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CRYSTALS OF 6,7-UNSATURATED-7-CARBAMOYL MORPHINANE DERIVATIVE, AND METHOD FOR PRODUCING SAME
专利权人:
LTD.;SIONOGI END KO.
发明人:
TAMURA Josinori (JP),ТАМУРА Йосинори (JP),NOGUTI Kouiti (JP),НОГУТИ Коуити (JP),INAGAKI Masanao (JP),ИНАГАКИ Масанао (JP),MORIMOTO Kendzi (JP),МОРИМОТО Кендзи (JP),KHAGA Nobukhiro (JP),ХАГА Нобухиро (,TAMURA Josinori,ТАМУРА Йосинори,NOGUTI Kouiti,НОГУТИ Коуити,INAGAKI Masanao,ИНАГАКИ Масанао,MORIMOTO Kendzi,МОРИМОТО Кендзи,KHAGA Nobukhiro,ХАГА Нобухиро,ODA Siniti,ОДА Синити,OMURA Sokhei,ОМУРА Сохеи
申请号:
RU2013126801
公开号:
RU0002607084C2
申请日:
2011.11.11
申请国别(地区):
RU
年份:
2017
代理人:
摘要:
FIELD: chemistry.SUBSTANCE: invention relates to salts of p-toluenesulphonic acid compound of formula (IA) or hydrate thereof, including crystalline forms thereof. Invention relates to form I of crystals of hydrate of salt of p-toluenesulphonic acid compound of formula (IA), where X-ray diffraction spectrum of powder of crystalline has peaks, corresponding to diffraction angles (2θ): 12.9°±0.2°, 17.6°±0.2°, 22.4°±0.2°, 25.4°±0.2° and 28.7°±0.2°. Invention also relates to form II of crystals of hydrate of salt of p-toluenesulphonic acid compound of formula (IA), where X-ray diffraction spectrum of powder of crystalline has peaks, corresponding to diffraction angles (2θ): 8.8°±0.2°, 17.5°±0.2°, 21.9°±0.2°, 23.7°±0.2° and 26.1°±0.2°. Crystalline forms of salts of p-toluenesulphonic acid compound of formula (IA) and hydrates thereof are intended for preparing a pharmaceutical composition, exhibiting agonistic activity with respect to opioid receptor. Crystalline form of salt of p-toluenesulphonic acid compound of formula (IA) or crystalline forms of hydrate of said salt of p-toluenesulphonic acid is obtained by adding p-toluenesulphonic acid to a compound of formula (IA) and crystallisation of salt of p-toluenesulphonic acid or hydrate thereof in a solvent. Method of producing crystalline form or crystalline form of hydrates of said salt of p-toluenesulphonic acid of formula (IA) can also be performed in following steps: 1) treating with a base compound of formula (IIE), where R1a is hydrogen or protecting hydroxyl group, which can be removed by a base selected from a group, consisting of acetyl, formyl, benzoyl, chloroacetyl, pivaloyl, methyl carbonate, isobutyl carbonate, benzyl carbonate, vinyl carbonate, phenyl carbamate, mesyl and tosyl, 2) adding p-toluenesulphonic acid and 3) crystallisation of salt of p-toluenesulphonic acid in a solvent.EFFECT: technical result is stable form of 6,7-unsaturated-7-carbamoyl morphinane.14 cl, 19 tbl, 26 ex,Изобретение относится к
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