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1. WO2006018846 - PROCESS FOR PREPARING 1,2,3,9-TETRAHYDRO-9-METHYL-3-METHYLENE-4H- CARBAZOL-4-ONE AND ONDANSETRON THEREFROM

Publication Number WO/2006/018846
Publication Date 23.02.2006
International Application No. PCT/IL2005/000893
International Filing Date 17.08.2005
IPC
C07D 233/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
233Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
04having one double bond between ring members or between a ring member and a non-ring member
C07D 403/10 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
10linked by a carbon chain containing aromatic rings
A61K 31/415 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
41having five-membered rings with two or more ring hetero atoms, at least one of which is nitrogen, e.g. tetrazole
4151,2-Diazoles
CPC
C07D 209/88
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
209Heterocyclic compounds containing five-membered rings, condensed with other rings, with one nitrogen atom as the only ring hetero atom
56Ring systems containing three or more rings
80[b, c]- or [b, d]-condensed
82Carbazoles; Hydrogenated carbazoles
88with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to carbon atoms of the ring system
C07D 403/06
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
02containing two hetero rings
06linked by a carbon chain containing only aliphatic carbon atoms
Applicants
  • TARO PHARMACEUTICAL INDUSTRIES LTD. [IL]/[IL] (AllExceptUS)
  • GUTMAN, Daniella [IL]/[IL] (UsOnly)
  • CYJON, Rosa [IL]/[IL] (UsOnly)
Inventors
  • GUTMAN, Daniella
  • CYJON, Rosa
Agents
  • PEARL COHEN ZEDEK LATZER
Priority Data
60/602,14117.08.2004US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) PROCESS FOR PREPARING 1,2,3,9-TETRAHYDRO-9-METHYL-3-METHYLENE-4H- CARBAZOL-4-ONE AND ONDANSETRON THEREFROM
(FR) PROCESSUS DE PREPARATION DE 1,2,3,9-TETRAHYDRO-9-METHYL-3-METHYLENE-4H-CARBAZOL-4-ONE ET ONDANSETRON ASSOCIE
Abstract
(EN) The present invention provides a rapid, high-yielding process for preparing 1,2,3,9-tetrahydro-9-methyl-3-methylene-4H-carbazol-4-one from 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one without using a secondary amine as a catalyst, and without using glacial acetic acid as a solvent. The present invention further provides a rapid, high-yielding process for preparing ondansetron from 1,2,3,9-tetrahydro-9-methyl-3-methylene-4H-carbazol-4-one without using alumina as a catalyst.
(FR) La présente invention concerne un processus rapide à rendement élevé de préparation de 1,2,3,9-tétrahydro-9-méthyl-3-méthylène-4H-carbazol-4-one à partir de 1,2,3,9-tétrahydro-9-méthyl-4H-carbazol-4-one sans utiliser une amine secondaire en tant que catalyseur et un acide acétique glacial en tant que solvant. Cette invention a aussi pour objet un processus rapide à rendement élevé de préparation d'ondansétron à partir de 1,2,3,9-tétrahydro-9-méthyl-3-méthylène-4H-carbazol-4-one sans utiliser d'alumine en tant que catalyseur.
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