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121. 发明专利

AU2003206121A8 Preparation of 4-(n, n-disubstitutedamino) butyraldehyde acetals 未知
公开(公告)号：AU2003206121A8
公开(公告)日：2003-12-19
申请号：AU2003206121
申请日：2003-02-03
申请人： NATCO PHARMA LTD
发明人： PULLA REDDY MUDDASANI , VENKAIAH CHOWDARY NANNAPANENI
IPC分类号： C07C213/00 , C07C217/00 , C07C217/40 , C07D295/08

122. 发明专利

CA2487957A1 AN IMPROVED PROCESS FOR THE PREPARATION OF 4-(N, N-DISUBSTITUTEDAMINO) BUTYRALDEHYDE ACETALS 未知
公开(公告)号：CA2487957A1
公开(公告)日：2003-12-11
申请号：CA2487957
申请日：2003-02-03
申请人： NATCO PHARMA LTD
发明人： PULLA REDDY MUDDASANI , VENKAIAH CHOWDARY NANNAPANENI
IPC分类号： C07C213/00 , C07C217/40 , C07D295/088 , C07C217/00
摘要： The invention disclosed in this application relates to an improved process f or the preparation of compounds of formula (I): R1R2NCH2CH2CH2CH(OR3)2; wherein , R1 = R2 = C1-C16 alkyl; C3-C7 cycloalkyl; R1 = C1-C16 alkyl; R2 = C3-C7 cycloalkyl; NR1R2 = pyrrolidino, piperidino, morpholino, thiomorpholino, R1 = C1-C6 alkyl; R2 = ArCH2; Ar =4-R4-C6H4-, R4 = MeO, EtO, Me, Et, NMe2, NEt2, SMe, SEt, etc; R3=C1-C6 alkyl; C3-C7 cycloalkyl which comprises: (i) Reactin g 3-(N, N-disubstitutedamino)propyl halide of formula (XXI): R1R2NCH2CH2CH2X; wherein, R1, R2 = 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(OR5)(OR3)2; wherein, R3 an d R5 is same or different and represent C1 to C6 alkyl, C3 to C7 cycloalkyl OR R3 is as defined above and R5 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 drug s, like sumatriptan, zolmitriptan, and rizatriptan.

123. 发明专利

NO20033743L 未知
公开(公告)号：NO20033743L
公开(公告)日：2003-10-16
申请号：NO20033743
申请日：2003-08-22
申请人： NATCO PHARMA LTD
发明人： PULLA REDDY MUDDASANI , VENKAIAH CHOWDARY NANNAPANENI
IPC分类号： A61K31/343 , A61P25/24 , C07B61/00 , 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.

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