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Pharmaceutical Substances Syntheses, Patents, Applications - Part 8

Pharmaceutical Substances Syntheses, Patents, Applications - Part 8. 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 | Alprazolam A 71 1. POCI 2. 0 h3c n ch3 1. phosphorus oxychloride 2. dipropylomine Referencef s EP 50 563 Synthelabo appl. 15.10.1981 F-prior. 22.10.1980 . US 4 382 938 Synthelabo 10.5.1983 F-prior. 22.10.1980 . US 4460 592 Synthelabo 17.7.1984 F-prior. 22.10.1980 . Formulation s tabl. 50 mg Trade Name s F Anaxyi Synthelabo 1991 wfm Alprazolam ATC N05BA12 Use tranquilizer RN 28981-97-7 MF C17H13C1N4 MW 308.77 EINECS 249-349-2 LD50 770 mg kg M p.o. 1220 mg kg R p.o. CN 8-chloro-1 -methyl-6 phenyl-4H- 1 2 4 triazolo 4 3-a 1 4 benzodiazepine h2n-nh2-h2o a hydrozine hydrote nh2 ch3-c o-ch2ch3 3 xylene triethyl orthoacetate 7-chloro-1 -methyl-5-phenylp 2 4 triozolo- 4 3-a quinaline I 2 6-dichloro- 6-chlaro 2-hydrazino 4-phenyiquinoline 4-phenylquinoline NoIO4 RuO2 ocetone f-LO I -----------2----- sodium periodate ruthenium dioxide 1. HCHO 2. PBr3 CHC13 1. formaldehyde 2. phosphorus lll bromide NH THF CH 0H n ------------ Alprazolam 72 A Alprenolol 4-chloroaniline benzoyl ZnCI2 2-omino-5-chloro-benzaphenone H2rOr -CH3 HCI 0 pyridine I ethyl glycinate hydrochloride chloride ocetohydrozide ch3-co-nh-nh2 butonol P4S1O -------------k phosphorus v sulfide 7-chloro-5-phenyl- 7-chloro-5-phenyl - 2- 2-ocetylhydrazinõ - 2-oxo-2 3-dihydro-1H- 2-thioxo-2 3-dihydro 7-ch loro-5-phenyl-3H- 1 4-benzodiazepine ni 1H- Ĩ 4-benzodiozepine 1 4-benzodiozepine IV 250 C IV ----------- Alprazolam Reference s US 3 987 052 Upjohn 19.10.1976 appl. 29.10.1969 USA-prior. 17.3.1969 . US 3 980 789 Upjohn 14.9.1976 appl. 19.6.1972 USA-prior. 29.3.1971 . DE 1 955 349 Takeda D-prior. 4.11.1969 . GB 1 298 364 Upjohn GB-prior. 27.10.1969 . a DOS 2 203 782 Upjohn appl. 27.1.1972 USA-prior. 9.2.1971 . US 3 709 898 Upjohn 9.1.1973 prior. 9.2.1971 . US 3 781 289 Upjohn 25.12.1973 prior. 11.5.1972 . b DOS 2 012 190 Upjohn appl. 14.3.1970 USA-prior. 17.3.1969 . Formulation s tabl. 0.25 mg 0.5 mg 1 mg 1 g Trade Name s D Cassadan 0 25 0 5 1 ASTA F Xanax Upjohn 1984 Medica AWD Tafil 0 5 1 0 Tabletten Pharmacia .