Coupling condensation synthesis of heterocycles

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United States of America Patent

PATENT NO 6774229
SERIAL NO

10151687

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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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 I ##STR1## a 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, B--X 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, Y--C.sub.n --Z 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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Patent Owner(s)

Patent OwnerAddress
MORPHOCHEM AG82152 MARTINSRIED

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
Ansorge, Markus Munchen, DE 1 2
Mueller, Thomas Munchen, DE 218 2691

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