Method of preparation of 1-[(diarylmethoxy)alkyl]-pyrrolidines or piperidines or organic or inorgani
专利摘要:
Use: as substances with antagonistic properties of calcium. The essence of the invention is: 1- (diarylmethoxy) alkyl-pyrrolidines or piperidines of the general formula: CH-O-AIK-rQjHdn XRJ where X is hydrogen or fluorine, Alk is linear or branched Ca-Cz-alkyl, RI and Na is hydrogen or linear or a branched C1 C4 alkoxy radical in any position of the aromatic ring, n 4 or 5; or their organic or inorganic salts. Reagent 1: 1- (diarylmethoxy) 2-bromoalkyl. Reagent 2: arylpyrrolidine or arylpiperidine. Reaction conditions: in the presence of an alkaline agent, such as carbonate or sodium or potassium hydride, in an inert solvent at 60-80 ° C. 1 tab. Yo 公开号:SU1757462A3 申请号:SU894742008 申请日:1989-09-22 公开日:1992-08-23 发明作者:Ферран Жерар;Барбантон Жак;Депэн Жан-Клод;Шавернак Жиль 申请人:Лифа, Лионнэз Эндюстриель Фармасетик (Фирма); IPC主号:
专利说明:
Product examples Perfusion pressure drop + standard error. % 1 4 10 11 13 14 15 Flunarizin 56 ± 6 54 ± 4 59 ± 4 56 ± 5 58 ± 5 54 ± 5 62 ± 5 41 ± 4
权利要求:
Claims (1) [1] Claim The method of obtaining 1 - [(diarylmethoxy) alkyl} -pyrrolidines or piperidines of the General formula X V X where X is hydrogen or fluorine; A1k is a linear or branched Cr ~ C3-alkyl; Щ and Кг - hydrogen or linear, or branched С1 ~ С4-alkoxy-radial in any position of the aromatic nucleus; η ~ 4 or 5, or their organic or inorganic salts of t Leach in that 1 - (diaryl methoxy) -2-bromoalkyl general formula audio 7fn _ z ') n I. where X and Aik have the indicated meanings, are reacted with arylpyrro-. din or arylpiperidine of the general formula Nia (b1 g ) p SU 4 'g 14 where Ri, R 2 and ή have the indicated meanings, in the presence of an alkaline agent, such as sodium or potassium carbonate or hydride, in an inert solvent at 605–80 ° С, followed by isolation of the target product in free form or in the form organic or inorganic salt, 10 ·.· Product by examples Perfusion pressure drop + standard error,% 1 56 ± 6. .··· 4 54 ± 4 10 59 ± 4 eleven 56 ± 5 thirteen 58 ± 5 14 54 + 5 fifteen 62 + 5 Flunarizine 41 + 4
类似技术:
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同族专利:
公开号 | 公开日 JPH02121964A|1990-05-09| AT101132T|1994-02-15| FR2636946A1|1990-03-30| DE68912860D1|1994-03-17| EP0360685A1|1990-03-28| HUT52049A|1990-06-28| DK468389A|1990-03-24| AR246255A1|1994-07-29| AU4169089A|1990-03-29| NO893764L|1990-03-26| AU617530B2|1991-11-28| MA21631A1|1990-04-01| PT91783A|1990-03-30| DE68912860T2|1994-08-11| OA09135A|1991-10-31| YU170189A|1991-02-28| TNSN89103A1|1991-02-04| CZ279282B6|1995-04-12| CZ540989A3|1994-11-16| HU208422B|1993-10-28| IE63648B1|1995-05-31| DK468389D0|1989-09-22| FR2636946B1|1990-11-02| PT91783B|1995-08-09| EP0360685B1|1994-02-02| ZA897212B|1991-03-27| IL91689D0|1990-06-10| NO893764D0|1989-09-22| DD284875A5|1990-11-28| NZ230744A|1991-06-25| ES2062071T3|1994-12-16| IE893050L|1990-03-23| CA1327364C|1994-03-01| US4957927A|1990-09-18|
引用文献:
公开号 | 申请日 | 公开日 | 申请人 | 专利标题 GB1545094A|1976-12-14|1979-05-02|Gist Brocades Nv|Piperazine derivatives|MX9100517A|1990-08-06|1992-04-01|Smith Kline French Lab|COMPOUNDS| MX9100513A|1990-08-06|1992-04-01|Smith Kline French Lab|COMPOUNDS| TW230771B|1990-08-09|1994-09-21|Sankyo Co| GB9113031D0|1991-06-17|1991-08-07|Smithkline Beecham Plc|Compounds| US5578639A|1994-07-01|1996-11-26|Warner-Lambert Company|PLA2 inhibitors and their use for inhibition of intestinal cholesterol absorption| US6153754A|1995-12-21|2000-11-28|Albany Molecular Research, Inc.|Process for production of piperidine derivatives| US6201124B1|1995-12-21|2001-03-13|Albany Molecular Research, Inc.|Process for production of piperidine derivatives| US5747523A|1996-01-24|1998-05-05|Guilford Pharmaceuticals Inc.|Substituted ethyl α,α-diarylmethyl ether derivatives| US6011035A|1998-06-30|2000-01-04|Neuromed Technologies Inc.|Calcium channel blockers| US6946475B1|1999-04-07|2005-09-20|University Of Virginia Patent Foundation|Anticancer calcium channel blockers| WO2000059882A1|1999-04-07|2000-10-12|Gray Lloyd S|Anticancer calcium channel blockers| EP1406624A4|2001-06-13|2005-03-30|Teva Pharma|Process for the preparation of paroxetine substantially free of alkoxy impurities| CN102781316B|2010-03-01|2016-07-06|陶制药有限责任公司|Cancer diagnosis and imaging|
法律状态:
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申请号 | 申请日 | 专利标题 FR8812430A|FR2636946B1|1988-09-23|1988-09-23| ALCOYL) -1 PYRROLIDINES AND PIPERIDINES, METHODS OF PREPARATION AND MEDICAMENTS CONTAINING THEM| 相关专利
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