专利号:US-7563904-B2 优先权日:2002-08-07 标题:Synthesis intermediates useful for preparing zolmitriptan 发明人:DALMASES BARJOAN PERE; ARMENGOL ASPARO MONTSERRAT 权利人:INKE SA 摘要:In particular, this invention relates to the synthesis intermediates (IV), (V), (VI) and (VIII) useful for preparing zolmitriptanzohnitriptan or a pharmaceutically acceptable salt thereof, which includes a) Ppreparation of the diazonium salt of the aniline hydrochloride (II); followed by reduction and acidification to give hydrazine (III); b) In situ Reaction of the hydrazine hydrochloride (III) with α-keto-δ-valerolactone, to give the hydrazone (IV); c) Fischer indole synthesis of the hydrazone (IV), to give the pyranoindolone of formula (V); d) Ttransesterification of the pyranoindolone (V) to provide the compound (VI), in which R means a straight or branched C1-C4 alkyl; e) Conversion of the hydroxyl group of the compound (VI) into dimethylamino to give the indolecarboxylate (VII), in which R means a straight or branched C1-C4 alkyl; f) Ssaponification of the 2-carboalkoxy group of the compound (VII), to provide indolecarboxylic acid (VIII); g) Ddecarboxylation of the indolecarboxylic acid (VIII), to provide zolmitriptan and, eventually, to provide a pharmaceutically acceptable salt thereof.
专利号:US-6160123-A 优先权日:1995-08-07 标 题:One pot synthesis of 2-oxazolidinone derivatives 发明人:PATEL RAJNIKANT 权利人:ZENECA LTD 摘要:The present invention provides an improved process for preparing (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone which comprises: a) forming a carbamate of formula (III), from methyl 4-nitro-(L)-phenylalaninate hydrochloride; b) reducing the compound of formula (III) to give the compound of formula (IV); c) reducing the methyl ester grouping in the compound of formula (IV) to give the compound of formula (V); d) ring closure of the compound of formula (V) to give the compound of formula (VI); e) diazonium salt formation from the compound of formula (VI) followed by reduction to give the compound of formula (VII); f) Fischer reaction of the compound of formula (VIl) to give (S)-4-{[3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone.
专利号:US-6084103-A 优先权日:1995-08-07 标题 :One pot synthesis of 2-oxazolidinone derivatives
专利号:US-2006264643-A1 优先权日:1995-08-07 标 题 :One Pot Synthesis of 2-Oxazolidinone Derivatives
专利号:WO-9706162-A1 优先权日:1995-08-07 标 题:One pot synthesis of 2-oxazolidinone derivatives
专利号:US-2005187274-A1 优先权日:1995-08-07 标题 :One pot synthesis of 2-oxazolidinone derivatives