IT1295309B1 - Preparation of new and known aminocarbonyl geneseroline derivatives - for use as acetylcholinesterase inhibitors - Google Patents

Preparation of new and known aminocarbonyl geneseroline derivatives - for use as acetylcholinesterase inhibitors

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Publication number
IT1295309B1
IT1295309B1 ITMI972299A IT1295309B1 IT 1295309 B1 IT1295309 B1 IT 1295309B1 IT MI972299 A ITMI972299 A IT MI972299A IT 1295309 B1 IT1295309 B1 IT 1295309B1
Authority
IT
Italy
Prior art keywords
geneseroline
preparation
aminocarbonyl
derivatives
new
Prior art date
Application number
Other languages
Italian (it)
Inventor
Paolo Chiesi
Paolo Ventura
Vittorino Servadio
Roberto Pighi
Fausto Pivetti
Bluetta Salsi
Maurizio Delcanale
Original Assignee
Chiesi Farma Spa
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Priority to IT002299 priority Critical patent/IT1295309B1/en
Application filed by Chiesi Farma Spa filed Critical Chiesi Farma Spa
Priority to PCT/EP1998/006377 priority patent/WO1999019329A1/en
Priority to EA200000300A priority patent/EA003192B1/en
Priority to NZ503773A priority patent/NZ503773A/en
Priority to HU0003747A priority patent/HUP0003747A3/en
Priority to CA002274658A priority patent/CA2274658A1/en
Priority to EP98954370A priority patent/EP1023297A1/en
Priority to CN98810683A priority patent/CN1278264A/en
Priority to KR1020007003805A priority patent/KR20010015714A/en
Priority to AU11516/99A priority patent/AU750964B2/en
Priority to IL13539998A priority patent/IL135399A0/en
Priority to PL98339761A priority patent/PL339761A1/en
Priority to SK503-2000A priority patent/SK5032000A3/en
Priority to TR2000/00951T priority patent/TR200000951T2/en
Priority to BR9815237-8A priority patent/BR9815237A/en
Priority to US09/319,693 priority patent/US6297237B1/en
Priority to ARP980105062A priority patent/AR018511A1/en
Priority to ZA989237A priority patent/ZA989237B/en
Priority to TW087117571A priority patent/TW490467B/en
Publication of ITMI972299A1 publication Critical patent/ITMI972299A1/en
Application granted granted Critical
Publication of IT1295309B1 publication Critical patent/IT1295309B1/en

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  • Steroid Compounds (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Abstract

Preparation of aminocarbonyl derivatives of geneseroline (I) comprises oxidation of eserine, followed by hydrolysis to geneseroline, without isolating the intermediate geneserine, followed by acylation of geneseroline with an isocyanate and optional conversion to a salt. - Preparation of aminocarbonyl derivatives of geneseroline of formula (I) comprises: (a) oxidation of eserine with hydrogen peroxide in the presence of a base; (b) hydrolysis of the intermediate geneserine without isolation to give geneseroline; (c) acylation geneseroline with an isocyanate of formula R-N=C=O in the presence of a basic catalyst; and (d) optionally conversion into a salt. R = 2-20C alkyl, 3-7C cycloalkyl, phenyl or benzyl optionally substituted by 1-4C alkyl, halo or 1-4C alkoxy.
IT002299 1997-10-10 1997-10-10 Preparation of new and known aminocarbonyl geneseroline derivatives - for use as acetylcholinesterase inhibitors IT1295309B1 (en)

Priority Applications (19)

Application Number Priority Date Filing Date Title
IT002299 IT1295309B1 (en) 1997-10-10 1997-10-10 Preparation of new and known aminocarbonyl geneseroline derivatives - for use as acetylcholinesterase inhibitors
SK503-2000A SK5032000A3 (en) 1997-10-10 1998-10-07 A process for the preparation of aminocarbonyl derivatives of geneseroline having selective brain anticholinesterase activity, pharmaceutical composition containing the same, use thereof and intermediates
NZ503773A NZ503773A (en) 1997-10-10 1998-10-07 A process for the preparation of aminocarbonyl derivatives of geneseroline having selective brain anticholinesterase activity
HU0003747A HUP0003747A3 (en) 1997-10-10 1998-10-07 A process for the preparation of aminocarbonyl derivatives of geneseroline having selective brain anticholinesterase activity
CA002274658A CA2274658A1 (en) 1997-10-10 1998-10-07 A process for the preparation of aminocarbonyl derivatives of geneseroline having selective brain anticholinesterase activity
EP98954370A EP1023297A1 (en) 1997-10-10 1998-10-07 A process for the preparation of aminocarbonyl derivatives of geneseroline having selective brain anticholinesterase activity
CN98810683A CN1278264A (en) 1997-10-10 1998-10-07 Process for prepn. of aminocarbonyl derivatives of geneseroline having selective brain anticholinesterase activity
KR1020007003805A KR20010015714A (en) 1997-10-10 1998-10-07 A Process for the Preparation of Aminocarbonyl Derivatives of Geneseroline Having Selective Brain Anticholinesterase Activity
PCT/EP1998/006377 WO1999019329A1 (en) 1997-10-10 1998-10-07 A process for the preparation of aminocarbonyl derivatives of geneseroline having selective brain anticholinesterase activity
IL13539998A IL135399A0 (en) 1997-10-10 1998-10-07 A process for the preparation of aminocarbonyl derivatives of geneseroline having selective brain anticholinesterase activity
PL98339761A PL339761A1 (en) 1997-10-10 1998-10-07 Method of obtaining aminocabonylic genezerolin of selective activity against cerebral cholinesterase
EA200000300A EA003192B1 (en) 1997-10-10 1998-10-07 A process for the preparation of aminocarbonyl derivatives of geneseroline having selective brain anticholinesterase activity
TR2000/00951T TR200000951T2 (en) 1997-10-10 1998-10-07 A process for the preparation of aminocarbonyl derivatives of geneserol with selective brain anticholinesterase activity.
BR9815237-8A BR9815237A (en) 1997-10-10 1998-10-07 Process for preparing aminocarbonyl derivatives of geneseroline that have selective anticholinesterase activity in the brain
US09/319,693 US6297237B1 (en) 1997-10-10 1998-10-07 Process for the preparation of aminocarbonyl derivatives of geneseroline having selective brain anticholinesterase activity
AU11516/99A AU750964B2 (en) 1997-10-10 1998-10-07 A process for the preparation of aminocarbonyl derivatives of geneseroline having selective brain anticholinesterase activity
ARP980105062A AR018511A1 (en) 1997-10-10 1998-10-09 PROCESS TO PREPARE AMINOCARBONILE DERIVATIVES OF GENESEROLINE, PHARMACEUTICAL COMPOSITION CONTAINING THEM, INTERMEDIARY COMPOUNDS CONTAINING GENINERARBONYL DERIVATIVES OF GENESEROLINE AND THE USE OF SUCH COMPOUNDS
ZA989237A ZA989237B (en) 1997-10-10 1998-10-09 A process for the preparation of aminocarbonyl derivatives of geneseroline having selective brain anticholinesterase activity
TW087117571A TW490467B (en) 1997-10-10 1998-10-23 A process for the preparation of aminocarbonyl derivatives of geneseroline having selective brain anticholinesterase activity

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
IT002299 IT1295309B1 (en) 1997-10-10 1997-10-10 Preparation of new and known aminocarbonyl geneseroline derivatives - for use as acetylcholinesterase inhibitors

Publications (2)

Publication Number Publication Date
ITMI972299A1 ITMI972299A1 (en) 1999-04-10
IT1295309B1 true IT1295309B1 (en) 1999-05-04

Family

ID=11378023

Family Applications (1)

Application Number Title Priority Date Filing Date
IT002299 IT1295309B1 (en) 1997-10-10 1997-10-10 Preparation of new and known aminocarbonyl geneseroline derivatives - for use as acetylcholinesterase inhibitors

Country Status (2)

Country Link
IT (1) IT1295309B1 (en)
ZA (1) ZA989237B (en)

Also Published As

Publication number Publication date
ZA989237B (en) 1999-04-19
ITMI972299A1 (en) 1999-04-10

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0001 Granted