欧盟法规
REACH注册ECHA物质ECHA物质C&L通报REACH预注册专利信息
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-3853946-A
优先权日:1971-11-11
标题 :Process for the preparation of aminomethylene malononitrile
发明人:LEIMGRUBER W; WEIGELE M
权利人:HOFFMANN LA ROCHE
摘要:This invention is directed to a process for the preparation of aminomethylene malononitrile from dialkyl aminoacylonitrile including intermediates therein. Aminomethylene malononitrile is a known compound which is a valuable intermediate in the synthesis of thiamine.
专利号:US-3900511-A
优先权日:1973-03-05
标 题 :Process for the preparation of aminomethylene malononitrile
发明人:LEIMGRUBER WILLY; WEIGELE MANFRED
权利人:HOFFMANN LA ROCHE
摘要:This invention is directed to a process for the preparation of aminomethylene malononitrile from dialkyl aminoacylonitrile including intermediates therein. Aminomethylene malononitrile is a known compound which is a valuable intermediate in the synthesis of thiamine.
专利号:US-3742015-A
优先权日:1968-04-09
标题:Process for the preparation of aminomethylene malononitrile
发明人:LEIMGRUBER W; WEIGELE M
权利人:HOFFMANN LA ROCHE
摘要:This invention is directed to a process for the preparation of aminomethylene malononitrile from dialkyl aminoacrylonitrile including intermediates therein. Aminomethylene malononitrile is a known compound which is a valuable intermediate in the synthesis of thiamine.
专利号:US-3689498-A
优先权日:1970-07-20
标题 :Halide and sulfate salts of 5-amino-isoxazolylmethylene dialkylamine
发明人:LEIMGRUBER WILLY; WEIGELE MANFRED
权利人:HOFFMANN LA ROCHE
摘要:Halide and sulfate salts of 5-amino-4-isoxazolylmethylene dialkylamine and a process for the preparation of these salts. These salts are intermediates for 4-amino-2-methylpyrimidine utilized in the synthesis of thiamine.
专利号:US-3792076-A
优先权日:1972-02-04
标 题:Process for the preparation of 4-amino-2-methylpyridine 5-carboxamide
发明人:LEIMGRUBER W; WEIGELE M
权利人:HOFFMANN LA ROCHE
摘要:THIS INVENTION IS DIRECTED TO A PROCESS FOR THE PREPARATION OF 4-AMINO-2-METHYLPYRIMIDINE 5-CARBOXAMINE FROM 2-CYANO-3-DI(LOWER ALKYL)AMINO ACROLEIN. THE 4-AMINO2-METHYLPYRIMIDINE 5-CARBOXAMIDE IS A KNOWN COMPOUND WHICH IS A VALUABLE INTERMEDIATE IN THE SYNTHESIS OF THIAMINE.