TAILIEUCHUNG - Pharmaceutical Substances Syntheses, Patents, Applications - Part 27

Pharmaceutical Substances Syntheses, Patents, Applications - Part 27. 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 | Brinzolamide B 261 11 J CH2 Tos-OH THE ------------- 0 ethyl vinyl ether O O CH-5 ch3 -2- 3-bromopropyl -4- l -ethoxyethoxy -3 4-dihydro-2H-thieno- -1 2-thiazine H3C ONa -----------k V sodium methylate 1 1 -dioxide CH 3 ch3 V CrOj HjSO acetone VI ------------------- 1. BuLi THF 2. S02 3. HOSA 2. sulfur dioxide VI 0 V CH H2N iKXJj 0 0 3 4-dihydro-2- 3-methoxypropyl -4-oxo 2H-thieno 3 2-e -1 2-thiazine-6-sulfonamide VII 1. -Jpc2BCI THF 2. Tos-CI. THF 3. H2N CH3 VII ------------------------------ 1. - 3-chlorodiisopropyl-campheyl borane 2. tosyl chloride 3. ethylamine Vin 0 V CH H N S-4 1 J 2 II 0 HN CHj Brinzolamide 1. HCI THF 2. pyridinium perbromide 3aS -tetrahydro-1 -methyl-3 3-diphenyl-1H 3H-pyrrolo l 2-c -1 3 2-oxozaborole BH THF i------------------- a NaOH ------ NaH THF ---------------------- 3-bromo-1 -methoxy- propone X V Brinzolamide 262 B Brinzolamide U . H2N NH2 ethonol H2O thiourea 0 3-acetyl-2 5- benzyl dichlorothiophene chloride 3-acetyl-5-chlaro- 2- benzylthio - thiophene XII XII 1. Cl2 ethyl acetate 2. NH3 3. H2O2 3-ocetyl-5-chloro- pyridinium perbromide ethyl acetate O C ---------------------- XIII 2-thiophene- sulfonamide 3- bromoocetyl - 5-chloro-2-thiophenesulfonamide XIII 1. - pc2BCI. MTBE 40 C 2. NoOH K CO DMSO XIV 4- x 2__-__ OH S -3 4-dihydro-6-chlaro- 4- hydroxy- 2 - 3- meth oxypropyl -2H-thieno 3 2-e - 1 2-thiazine 1 1-dioxide XV 1. BuLi 2. SO2 THF 70 C 3. HOSA XV ------------------- XVI 1 HjC- -O CH3 o ch3 2. Tos CI N C2H5 3 3. H2N CH3 THF 1. trimethyl orthoacetate 3. ethylamine XVI Brinzolamide Reference s a US 5 378 703 Alcon USA-prior. . b US 5 470 973 Alcon USA-prior. . c Conrow . et al. Org. Process Res. Dev. OPRDFK 3 114-120 1999 . Brodimoprim B 263 ophthalmic compositions with prostaglandins WO9 853 809 Merck Co. appl. USA-prior. . WO 9 819 680 Alcon appl. USA-prior. . process for manufacturing .

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