Global Patent Index - EP 0950044 A1

EP 0950044 A1 19991020 - PREPARATION OF GABAPENTIN

Title (en)

PREPARATION OF GABAPENTIN

Title (de)

HERSTELLUNG VON GABAPENTIN

Title (fr)

PREPARATION DE GABAPENTINE

Publication

EP 0950044 A1 19991020 (EN)

Application

EP 97954134 A 19971224

Priority

  • IL 11989096 A 19961224
  • US 9723164 W 19971224

Abstract (en)

[origin: WO9828255A1] There is disclosed a method of converting gabapenting hydrochloride substantially free of inorganic salts to gabapenting form II. The method comprises the steps of: (1) obtaining gabapentin hydrochloride that is substantially free of inorganic salts; (2) mixing a solution of the gabapenting hydrochloride with an additional amine in a first solvent so as to obtain a precipitate comprising gabapenting; and then (3) recovering gabapentin form II from the precipitate. The precipitated gabapentin is a novel polymorphic form of gabapentin possessing a crystalline structure characterized by novel sets of peaks in the powder X-ray diffraction pattern and in the FTIR spectra. This newly disclosed polymorph of gabapentin is characterized herein as gabapentin form III. The recovery step may comprise, for example, one of two alternative methods, slurrying the gabapentin form II in methanol, and then filtering the suspension to obtain gabapentin form II, or solubilizing the gabapentin form III in methanol with heating by reflux, and then cooling the solution to obtain gabapentin form II by crystallization.

IPC 1-7

C07C 61/06

IPC 8 full level

C07C 227/42 (2006.01); C07C 229/28 (2006.01)

CPC (source: EP)

C07C 227/42 (2013.01); C07C 229/28 (2013.01); C07C 2601/14 (2017.04)

Designated contracting state (EPC)

AT BE CH DE DK ES FI FR GB GR IE IT LI LU MC NL PT SE

DOCDB simple family (publication)

WO 9828255 A1 19980702; AU 5799098 A 19980717; CA 2275912 A1 19980702; DE 97954134 T1 20040415; EP 0950044 A1 19991020; EP 0950044 A4 20030326; ES 2204362 T1 20040501; IL 119890 A0 19970318; IL 119890 A 20020310

DOCDB simple family (application)

US 9723164 W 19971224; AU 5799098 A 19971224; CA 2275912 A 19971224; DE 97954134 T 19971224; EP 97954134 A 19971224; ES 97954134 T 19971224; IL 11989096 A 19961224