Pharmaceutical Substances Syntheses, Patents, Applications - Part 37. 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 | Carticaine C 361 synthesis of intermediate 5-hydroxy-1 2 3 4-tetrahydroquinolin-2-one Shono T. et al. J. Org. Chem. JOCEAH 46 3719 1981 . Formulation s eye drops 1 2 tabl. mg 5 mg 20 mg as hydrochloride Trade Name s Arteoptic CIBA Vision 1984 Endak Madaus 1982 Carpilo Chauvin -comb. Cartéol Chauvin 1985 Mikelan Lipha Saneé GB Teoptic CIBA Vision 1986 I Carteol SIFI 1987 J Mikelan Otsuka 1980 USA Cartrol Abbott Carticaine ATC N01B N01BB08 NO1BB58 Use local anesthetic RN 23964-58-1 MF C13H20N2O3S MW CN 4-methyl-3- l-oxo-2- propylamino propyl amino -2-thiophenecarboxylic acid methyl ester monohydrochloride RN 23964-57-0 MF C13H20N2O3S HC1 MW EINECS 245-957-7 LD50 37 mg kg M . . h3c nh2 methyl 3-omina-4-methylthiophene-2-carboxylote 2-bromo-propionyl chloride propylomine Carticaine Reference s DAS 1 643 325 Hoechst appl. . US 3 855 243 Hoechst D-prior. . Formulation s amp. lOmg ml 20 mg ml 40 mg ml 50 mg ml Trade Name s D Ultracain Hoechst F Alphacaine SPAD -comb. Carumonam AMA-1080 Ro-17-2301 ATC S01AA Use antibacterial monobactam antibiotic RN 87638-04-8 MF C12H14N6O10S2 MW CN 2S- 2a 3a Z - 2- 2- aminocarbonyl oxy methyl -4-oxo-l-sulfo-3-azetidinyl amino -l- 2-amino-4-thiazolyl -2-oxoethylidene amino oxy acetic acid disodium salt RN 86832-68-0 MF C12H12N6Na2Oi0S2 MW 362 c Carumonam azetidinone intermediate H2O2 CoCO-j hydragen peroxide 1. HBr. CH3COOH 2. HjC OH 0 Br o-ch3 ascorbic ocid I 0 KO- ch3 DMF. KI I ------------ methyl 2R 3S -4- CH3OH 2. NH40H ---------------- acetoxy-2 3-epoxy-butanoate 1. CH30H hci 2. NH-j CH3OH 3. NaHC03 Z Cl n ------------------------------ 3. benzyl chlorofarmote nh2 Ct V01 DMAA 0 - -------------------- ni chloroacetyl chloride dimethylacetamide z NH OH 0 II ci s CH. II 3 0 N C2Hs 3 IV methonesulfonyl chloride ỞCH3 ch2ci2 2. KHS04 3. Bu4n hso ------------------------- 1. sulfur triaxide-2-picoline complex 3. tetrobutylammonium hydrogen sulfote V Bu4N Carumonam c 363 .
