COMBINATORIAL ACTIVE COMPOUND SYNTHESIS AND ITS INTERMEDIATES

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United States of America Patent

APP PUB NO 20020128383A1
SERIAL NO

08948557

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ATTORNEY / AGENT: (SPONSORED)

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Abstract

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The invention relates to a resin-bound synthesis process for the preparation of chemical compounds of the formula (I) R.sup.1--SO.sub.2--NH--CO--R.sup.2 (I) in which R.sup.1 and R.sup.2 each are an organic radical, which comprises a) reacting a resin-linker compound of the formula [resin polymer]-[L-Nuc].sub.n (II) in which nucleofugic groups Nuc are bonded to a resin [=resin polymer] via the linker L, with an acylsulfonamide of the formula E.sup.1--SO.sub.2--NH--CO--E.sup.2 (III) in which E.sup.1 and E.sup.2 independently of one another in each case are an organic radical suitable for the preparation of the radicals R.sup.1 and R.sup.2 in compound (I), in the presence of a condensing agent to give a resin-bound adduct of the formula (IV) 1 in which [resin polymer], L, n, E.sup.1 and E.sup.2 are as defined in formula (II) or formula (III), b) derivatizing the adduct (IV) obtained in one or more further reaction steps on the organic radicals E.sup.1 or E.sup.2 to give the radicals R.sup.1 or R.sup.2, and c) cleaving the compound of the formula (I) from the resin-linker adduct of the formula (IV') obtained.

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Patent Owner(s)

Patent OwnerAddress
HOECHST SCHERING AGREVO GMBHD-13342 BERLIN

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Inventor(s)

Inventor Name Address # of filed Patents Total Citations
HAAF, KLAUS KELKHEIM, DE 10 101
WILLMS, LOTHAR HOFHEIM, DE 225 1807

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