl J. J. Am. Chem. Soc. JACSAT 115 18 8401 1993 Straessler c. Linden A. Heimgartner H. Helv. Chim. Acta HCACAV 80 5 1528 1997 Angelastro . Baugh Bey p. Burkhardt Chen Teng-Man J. Med. Chem. JMCMAR 37 26 4538 1994 preparation ơ 3- 2-hydroxyethyl -2-methylpyrido l 2-a pyrimidin-4-one Willenbrock et al. Justus Liebigs Ann. Chem. JLACBF 1973 107 108 109 Formulation s f. c. tabl. 1 mg 2 mg 3 mg 4 mg sol. 100 ml 1 mg ml Trade Name s D Risperdal Janssen-Cilag I Risperdal Organon Belivon Organon Risperdal Janssen-Cilag USA Risperdal Janssen Pharmac. GB. Risperdal Janssen-Cilag J Risperdal Janssen-Kyowa Ritodrine ATC G02CA01 Use uterus relaxant RN 26652-09-5 MF C17H21NO3 MW EINECS 247-879-9 CN J 5 -4-hydroxy-a- l- 2- 4-hydroxyphenyl ethyl amino ethyl benzenemethanol hydrochloride RN 23239-51-2 MF CI7H21NO3 HC1 MW EINECS 245-514-8 LD50
