Combinatorial active compound synthesis and its intermediates

A process for the preparation of chemical compounds of the formula (I)

• R1—SO2—NH—CO—R2 (I)
• in which R1 and R2 are each an organic radical,
• which comprises
• a) reacting a resin-linker compound of the formula (II)
• [resin polymer]-[L-Nuc]n (II)
• in which
• [resin polymer] is the radical of a resin which is connected via n binding sites with the n groups of the formula -L-Nuc as defined in formula (II),
• L is in each case an organic linker,
• Nuc is a nucleofugic group (leaving group) or a group to be activated under the reaction conditions to give a leaving group,
• n is the number of functional groups L-Nuc on the resin and is greater than or equal to 1,
• with an acylsulfonamide of the formula (III)
• E1-SO2—NH—CO—E2 (III)
• in which E1 and E2 independently of one another in each case are an organic radical which is suitable for the preparation of the radicals R1 and R2 in compound (I),
• in the presence of a condensing agent to give a resin-bound adduct of the formula (IV)
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• in which [resin polymer], L, n, E1 and E2 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 E1 or E2 and thus optionally reacting via resin-bound intermediates of the formula (IV′), which in contrast to formula (IV) contain the organic radicals (E1)′ or (E2)′ of the derivatives, to give the compound (IV″)
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• in which R1 and R2 are as defined in formula (I) and [resin polymer], L and n are as defined in formula (II) or formula (IV), and
• c) removing the compound of the formula (I) from the resin-linker adduct of the formula (IV″).