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1. 发明申请

WO0138302A3 COUPLING CONDENSATION SYNTHESIS OF HETEROCYCLES 审中-公开
标题翻译：杂环离合器凝汽合成
公开(公告)号：WO0138302A3
公开(公告)日：2002-03-14
申请号：PCT/EP0011600
申请日：2000-11-21
申请人： MORPHOCHEM AG , MUELLER THOMAS , ANSORGE MARKUS
发明人： MUELLER THOMAS , ANSORGE MARKUS
IPC分类号： A61P31/04 , A61P31/10 , C07D231/06 , C07D417/12 , C07D417/14 , C07D471/04 , A61K31/415 , A61K31/435 , A61K31/44 , A61K31/55 , A61K33/00
CPC分类号： C07D231/06 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The invention relates to a method for producing heterocycles, characterised in that the following components are reacted, preferably in a one-pot reaction by cyclocondensation, to obtain a 4- to 10-, preferably 5- to 7-membered, heterocyclic aromatic or non-aromatic ring system: i) a propargyl derivative of general structural formula (I), Het being an optionally substituted hetero atom and A being a substituted or unsubstituted aromatic, a substituted or unsubstituted aromatic heterocycle, a substituted or unsubstituted vinyl arene and/or a derivative thereof, an olefin, an alkin, an acceptor group or a nitrile; (ii) a compound of general structural formula (II), wherein B is an electron-deficient substituted or unsubstituted aromatic with or without an acceptor group, an electron-deficient substituted or unsubstituted heteroaromatic with or without an acceptor group, an electron-deficient olefin and/or alkin, a metal complex; and X is a leaving group; (iii) a nucleophile of general structural formula (III), wherein Y and/or Z, independently of each other are an amino group, a thio group (mercapto group), a seleno group, a telluro group, a hydroxy group (alcohol group), an imido group, a carbonyl group, a thiocarbonyl group, a selenocarbonyl group, a tellurocarbonyl group; C is a substituted or unsubstituted C atom, a substituted or unsubstituted or anellated CC double bond or simple bond and n = 0-10, preferably 1-5.
摘要翻译：本发明涉及一种用于杂环的制备方法，其特征在于以下组分：i）的通用结构式（Ⅰ），其中Het是任选取代的杂原子，A是取代或未取代的芳族的，取代或未取代的芳族杂环炔丙基衍生物是取代的或未取代的乙烯基芳烃和/或其衍生物，烯烃，炔烃，受体基团或腈; （ii）具有结构通式的化合物（II）其中B是缺电子取代或未取代的芳族的，具有或不具有受体基团，缺电子取代或未取代的杂芳族，具有或不具有受体基团，缺电子烯烃和/或炔烃，金属络合物，且X是是离去基团; （iii）具有结构通式（III），其中Y和/或Z分别独立地表示氨基，硫基（巯基），硒基，Tellurogruppe，羟基（醇基团），酰亚氨基，羰基，硫代羰基，Selenocarbonylgruppe，Tellurocarbonylgruppe亲核试剂; C是一个取代的或未取代的C原子，取代或未取代的或稠合的C = C双键或单键，且n = 0-10，优选1-5，最好是在由环化缩合一锅反应，以4〜10，优选5 - 至7元杂环，是反应的芳族或非芳族环系统。

2. 发明专利

AT263148T 未知
公开(公告)号：AT263148T
公开(公告)日：2004-04-15
申请号：AT00987278
申请日：2000-11-21
申请人： MORPHOCHEM AG
发明人： MUELLER THOMAS , ANSORGE MARKUS
IPC分类号： A61P31/04 , A61P31/10 , C07D201/00 , C07D231/06 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The invention relates to a process for the preparation of heterocycles, characterised in that the following components:i) a propargyl derivative of the general structural formula Ia wherein Het is an optionally substituted hetero atom and A is a substituted or unsubstituted aromatic entity, a substituted or unsubstituted aromatic heterocycle, a substituted or unsubstituted vinyl arene and/or a derivative thereof, an olefin, an alkyne, an acceptor group or a nitrile;(ii) a compound of the general structural formula II,wherein B is an electron-deficient substituted or unsubstituted aromatic entity with or without an acceptor group, an electron-deficient substituted or unsubstituted heteroaromatic entity with or without an acceptor group, an electron-deficient olefin and/or alkyne, a metal complex, and X is a leaving group;(iii) a nucleophile of the general structural formula III,wherein Y and/or Z, each independently of the other, is an amino group, thio group (mercapto group), seleno group, telluro group, hydroxy group (alcohol group), imido group, carbonyl group, thiocarbonyl group, selenocarbonyl group, tellurocarbonyl group; C is a substituted or unsubstituted C atom, a substituted or unsubstituted or annelated CC double bond or single bond and n=0-10, preferably 1-5, preferably are reacted in a one-pot reaction by cyclocondensation to form 4- to 10-membered, preferably 5- to 7-membered, heterocyclic, aromatic or non-aromatic ring systems.

3. 发明专利

DE50005935D1 未知
公开(公告)号：DE50005935D1
公开(公告)日：2004-05-06
申请号：DE50005935
申请日：2000-11-21
申请人： MORPHOCHEM AG
发明人： MUELLER THOMAS , ANSORGE MARKUS
IPC分类号： A61P31/04 , A61P31/10 , C07D201/00 , C07D231/06 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The invention relates to a process for the preparation of heterocycles, characterised in that the following components:i) a propargyl derivative of the general structural formula Ia wherein Het is an optionally substituted hetero atom and A is a substituted or unsubstituted aromatic entity, a substituted or unsubstituted aromatic heterocycle, a substituted or unsubstituted vinyl arene and/or a derivative thereof, an olefin, an alkyne, an acceptor group or a nitrile;(ii) a compound of the general structural formula II,wherein B is an electron-deficient substituted or unsubstituted aromatic entity with or without an acceptor group, an electron-deficient substituted or unsubstituted heteroaromatic entity with or without an acceptor group, an electron-deficient olefin and/or alkyne, a metal complex, and X is a leaving group;(iii) a nucleophile of the general structural formula III,wherein Y and/or Z, each independently of the other, is an amino group, thio group (mercapto group), seleno group, telluro group, hydroxy group (alcohol group), imido group, carbonyl group, thiocarbonyl group, selenocarbonyl group, tellurocarbonyl group; C is a substituted or unsubstituted C atom, a substituted or unsubstituted or annelated CC double bond or single bond and n=0-10, preferably 1-5, preferably are reacted in a one-pot reaction by cyclocondensation to form 4- to 10-membered, preferably 5- to 7-membered, heterocyclic, aromatic or non-aromatic ring systems.

4. 发明专利

DE19955634A1 未知
公开(公告)号：DE19955634A1
公开(公告)日：2001-06-13
申请号：DE19955634
申请日：1999-11-21
申请人： MORPHOCHEM AG
发明人： MUELLER THOMAS J J , ANSORGE MARKUS
IPC分类号： A61P31/04 , A61P31/10 , C07D201/00 , C07D231/06 , C07D417/12 , C07D417/14 , C07D471/04 , C07D247/00 , C07D403/10 , C07D417/04 , A01N43/48
摘要： The invention relates to a method for producing heterocycles, characterised in that the following components are reacted, preferably in a one-pot reaction by cyclocondensation, to obtain a 4- to 10-, preferably 5- to 7-membered, heterocyclic aromatic or non-aromatic ring system: i) a propargyl derivative of general structural formula (I), Het being an optionally substituted hetero atom and A being a substituted or unsubstituted aromatic, a substituted or unsubstituted aromatic heterocycle, a substituted or unsubstituted vinyl arene and/or a derivative thereof, an olefin, an alkin, an acceptor group or a nitrile; (ii) a compound of general structural formula (II), wherein B is an electron-deficient substituted or unsubstituted aromatic with or without an acceptor group, an electron-deficient substituted or unsubstituted heteroaromatic with or without an acceptor group, an electron-deficient olefin and/or alkin, a metal complex; and X is a leaving group; (iii) a nucleophile of general structural formula (III), wherein Y and/or Z, independently of each other are an amino group, a thio group (mercapto group), a seleno group, a telluro group, a hydroxy group (alcohol group), an imido group, a carbonyl group, a thiocarbonyl group, a selenocarbonyl group, a tellurocarbonyl group; C is a substituted or unsubstituted C atom, a substituted or unsubstituted or anellated CC double bond or simple bond and n = 0-10, preferably 1-5.

5. 发明专利

AU2358601A Coupling condensation synthesis of heterocycles 未知
公开(公告)号：AU2358601A
公开(公告)日：2001-06-04
申请号：AU2358601
申请日：2000-11-21
申请人： MORPHOCHEM AG
发明人： MUELLER THOMAS , ANSORGE MARKUS
IPC分类号： A61P31/04 , A61P31/10 , C07D201/00 , C07D231/06 , C07D417/12 , C07D417/14 , C07D471/04
摘要： The invention relates to a process for the preparation of heterocycles, characterised in that the following components:i) a propargyl derivative of the general structural formula Ia wherein Het is an optionally substituted hetero atom and A is a substituted or unsubstituted aromatic entity, a substituted or unsubstituted aromatic heterocycle, a substituted or unsubstituted vinyl arene and/or a derivative thereof, an olefin, an alkyne, an acceptor group or a nitrile;(ii) a compound of the general structural formula II,wherein B is an electron-deficient substituted or unsubstituted aromatic entity with or without an acceptor group, an electron-deficient substituted or unsubstituted heteroaromatic entity with or without an acceptor group, an electron-deficient olefin and/or alkyne, a metal complex, and X is a leaving group;(iii) a nucleophile of the general structural formula III,wherein Y and/or Z, each independently of the other, is an amino group, thio group (mercapto group), seleno group, telluro group, hydroxy group (alcohol group), imido group, carbonyl group, thiocarbonyl group, selenocarbonyl group, tellurocarbonyl group; C is a substituted or unsubstituted C atom, a substituted or unsubstituted or annelated CC double bond or single bond and n=0-10, preferably 1-5, preferably are reacted in a one-pot reaction by cyclocondensation to form 4- to 10-membered, preferably 5- to 7-membered, heterocyclic, aromatic or non-aromatic ring systems.

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