THREE COMPONENT CO-CRYSTAL FORMATION BETWEEN DIASTEREOMERIC MIXTURES OF 3-ALKYL-4-((S)-1'PHENYLETHYLAMINO) BUTANOIC ACID AND OPTICALLY PURE 1, 1'-BI-2-NAPHTHOL

A ternary co-crystal consisting of 1 :0.5:0.5 molar proportion of (S)-1,1'-bi-2-naphthol, 3(S)-propyl-4-[(S)1 '-phenyl-ethylamino]-butanoic acid and 3(R)-propyl-4-[(S)1'- phenyl-ethylamino]-butanoic acid having characteristic powder X-ray diffraction pattern with 2T values of 8.41, 9....

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Hauptverfasser: SINGH, GIRIJ, PAL, LATHI, PIYUSH, SURESH, MITRA, RANGAN, ROY, BHAIRAB, NATH
Format: Patent
Sprache:eng ; fre
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Zusammenfassung:A ternary co-crystal consisting of 1 :0.5:0.5 molar proportion of (S)-1,1'-bi-2-naphthol, 3(S)-propyl-4-[(S)1 '-phenyl-ethylamino]-butanoic acid and 3(R)-propyl-4-[(S)1'- phenyl-ethylamino]-butanoic acid having characteristic powder X-ray diffraction pattern with 2T values of 8.41, 9.38, 10.32, 12.16, 15.52, 15.51, 17.84, 17.95, 19.16, 20.37, 21.74, 22.55, 24.44, 25.65, 28.40, 29.15, 29.69, 31.31, 33.54, 34.40, 35.43 (±0.2) and having differential scanning calorimetric peak at about 189.23 ° C when analyzed at the rate of heating of 10°C per minute and process for preparing the same. A process for resolution of (S)-1,1'-bi-2-naphthol from RS-1,1'-bi-2-naphthol. Cette invention concerne un co-cristal ternaire constitué de (S)-1,1'-bi-2-naphtol, acide 3(S)-propyl-4-[(S)-1'-phényléthylamino]- butanoïque et acide 3(R)-propyl-4-[(S)-1'-phényléthylamino]butanoïque dans un rapport en moles de 1:0,5:0,5, ayant un diagramme de diffraction des rayons X sur poudre caractéristique présentant des valeurs 2? de 8,41, 9,38, 10,32, 12,16, 15,52, 15,51, 17,84, 17,95, 19,16, 20,37, 21,74, 22,55, 24,44, 25,65, 28,40, 29,15, 29,69, 31,31, 33,54, 34,40, 35,43 (±0,2) et un pic en analyse calorimétrique différentielle d'environ 189,23°C quand il est analysé à une vitesse de chauffage de 10°C par minute. Cette invention concerne également un procédé de préparation dudit co-cristal ternaire et un procédé de dédoublement du (S)-1,1'-bi-2-naphtol à partir du RS-1,1'-bi-2-naphtol.