专利号:US-6211382-B1 优先权日:1997-07-25 标题 :Process for the preparation of 1,3-diaza-spiro (4.4) non-1-en-4-one derivatives and 1-cyano-1-acylaminocyclopentane intermediates 发明人:HUSZAR CSABA; KIS-TAMAS ATTILA; NEMETH ATTILA; NAD ZSUZSANNA; MAKOVI ZOLTAN; GAJARY ANTAL; KOLLAR ENDRE; ARANYOSI PETER; GYUERE KAROLY; MESZAROS ISTVAN; HARI ZSUZSANNA CSETRIN; SUPIC ATTILA; ZRINYI ILONA DERVALICSNE; DUBOVSZKI KATALIN; PALIN LAJOSNE; KARASH AGNES; BOGNAR ERZSEBET 权利人:SANOFI SYNTHELABO 摘要:Process for the preparation of compounds of formula (I) wherein R means hydrogen atom, or C1-6 alkyl group, or C7-12 aralkyl group or phenyl group, characterised in that a) the compound of formula (III) is reacted with a compound of formula (IV) wherein X means halogen atom or C1-5 alkoxy group or hydroxyl group, and the resulting compound of formula (II) is transformed, in a reaction medium with pH above 7, into the compound of formula (I) or b) the compound of formula (III) is reacted with an anhydride of general formula (V) and the resulting compound of formula (II) transformed, in a reaction medium with pH above 7, into the compound of formula (I), or c) a compound of formula (II) is transformed, in a reaction medium with pH above 7, into the compound of formula (I), and if desired, the resulting compounds of formula (I), before or after isolation, are transformed into acid addition salts, or the compounds of formula (I) are liberated from their acid addition salts. Thus a process for the preparation of intermediates useful in synthesis of angiotensin II antagonists is disclosed.
专利号:US-6239286-B1 优先权日:1997-07-25 标 题:Process for the preparation of 1,3-diaza-spiro (4.4) non-1-en-4-one derivatives and 1-cyano-1-acylamino-cyclopentane intermediates 发明人:KIS-TAMAS ATTILA; HUSZAR CSABA; CASTRO BERTRAND; NEMETH ATTILA; ARANYOSI PETER; GYUERE KAROLY; MESZAROS ISTVAN; ZRINYI ILONA DERVALICSN; DUBOVSZKI KATALIN; PALI LAJOSNE; GAJARY ANTAL; SUPIC ATTILA; NAD ZSUZSANNA; MAKOVI ZOLTAN; KOLLAR ENDRE; HARI ZSUZSANNA CSETRIN; KARASZA GN; BOGNAR ERZSEBET 权利人:SANOFI SYNTHELABO 摘要:Process for the preparation of compounds of formula (I) wherein R means hydrogen atom, or C1-6 alkyl group, or C7-12 aralkyl group or phenyl group, characterised in that: a) the compound of formula (III) is reacted with a compound of formula (IV) wherein X means halogen atom or C1-5 alkoxy group or hydroxyl group and the resulting compound of formula (II) is transformed in the presence of an oxidising agent in a reaction medium with pH above 7, into the compound of formula (I), or b) the compound of formula (III) is reacted with an anhydride of general formula (V) and the resulting compound of formula (II) transformed in the presence of an oxidising agent, in a reaction medium with pH above 7, into the compound of formula (I), or c) a compound of formula (II) is transformed in the presence of an oxidising agent, in a reaction medium with pH above 7, into the compound of formula (I), and if desired, the resulting compounds of formula (I), before or after isolation, are transformed into acid addition salts, or the compounds of formula (I) are liberated from their acid addition salts. Thus a process for the preparation of intermediates useful in synthesis of angiotensin II antagonists is disclosed.
专利号:CN-102285923-A 优先权日:2011-08-02 标 题 :'One-pot' synthesis of irbesartan intermediate
专利号:US-8129411-B2 优先权日:2005-12-30 标题:Organic compounds 发明人:EHARA TAKERU; GROSCHE PHILIPP; IRIE OSAMU; IWAKI YUKI; KANAZAWA TAKANORI; KAWAKAMI SHIMPEI; KONISHI KAZUHIDE; MOGI MUNETO; SUZUKI MASAKI; YOKOKAWA FUMIAKI 权利人:EHARA TAKERU; GROSCHE PHILIPP; IRIE OSAMU; IWAKI YUKI; KANAZAWA TAKANORI; KAWAKAMI SHIMPEI; KONISHI KAZUHIDE; MOGI MUNETO; SUZUKI MASAKI; YOKOKAWA FUMIAKI; NOVARTIS AG 摘要:The invention relates to 3,5-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-substituted piperidine compound, and/or a method of treatment comprising administering a 3,5-substituted piperidine compound, a method for the manufacture of a 3,5-substituted piperidine compound, and novel intermediates and partial steps for its synthesis. n The compounds have the formula I′ n nwherein R1, R2, T, R3 and R4 are as defined in the specification.
专利号:CN-102050761-A 优先权日:2010-12-10 标 题 :Key intermediate of irbesartan and its synthesis method and method for synthesizing irbesartan from the intermediate