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Pharmaceutical Substances Syntheses, Patents, Applications - Part 137

Pharmaceutical Substances Syntheses, Patents, Applications - Part 137. 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 | Montelukast sodium M 1361 aa synthesis of intermediate VI OH OH soci2 ch2ci2 ---------------- NaCN CH2CI2 -------------- NC OH 1 1 -cyclopropanedimethanol 2- 1 - hydroxymethyl -cyclop ropyl -acetonitrile VUI 1. h3cso2ci n c2h5 3 2. H3C CO SK Vin ---------------------------- 1. mesyl chloride 2. potassium thioacetate NoOH taluene H2O ----------------- 2 1 - ocetylthio -cyclopropyl ocetonitrile LiAIH4 THF 0 pyridine CH2CI2 benzoyl chloride IX diethyl cyclo-propone-1.1-di-carboxylate 1. h3cso2ci 2. NaCN DMSO ---------------- K 2- 1- benzoyloxy- methyl cyclopropyl - acetonitrile X 1. KOH ethonol 2. CH2N2 8 3. H3C S Cl 2 u H-jC SCs CH2CI2 ----------- cesium thioacetate methyl 2- 1- acetyl-thiomethyl cyclopropyl -acetate XI xn 1362 M Moperone xni 1. Tos OH pyridine 2. NaOH --- ------------- Montelukast sodium fH3 ÇHj 1. Cl ----I---CH3k ch3 ch3 DMAP CH2CI2 XIV 1. tert-butyldimethyl-silyl chloride 2. 3 4-dihydro-2H-pyran 1. Bu4N F . THF L. 2. HjC Cl 0 MV XII Reference s a EP 480 717 Merck Frosst appl. 10.10.1991 USA-prior. 12.10.1990 8.8.1991 . aa US 5 523 477 Merck Co. 4.6.1996 USA-prior. 23.1.1995 . b wo 9 518 107 Merck Co. appl. 22.12.1994 USA prior. 28.12.1993 9.12.1994 . Labelle M. et al. Bioorg. Med. Chem. Lett. BMCLE8 5 283 1995 . synthesis of starting material I US 4 851 409 Merck Frosst Can. 25.7.1987 USA-prior. 14.2.1986 . pharmaceutical composition with loratidine WO 9 728 797 Merck Co. appl. 4.2.1997 USA-prior. 8.2.1996 . Formulation s chewable tabl. 5 mg 50 mg f. c. tabl. 10 mg tabl. 5 mg 10 mg as sodium salt Trade Name s D Singulair MSD I Lukasm Sigmatau USA Singulair Merck Sharp Dieckmann Montegen Gentili Dohme 1998 GB Singulair Merck Sharp Singulair Merck Sharp Dohme Dohme Moperone Methylperidol Mopiperone ATC N05AD04 Use neuroleptic antipsychotic RN 1050-79-9 MF C22H26FNO2 MW 355.45 EINECS 213-887-6 CN l- 4-fluorophenyl -4- 4-hydroxy-4- 4-methylphenyl -l-piperidinyl -l-butanone Mopidamol M 1363 hydrochloride RN 3871-82-7 MF C22H26FNO2 HC1 MW 391.91 EINECS