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51. 发明申请

WO2004080945A1 PROCESS FOR THE PREPARATION OF N-METHYL-1-NAPHTHALENEMETHANAMINE 审中-公开
标题翻译：制备N-甲基-1-萘磺酰胺的方法
公开(公告)号：WO2004080945A1
公开(公告)日：2004-09-23
申请号：PCT/IN2004/000051
申请日：2004-03-01
申请人： NATCO PHARMA LIMITED , PULLA REDDY, Muddasani , RAJASHEKHARA REDDY, Peddi , RADHARANI, Kagitha , VENKAIAH CHOWDARY, Nannapaneni
发明人： PULLA REDDY, Muddasani , RAJASHEKHARA REDDY, Peddi , RADHARANI, Kagitha , VENKAIAH CHOWDARY, Nannapaneni
IPC分类号： C07C231/12
CPC分类号： C07C211/30 , C07C209/08 , C07C233/03
摘要： The present invention discloses an improved and impurity-free process for the preparation of N-methyl-1-naphthalenemethanamine of formula (I) starting from 1-chloromethylnaphthalene of formula (III). N-methylformamide is reacted with a strong base in N,N-dimethylformamide and/or non-polar solvent to get its anion and this anion is reacted with 1-chloromethylnaphthalene to get the formamide derivative of formula (VI). Alternatively, N-methylformamide (without generating the anion separately) and 1-chloromethylnaphthalene can be reacted together in the presence of a mild base and a phase transfer catalyst in N,N-dimethylformamide and/or a non-polar solvent to get the required formamide of formula (VI). The compound of formula (VI) on acid or base hydrolysis gave the required compound of formula (I). The main advantages of the present invention are it involves simple, economical, and easy to adopt process on a commercial scale. No tertiary-amine impurity is formed in this process. Compound of formula (I) is a key intermediate used in the synthesis of anti-fungal drug, terbinafine of formula (II).
摘要翻译：本发明公开了一种从式（III）的1-氯甲基萘开始制备式（I）的N-甲基-1-萘甲胺的改进和无杂质的方法。 N-甲基甲酰胺与N，N-二甲基甲酰胺和/或非极性溶剂中的强碱反应得到其阴离子，该阴离子与1-氯甲基萘反应得到式（VI）的甲酰胺衍生物。或者，在温和的碱和相转移催化剂存在下，在N，N-二甲基甲酰胺和/或非极性溶剂中，N-甲基甲酰胺（不分别生成阴离子）和1-氯甲基萘可一起反应，得到所需的式（VI）的甲酰胺。在酸或碱水解上，式（Ⅵ）化合物得到所需的式（I）化合物。本发明的主要优点是在商业规模上涉及简单，经济，易于采用的方法。在该方法中不形成叔胺杂质。式（I）化合物是用于合成抗真菌药物，式（II）特比萘芬的关键中间体。

52. 发明申请

WO2003104180A1 PROCESS FOR THE PREPARATION OF 4-(4-FLUOROBENZOYL) BUTYRIC ACID 审中-公开
标题翻译：制备4-（4-氟代苯甲酰基）丁酸的方法
公开(公告)号：WO2003104180A1
公开(公告)日：2003-12-18
申请号：PCT/IN2003/000159
申请日：2003-04-16
申请人： NATCO PHARMA LIMITED , VENKAIAH CHOWDARY NANNAPANENI , PULLA REDDY, Muddasani
发明人： PULLA REDDY, Muddasani
IPC分类号： C07C51/347
CPC分类号： C07C51/083 , C07C59/88
摘要： The present invention provides an improved process for the preparation of 4-(4-Fluorobenzoyl)butyric acid of formula (I), which is prepared on a commercial scale using normal quality fluorobenzene (benzene content 300-700ppm) with the desfluoro analogue impurity at an acceptable level (less than 0.1 % by HPLC). The 4-(4-fluorobenzoyl)butyric acid has the formula (I) is a key raw material for the synthesis of anti-hyperlipoproteinemetic drug ezetimibe.
摘要翻译：本发明提供了制备式（I）的4-（4-氟苯甲酰基）丁酸的改进方法，其用商业规模使用正常质量的氟苯（苯含量为300-700ppm）与脱氟类似物杂质制备可接受水平（HPLC低于0.1％）。 4-（4-氟苯甲酰基）丁酸具有式（I）是合成抗高脂蛋白药物依泽替米贝的关键原料。

53. 发明申请

WO03101931A2 AN IMPROVED PROCESS FOR THE PREPARATION OF 4-(N, N-DISUBSTITUTEDAMINO) BUTYRALDEHYDE ACETALS 审中-公开
标题翻译：制备4-（N，N-二异丁基氨基）丁基]乙炔的改进方法
公开(公告)号：WO03101931A2
公开(公告)日：2003-12-11
申请号：PCT/IN0300016
申请日：2003-02-03
申请人： NATCO PHARMA LTD , PULLA REDDY MUDDASANI , VENKAIAH CHOWDARY NANNAPANENI
发明人： PULLA REDDY MUDDASANI , VENKAIAH CHOWDARY NANNAPANENI
IPC分类号： C07C213/00 , C07C217/40 , C07D295/088 , C07C217/00
CPC分类号： C07D295/088 , C07C213/00 , C07C217/40
摘要： The invention disclosed in this application relates to an improved process for the preparation of compounds of formula (I): R R NCH2CH2CH2CH(OR )2; wherein, R = R = C1-C16 alkyl; C3-C7 cycloalkyl; R = C1-C16 alkyl; R = C3-C7 cycloalkyl; NR R = pyrrolidino, piperidino, morpholino, thiomorpholino, R = C1-C6 alkyl; R = ArCH2; Ar =4-R -C6H4-, R = MeO, EtO, Me, Et, NMe2, NEt2, SMe, SEt, etc; R =C1-C6 alkyl; C3-C7 cycloalkyl which comprises: (i) Reacting 3-(N, N-disubstitutedamino)propyl halide of formula (XXI): R R NCH2CH2CH2X; wherein, R , R = as defined above, X = C1 or Br, with magnesium in the presence of a solvent to get the Grrgnard reagent 3-(N, N-disubstitutedamino)-propylmagnesium halide; (ii) Reacting the resulting 3-(N, N-disubstitutedamino) propylmagnesium halide (Grignard reagent) with the trisubstituted orthoformate of formula (XVII): HC(OR )(OR )2; wherein, R and R is same or different and represent C1 to C6 alkyl, C3 to C7 cycloalkyl OR R is as defined above and R represents phenyl radical; (iii) Filtering off the resultant reaction mixture and distilling the filtrate to isolate the compound of the formula (I). These substituted butyraldehyde derivatives of the formula (I) are very important building blocks for the synthesis of various tryptamine derivatives. In particular 4-(N, N-dimethylamino)butyraldehyde dimethyl or diethyl acetals are crucial intermediates for the synthesis of commercially available anti-migraine drugs, like sumatriptan, zolmitriptan, and rizatriptan.
摘要翻译：本申请中公开的本发明涉及制备式（I）化合物的改进方法：R 1 R 2 NCH 2 CH 2 CH 2 CH（OR 3）2; 其中R 1 = R 2 = C 1 -C 16烷基; C3-C7环烷基; R 1 = C 1 -C 16烷基; R 2 = C 3 -C 7环烷基; NR 1 R 2 =吡咯烷子基，哌啶子基，吗啉代，硫代吗啉代，R 1 = C 1 -C 6烷基; R 2 = ArCH2; Ar = 4-R 4 -C 6 H 4 - ，R 4 = MeO，EtO，Me，Et，NMe 2，NEt 2，SMe，SEt等; R 3 = C 1 -C 6烷基; C 3 -C 7环烷基，其包含：（i）反应式（XXI）的3-（N，N-二取代氨基）丙基卤：R 1 R 2 NCH 2 CH 2 CH 2 X; 其中R 1，R 2 =如上定义，X = C 1或Br，与镁在溶剂存在下反应，得到Grrgnard试剂3-（N，N-二取代氨基） - 丙基卤化镁; （ii）将所得3-（N，N-二取代氨基）丙基卤化镁（格氏试剂）与式（XVII）的三取代原甲酸酯反应：HC（OR 5）（OR 3））2; 其中R 3和R 5相同或不同，表示C1至C6烷基，C3至C7环烷基OR R3如上定义，R 5表示苯基; （iii）过滤所得反应混合物并蒸馏滤液以分离式（I）化合物。这些式（I）的取代的丁醛衍生物是合成各种色胺衍生物的非常重要的构件。特别是4-（N，N-二甲基氨基）丁醛二甲基或二乙基缩醛是合成市售的抗偏头痛药物的重要中间体，如舒马曲坦，佐米曲坦和利扎曲坦。

54. 发明申请

WO2002066453A1 PROCESS FOR THE PREPARATION OF CITALOPRAM 审中-公开
标题翻译：制备CITALOPRAM的方法
公开(公告)号：WO2002066453A1
公开(公告)日：2002-08-29
申请号：PCT/IN2002/000023
申请日：2002-02-11
申请人： NATCO PHARMA LIMITED , PULLA, Reddy, Muddasani , VENKAIAH, Chowdary, Nannapaneni
发明人： PULLA, Reddy, Muddasani , VENKAIAH, Chowdary, Nannapaneni
IPC分类号： C07D307/87
CPC分类号： C07D307/87
摘要： This invention discloses an improved process for the preparation of citalopram of the formula III which comprises (i) preparing the compound of the formula VIII by reducing an unisolable magnesium salt of a benzophenone derivative of the formula V using sodium borohydride in the presence of a protic solvent, (ii) reacting the compound of the formula VIII obtained in step (i) with an acid catalyst in a non-polar solvent to obtain a compound of the formula I, (iii) reacting the compound of the formula I obtained in step (ii) with copper (I) cyanide in a polar solvent medium and isolating the resulting cyano compound, by recrystallization by using polar and/or alcoholic solvents to obtain the compound of the formula II and (III) reacting the resulting compound of the formula II by conventional methods to form citalopram of the formula III. Citalopram is widely used as an antidepressant.
摘要翻译：本发明公开了一种制备式III西酞普兰的改进方法，其包括（i）通过在质子存在下使用硼氢化钠还原式V的二苯甲酮衍生物的单不溶性镁盐来制备式VIII化合物溶剂，（ⅱ）使步骤（ⅰ）中获得的式Ⅷ的化合物与酸催化剂在非极性溶剂中反应，得到式Ⅰ化合物，（ⅲ）使步骤（ii）在极性溶剂介质中加入氰化铜（I），并通过使用极性和/或醇溶剂重结晶分离得到的氰基化合物，得到式II和（III）的化合物，使所得式 II通过常规方法形成式III的西酞普兰。西酞普兰被广泛用作抗抑郁药。

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