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1. 发明申请

WO2008034644A3 PROCESS FOR MAKING ANASTROZOLE 审中-公开
标题翻译：制备阿诺方唑的方法
公开(公告)号：WO2008034644A3
公开(公告)日：2008-06-26
申请号：PCT/EP2007008338
申请日：2007-09-20
申请人： SYNTHON BV , BENES MICHAL , PROSEK ZDENEK , HYKL JIRI , PIS JAROSLAV
发明人： BENES MICHAL , PROSEK ZDENEK , HYKL JIRI , PIS JAROSLAV
IPC分类号： C07D249/08 , A61K31/4196 , A61P35/00 , C07C255/36
CPC分类号： C07D249/08 , C07C255/36
摘要： A process for making anastrozole using a 1-substituted triazole can reduce formation of the undesired iso-anastrozole. A typical process is represented by (I), wherein compound (10) is a 1-substituted triazole and compound (1) is anastrozole.
摘要翻译：使用1-取代的三唑制备阿那曲唑的方法可以减少不希望的异阿拉曲唑的形成。典型的方法由（I）表示，其中化合物（10）是1-取代的三唑，化合物（1）是阿那曲唑。

2. 发明专利

GB2398071B Process for making ondansetron and intermediate thereof 未知
公开(公告)号：GB2398071B
公开(公告)日：2006-06-07
申请号：GB0304924
申请日：2003-03-04
申请人： SYNTHON BV
发明人： HESOUN DUSAN , HYKL JIRI
IPC分类号： C07D403/06 , A61P1/08 , A61P25/06 , A61P35/00 , C07D209/82 , C07D209/88 , C07D233/61 , C07D521/00
摘要： Production of 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl)-methyl)-4H-carbazol-4-one (I), by reacting 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one (II), formaldehyde, a secondary amine and 2-methyl-imidazole at elevated temperature in a polar, non-aqueous solvent, is carried out in presence of an acid binding agent. Production of 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl)-methyl)-4H-carbazol-4-one of formula (I) involves reacting 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one (II), formaldehyde (or its precursor), an amine of formula NHR1R2 (III) (or its salt) and 2-methyl-imidazole of formula (V) (or its salt) at elevated temperature in a polar, non-aqueous solvent in presence of an acid binding agent. R1, R2 = 1-4C alkyl; or together complete a 5- or 6-membered ring. An Independent claim is also included for the preparation of a carbazolone intermediate-containing reaction mixture, by contacting (II), formaldehyde (or its precursor) and (III) (or its salt) in a polar, non-aqueous solvent in presence of an acid binding agent.

3. 发明专利

GB2398071A Preparation of ondansetron 未知
公开(公告)号：GB2398071A
公开(公告)日：2004-08-11
申请号：GB0304924
申请日：2003-03-04
申请人： SYNTHON BV
发明人： HESOUN DUSAN , HYKL JIRI
IPC分类号： A61P1/08 , A61P25/06 , A61P35/00 , C07D209/88 , C07D403/06 , C07D521/00
摘要： A process for forming ondansetron involves reacting a carbazolone with formaldehyde or a formaldehyde precursor and an amine, and an imidizole, at elevated temperature in a non-aqueous polar solvent and characterised by presence of a water binding agent. The water binding agent may be acetic anhydride, methane sulphonic acid or phosphorus pentoxide anhydrate. Generally the imidizole is reacted later in a second step. The reaction allows commercial scale of production of ondansetron.

4. 发明专利

NL1022894C2 Proces voor het maken van ondansetron en intermediairen daarvan. 未知
公开(公告)号：NL1022894C2
公开(公告)日：2004-07-28
申请号：NL1022894
申请日：2003-03-11
申请人： SYNTHON BV
发明人： HESOUN DUSAN , HYKL JIRI
IPC分类号： A61P1/08 , A61P25/06 , A61P35/00 , C07D209/88 , C07D403/06 , C07D521/00 , A61K31/4178

5. 发明专利

FR2850381B1 未知
公开(公告)号：FR2850381B1
公开(公告)日：2006-06-09
申请号：FR0304140
申请日：2003-04-03
申请人： SYNTHON BV
发明人： HESOUN DUSAN , HYKL JIRI
IPC分类号： C07D403/06 , A61K31/4155 , A61P1/08 , A61P25/06 , A61P35/00 , C07D209/88 , C07D209/90 , C07D233/58 , C07D521/00
摘要： Production of 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl)-methyl)-4H-carbazol-4-one (I), by reacting 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one (II), formaldehyde, a secondary amine and 2-methyl-imidazole at elevated temperature in a polar, non-aqueous solvent, is carried out in presence of an acid binding agent. Production of 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl)-methyl)-4H-carbazol-4-one of formula (I) involves reacting 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one (II), formaldehyde (or its precursor), an amine of formula NHR1R2 (III) (or its salt) and 2-methyl-imidazole of formula (V) (or its salt) at elevated temperature in a polar, non-aqueous solvent in presence of an acid binding agent. R1, R2 = 1-4C alkyl; or together complete a 5- or 6-membered ring. An Independent claim is also included for the preparation of a carbazolone intermediate-containing reaction mixture, by contacting (II), formaldehyde (or its precursor) and (III) (or its salt) in a polar, non-aqueous solvent in presence of an acid binding agent.

6. 发明专利

NO20053928D0 未知
公开(公告)号：NO20053928D0
公开(公告)日：2005-08-23
申请号：NO20053928
申请日：2005-08-23
申请人： SYNTHON BV
发明人： HESOUN DUSAN , HYKL JIRI
IPC分类号： A61P1/08 , A61P25/06 , A61P35/00 , C07D209/88 , C07D403/06 , C07D521/00 , C07D
摘要： Production of 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl)-methyl)-4H-carbazol-4-one (I), by reacting 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one (II), formaldehyde, a secondary amine and 2-methyl-imidazole at elevated temperature in a polar, non-aqueous solvent, is carried out in presence of an acid binding agent. Production of 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl)-methyl)-4H-carbazol-4-one of formula (I) involves reacting 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one (II), formaldehyde (or its precursor), an amine of formula NHR1R2 (III) (or its salt) and 2-methyl-imidazole of formula (V) (or its salt) at elevated temperature in a polar, non-aqueous solvent in presence of an acid binding agent. R1, R2 = 1-4C alkyl; or together complete a 5- or 6-membered ring. An Independent claim is also included for the preparation of a carbazolone intermediate-containing reaction mixture, by contacting (II), formaldehyde (or its precursor) and (III) (or its salt) in a polar, non-aqueous solvent in presence of an acid binding agent.

7. 发明专利

DE60309511T2 未知
公开(公告)号：DE60309511T2
公开(公告)日：2007-06-28
申请号：DE60309511
申请日：2003-03-14
申请人： SYNTHON BV
发明人： HESOUN DUSAN , HYKL JIRI
IPC分类号： C07D403/06 , A61P1/08 , A61P25/06 , A61P35/00 , C07D209/88 , C07D521/00
摘要： Production of 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl)-methyl)-4H-carbazol-4-one (I), by reacting 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one (II), formaldehyde, a secondary amine and 2-methyl-imidazole at elevated temperature in a polar, non-aqueous solvent, is carried out in presence of an acid binding agent. Production of 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl)-methyl)-4H-carbazol-4-one of formula (I) involves reacting 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one (II), formaldehyde (or its precursor), an amine of formula NHR1R2 (III) (or its salt) and 2-methyl-imidazole of formula (V) (or its salt) at elevated temperature in a polar, non-aqueous solvent in presence of an acid binding agent. R1, R2 = 1-4C alkyl; or together complete a 5- or 6-membered ring. An Independent claim is also included for the preparation of a carbazolone intermediate-containing reaction mixture, by contacting (II), formaldehyde (or its precursor) and (III) (or its salt) in a polar, non-aqueous solvent in presence of an acid binding agent.

8. 发明专利

AT344258T 未知
公开(公告)号：AT344258T
公开(公告)日：2006-11-15
申请号：AT03718688
申请日：2003-03-14
申请人： SYNTHON BV
发明人： HESOUN DUSAN , HYKL JIRI
IPC分类号： A61P1/08 , A61P25/06 , A61P35/00 , C07D209/88 , C07D403/06 , C07D521/00
摘要： Production of 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl)-methyl)-4H-carbazol-4-one (I), by reacting 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one (II), formaldehyde, a secondary amine and 2-methyl-imidazole at elevated temperature in a polar, non-aqueous solvent, is carried out in presence of an acid binding agent. Production of 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl)-methyl)-4H-carbazol-4-one of formula (I) involves reacting 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one (II), formaldehyde (or its precursor), an amine of formula NHR1R2 (III) (or its salt) and 2-methyl-imidazole of formula (V) (or its salt) at elevated temperature in a polar, non-aqueous solvent in presence of an acid binding agent. R1, R2 = 1-4C alkyl; or together complete a 5- or 6-membered ring. An Independent claim is also included for the preparation of a carbazolone intermediate-containing reaction mixture, by contacting (II), formaldehyde (or its precursor) and (III) (or its salt) in a polar, non-aqueous solvent in presence of an acid binding agent.

9. 发明专利

NO20053928A 未知
公开(公告)号：NO20053928A
公开(公告)日：2005-10-24
申请号：NO20053928
申请日：2005-08-23
申请人： SYNTHON BV
发明人： HESOUN DUSAN , HYKL JIRI
IPC分类号： A61P1/08 , A61P25/06 , A61P35/00 , C07D209/88 , C07D403/06 , C07D521/00
CPC分类号： C07D231/12 , C07D209/88 , C07D233/56 , C07D249/08 , C07D403/06

10. 发明专利

AU2003222763A1 PROCESS FOR MAKING ONDANSETRON AND INTERMEDIATES THEREOF 未知
公开(公告)号：AU2003222763A1
公开(公告)日：2004-08-13
申请号：AU2003222763
申请日：2003-03-14
申请人： SYNTHON BV
发明人： HESOUN DUSAN , HYKL JIRI
IPC分类号： A61P1/08 , A61P25/06 , A61P35/00 , C07D209/88 , C07D403/06 , C07D521/00
摘要： Production of 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl)-methyl)-4H-carbazol-4-one (I), by reacting 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one (II), formaldehyde, a secondary amine and 2-methyl-imidazole at elevated temperature in a polar, non-aqueous solvent, is carried out in presence of an acid binding agent. Production of 1,2,3,9-tetrahydro-9-methyl-3-((2-methyl-1H-imidazol-1-yl)-methyl)-4H-carbazol-4-one of formula (I) involves reacting 1,2,3,9-tetrahydro-9-methyl-4H-carbazol-4-one (II), formaldehyde (or its precursor), an amine of formula NHR1R2 (III) (or its salt) and 2-methyl-imidazole of formula (V) (or its salt) at elevated temperature in a polar, non-aqueous solvent in presence of an acid binding agent. R1, R2 = 1-4C alkyl; or together complete a 5- or 6-membered ring. An Independent claim is also included for the preparation of a carbazolone intermediate-containing reaction mixture, by contacting (II), formaldehyde (or its precursor) and (III) (or its salt) in a polar, non-aqueous solvent in presence of an acid binding agent.

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