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

Applicant: MORPHOCHEM AG ,  MUELLER THOMAS ,  ANSORGE MARKUS

Inventor： MUELLER THOMAS ,  ANSORGE MARKUS

IPC: A61P31/04 ,  A61P31/10 ,  C07D231/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  A61K31/415 ,  A61K31/435 ,  A61K31/44 ,  A61K31/55 ,  A61K33/00

CPC classification number: C07D231/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: 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.

Abstract translation: 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。

公开(公告)号：DE50005935D1

公开(公告)日：2004-05-06

申请号：DE50005935

申请日：2000-11-21

Applicant: MORPHOCHEM AG

Inventor： MUELLER THOMAS ,  ANSORGE MARKUS

IPC: A61P31/04 ,  A61P31/10 ,  C07D201/00 ,  C07D231/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: 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.

公开(公告)号：AT263148T

公开(公告)日：2004-04-15

申请号：AT00987278

申请日：2000-11-21

Applicant: MORPHOCHEM AG

Inventor： MUELLER THOMAS ,  ANSORGE MARKUS

IPC: A61P31/04 ,  A61P31/10 ,  C07D201/00 ,  C07D231/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: 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.

公开(公告)号：AU2358601A

公开(公告)日：2001-06-04

申请号：AU2358601

申请日：2000-11-21

Applicant: MORPHOCHEM AG

Inventor： MUELLER THOMAS ,  ANSORGE MARKUS

IPC: A61P31/04 ,  A61P31/10 ,  C07D201/00 ,  C07D231/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04

Abstract: 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.