PROCESSES FOR THE PREPARATION OF AMINOALKYL PHENYLCARBAMATES

WIPO Patent Application WO2005061446

A3

The present invention relates to a process for preparing an aminoalkyl phenylcarbamate (4), comprising the steps of converting a hydroxy phenyl ketone (2) to a phenylcarbamate ketone (3), and converting the phenylcarbamate ketone (3) to the desired aminoalkyl phenylcarbamate (4). Optionally the aminoalkyl phenylcarbamate (4) may be resolved into its enantiomers and/or converted into a pharmaceutically acceptable acid addition salt. The invention further relates to aminoalkyl phenylcarbamates (4) and pharmaceutically acceptable salts prepared by the above process, in particular, to rivastigmine (1) and rivastigmine hydrogen tartrate (9). The aminoalkyl phenylcarbamates (4) may be comprised in pharmaceutical compositions. The invention further relates to a method of inhibiting acetylcholine esterase or treating dementia, senile dementia, Alzheimer's disease, Huntington's chorea, tardive dyskinesias, hyperkinesia, a confusion disorder, ataxia, Friedrich's ataxia, Down's syndrome, mania or an acute confusion disorder, using the aminoalkyl phenylcarbamates (4) of the present invention.

GAITONDE ABHAY (IN)
MANGLE MANGESH (IN)
PAWAR SANJAY R (IN)

PCT/GB2004/050042

January 05, 2006

December 17, 2004

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GENERICS UK LTD (GB)
GAITONDE ABHAY (IN)
MANGLE MANGESH (IN)
PAWAR SANJAY R (IN)

A61K31/27; C07C269/00; C07C269/02; C07C269/04; C07C269/06; C07C269/08; C07C271/44; (IPC1-7): C07C269/02; A61K31/27; C07C269/04; C07C269/06; C07C269/08; C07C271/44

WO2004037771A1	2004-05-06
WO2000014057A1	2000-03-16

US4948807A

1990-08-14

CISZEWSKA G ET AL: "SYNTHESIS OF TRITIUM, DEUTERIUM, AND CARBON-14 LABELED (S)-N-ETHYL-N-METHYL-3-[1-(DIMETHYLAMINO)ETHYL]CARBAMIC ACID, PHENYL ESTER,(L)-2,3-DIHYDROXYBUTANEDIOIC ACID SALT (SDZ ENA 713 HTA), AN INVESTIGATIONAL DRUG FOR THE TREATMENT OF ALZHEIMER'S DISEASE", JOURNAL OF LABELLED COMPOUNDS AND RADIOPHARMACEUTICALS, SUSSEX, GB, vol. 39, no. 8, 1997, pages 651 - 668, XP002269029, ISSN: 0362-4803
DATABASE BEILSTEIN [online] XP002327188, accession no. RID 8695727
DATABASE BEILSTEIN [online] XP002327189, accession no. RID 816415
DATABASE BEILSTEIN [online] XP002327190, accession no. RID 945119
DATABASE BEILSTEIN [online] XP002327191, accession no. RID 771876
DATABASE BEILSTEIN [online] XP002327192, accession no. BRN 3652483
DATABASE BEILSTEIN [online] XP002327193, accession no. BRN 3646129
DATABASE BEILSTEIN [online] XP002327194, accession no. BRN 3644242
DATABASE BEILSTEIN [online] XP002327195, accession no. BRN 3340624
DATABASE BEILSTEIN [online] XP002327196, accession no. BRN 3331553
DATABASE BEILSTEIN [online] XP002327197, accession no. BRN 3283495
DATABASE BEILSTEIN [online] XP002327198, accession no. BRN 3205503
DATABASE BEILSTEIN [online] XP002327199, accession no. BRN 3101218
DATABASE BEILSTEIN [online] XP002327200, accession no. BRN 9449166
DATABASE BEILSTEIN [online] XP002327201, accession no. BRN 9030136
See also references of EP 1697313A2

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