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公开(公告)号:US20070249662A1
公开(公告)日:2007-10-25
申请号:US11737852
申请日:2007-04-20
申请人: Pietro ALLEGRINI , Marcello Rasparini , Gabriele Razzetti , Roberto Rossi , Gianpiero Ventimiglia
发明人: Pietro ALLEGRINI , Marcello Rasparini , Gabriele Razzetti , Roberto Rossi , Gianpiero Ventimiglia
IPC分类号: A61K31/4439 , A61K31/4745 , C07D471/02 , C07D403/02
CPC分类号: C07D471/04 , C07D401/12
摘要: A process for preparation of a compound of formula (I), both as the isomeric mixture and individual isomers, wherein Q is ═CR8— or ═N—; each R1, R2, R3, R4 is independently selected from hydrogen, halogen, hydroxy; nitro; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen or C1-C6 alkoxy; phenyl-C1-C6 alkyl; phenyl-C1-C6 alkoxy; and —N(RaRb) wherein each Ra and Rb is independently hydrogen or C1-C6 alkyl or Ra and Rb, taken together with the nitrogen atom they are linked to, form a saturated heterocyclic ring; andeach R5, R6, R7, R8 is independently selected from hydrogen, halogen, hydroxy; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen; C1-C6 alkyl-carbonyl, C1-C6 alkoxy-carbonyl, and oxazol-2-yl; comprising converting a compound of formula (IV), to said compound of formula (I), in the presence of a catalyst, if necessary in an organic solvent.
摘要翻译: 制备式(I)化合物的方法,均为异构体混合物和各异构体,其中Q为-CR 8 - 或-N-; 每个R 1,R 2,R 3,R 4,R 4独立地选自氢,卤素,羟基; 硝基 任选被羟基取代的C 1 -C 6烷基; 烷硫基C 1 -C 6烷基; 任选被卤素或C 1 -C 6烷氧基取代的C 1 -C 6烷氧基; 苯基-C 1 -C 6烷基; 苯基-C 1 -C 6烷氧基; 和-N(RaRb),其中每个R a和R b独立地是氢或C 1 -C 6烷基或R a和R b与它们所连接的氮原子一起 形成饱和杂环; 并且每个R 5,R 6,R 7,R 8和R 8独立地选自氢,卤素,羟基 ; 任选被羟基取代的C 1 -C 6烷基; 烷硫基C 1 -C 6烷基; 任选被卤素取代的C 1 -C 6烷氧基; C 1 -C 6烷基 - 羰基,C 1 -C 6烷氧基 - 羰基和恶唑-2(C 1 -C 6) - 基; 包括在催化剂存在下,如果需要在有机溶剂中将式(Ⅳ)化合物转化为所述式(Ⅳ)化合物。
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公开(公告)号:US07605268B2
公开(公告)日:2009-10-20
申请号:US11737852
申请日:2007-04-20
申请人: Pietro Allegrini , Marcello Rasparini , Gabriele Razzetti , Roberto Rossi , Gianpiero Ventimigla
发明人: Pietro Allegrini , Marcello Rasparini , Gabriele Razzetti , Roberto Rossi , Gianpiero Ventimigla
IPC分类号: C07D401/12
CPC分类号: C07D471/04 , C07D401/12
摘要: A process for preparation of a compound of formula (I), both as the isomeric mixture and individual isomers, wherein Q is ═CR8— or ═N—; each R1, R2, R3, R4 is independently selected from hydrogen, halogen, hydroxy; nitro; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen or C1-C6 alkoxy; phenyl-C1-C6 alkyl; phenyl-C1-C6 alkoxy; and —N(RaRb) wherein each Ra and Rb is independently hydrogen or C1-C6 alkyl or Ra and Rb, taken together with the nitrogen atom they are linked to, form a saturated heterocyclic ring; and each R5, R6, R7, R8 is independently selected from hydrogen, halogen, hydroxy; C1-C6 alkyl optionally substituted with hydroxy; alkylthio C1-C6; C1-C6 alkoxy optionally substituted with halogen; C1-C6 alkyl-carbonyl, C1-C6 alkoxy-carbonyl, and oxazol-2-yl; comprising converting a compound of formula (IV), to said compound of formula (I), in the presence of a catalyst, if necessary in an organic solvent.
摘要翻译: 制备式(I)化合物的方法,均为异构体混合物和各异构体,其中Q为-CR8-或-N-; 每个R 1,R 2,R 3,R 4独立地选自氢,卤素,羟基; 硝基 任选被羟基取代的C 1 -C 6烷基; 烷硫基C1-C6; 任选被卤素或C 1 -C 6烷氧基取代的C 1 -C 6烷氧基; 苯基-C 1 -C 6烷基; 苯基-C 1 -C 6烷氧基; 和-N(RaRb),其中每个R a和R b独立地是氢或C 1 -C 6烷基或R a和R b与它们连接的氮原子一起形成饱和杂环; 并且每个R 5,R 6,R 7,R 8独立地选自氢,卤素,羟基; 任选被羟基取代的C 1 -C 6烷基; 烷硫基C1-C6; 任选被卤素取代的C 1 -C 6烷氧基; C 1 -C 6烷基 - 羰基,C 1 -C 6烷氧羰基和恶唑-2-基; 包括在催化剂存在下,如果需要在有机溶剂中将式(Ⅳ)化合物转化为所述式(Ⅳ)化合物。
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3.
公开(公告)号:US20070093540A1
公开(公告)日:2007-04-26
申请号:US11551094
申请日:2006-10-19
申请人: Pietro ALLEGRINI , Gabriele Razzetti , Roberto Rossi , Vittorio Lucchini , Simone Mantegazza , Marcello Rasparini
发明人: Pietro ALLEGRINI , Gabriele Razzetti , Roberto Rossi , Vittorio Lucchini , Simone Mantegazza , Marcello Rasparini
IPC分类号: A61K31/4184 , C07D403/02
CPC分类号: C07D403/10 , C07D257/04
摘要: A process for the preparation of angiotensin II antagonists and novel intermediates useful for the synthesis thereof.
摘要翻译: 用于制备血管紧张素II拮抗剂的方法和用于其合成的新中间体。
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公开(公告)号:US07692027B2
公开(公告)日:2010-04-06
申请号:US11415429
申请日:2006-05-02
IPC分类号: C07D403/04
CPC分类号: C07D235/20
摘要: A process for the preparation of telmisartan (I) and novel intermediates useful for its synthesis.
摘要翻译: 一种制备替米沙坦(I)的方法和用于其合成的新型中间体。
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公开(公告)号:US20060264644A1
公开(公告)日:2006-11-23
申请号:US11415429
申请日:2006-05-02
IPC分类号: C07D403/02
CPC分类号: C07D235/20
摘要: A process for the preparation of telmisartan (I) and novel intermediates useful for its synthesis.
摘要翻译: 一种制备替米沙坦(I)的方法和用于其合成的新型中间体。
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6.
公开(公告)号:US07790891B2
公开(公告)日:2010-09-07
申请号:US11927009
申请日:2007-10-29
申请人: Pietro Allegrini , Marcello Rasparini , Gabriele Razzetti , Simone Mantegazza , Vittorio Lucchini , Alberto Bologna
发明人: Pietro Allegrini , Marcello Rasparini , Gabriele Razzetti , Simone Mantegazza , Vittorio Lucchini , Alberto Bologna
IPC分类号: C07D471/02 , C07D401/12
CPC分类号: C07D401/12 , C07D471/04
摘要: A process for the preparation of a compound of formula (I), or a salt thereof, wherein Q is ═CR8— or ═N—; and R1-R8 are as herein defined; comprising the reaction of a compound of formula (II), or a salt thereof, wherein Q, R1-R7 are as herein defined; with a reducing agent selected from a trivalent phosphorous compound, an oxidizable solvent and a sulfonic acid chloride; and, if desired, the conversion of a compound of formula (I) to another compound of formula (I) or a salt thereof.
摘要翻译: 一种制备式(I)化合物或其盐的方法,其中Q为= CR8-或= N-; 和R 1 -R 8如本文所定义; 包括式(II)化合物或其盐的反应,其中Q,R 1 -R 7如本文所定义; 与选自三价磷化合物,可氧化溶剂和磺酰氯的还原剂反应; 如果需要,式(I)化合物转化为另一种式(I)化合物或其盐。
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公开(公告)号:US07385062B2
公开(公告)日:2008-06-10
申请号:US10567492
申请日:2004-07-30
申请人: Graziano Castaldi , Pietro Allegrini , Gabriele Razzetti , Alberto Bologna , Marcello Rasparini , Vittorio Lucchini
发明人: Graziano Castaldi , Pietro Allegrini , Gabriele Razzetti , Alberto Bologna , Marcello Rasparini , Vittorio Lucchini
IPC分类号: C07D257/04
CPC分类号: C07D257/04 , C07F3/02
摘要: A process for the preparation of phenyltetrazole derivatives of formula (II) wherein R and Y are as defined in the disclosure, by direct ortho-metallation of (tetrazol-5-γl)benzene. The compounds of formula (II) are useful intermediates for the preparation of angiotensin II antagonists.
摘要翻译: 制备式(II)的苯基四唑衍生物的方法,其中R和Y如本公开所定义,通过(四唑-5-基)苯的直接邻金属化。 式(II)化合物是制备血管紧张素II拮抗剂的有用的中间体。
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公开(公告)号:US20060183916A1
公开(公告)日:2006-08-17
申请号:US10567492
申请日:2004-07-30
申请人: Graziano Castaldi , Pietro Allegrini , Gabriele Razzetti , Alberto Bologna , Marcello Rasparini , Vittorio Lucchini
发明人: Graziano Castaldi , Pietro Allegrini , Gabriele Razzetti , Alberto Bologna , Marcello Rasparini , Vittorio Lucchini
IPC分类号: C07D403/02
CPC分类号: C07D257/04 , C07F3/02
摘要: A process for the preparation of phenyltetrazole derivatives of formula (II) wherein R and Y are as defined in the disclosure, by direct ortho-metallation of (tetrazol-5-γl)benzene. The compounds of formula (II) are useful intermediates for the preparation of angiotensin II antagonists.
摘要翻译: 制备式(II)的苯基四唑衍生物的方法,其中R和Y如本公开所定义,通过(四唑-5-基)苯的直接邻金属化。 式(II)化合物是制备血管紧张素II拮抗剂的有用的中间体。
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公开(公告)号:US08912327B2
公开(公告)日:2014-12-16
申请号:US14114781
申请日:2012-05-04
IPC分类号: C07D471/04 , C07D487/04 , C07D263/26 , C07C67/30 , C07C263/12 , C07C269/02 , C07C269/06 , C07C69/65 , C07C69/612
CPC分类号: C07D487/04 , C07C67/30 , C07C69/612 , C07C69/65 , C07C263/12 , C07C269/02 , C07C269/06 , C07D263/26 , C07C265/08 , C07C271/22
摘要: A novel process is described for the synthesis of Sitagliptin, IUPAC name 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1 2,4-triazolo[4,3-a]pyrazine, of formula (I).
摘要翻译: 描述了用于合成西他列汀的新方法,IUPAC名称7 - [(3R)-3-氨基-1-氧代-4-(2,4,5-三氟苯基)丁基] -5,6,7,8-六氢 - 四氢-3-(三氟甲基)-1,4-三唑并[4,3-a]吡嗪。
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公开(公告)号:US20140213821A1
公开(公告)日:2014-07-31
申请号:US14131973
申请日:2012-07-25
IPC分类号: C07C231/02 , C07C231/12
CPC分类号: C07C231/02 , C07C231/12 , C07C231/14 , C07C237/22
摘要: It is described a process for the opening of lactone or lactam rings useful in the synthesis of pharmaceutically active compounds and the intermediates thereof, particularly Aliskiren. It has found that by selecting a type of solvent it is possible to obtain excellent yields and high optical and chemical purity of the isolated products.
摘要翻译: 描述了用于合成药物活性化合物及其中间体,特别是阿利克仑的内酯或内酰胺环的开放方法。 已经发现,通过选择一种溶剂,可以获得优异的产率和高分离产物的光学和化学纯度。
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