COMBINATORIAL PREPARATIONS OF PHOSPHORUS-CONTAINING ACTIVE COMPOUNDS AND INTERMEDIATES BY SOLID PHASE SYNTHESIS
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United States of America Patent
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Issued Date -
Jun 12, 2003
app pub date -
Oct 7, 1998
filing date -
Oct 9, 1997
priority date (Note) -
Abandoned
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Abstract
The invention relates to solid phase processes for the systematic preparation of chemical compounds from the group of the phosphonous or phosphinic acids and/or derivatives thereof and the corresponding substance libraries which can be employed for test purposes, in particular tests for biological activity. The compounds (I) YR.sup.1P(.dbd.O)(OR.sup.3)R.sup.2 (I) in which Y, R.sup.1, R.sup.2, R.sup.3 are as defined in claim 1 are prepared by reacting a resin-linker adduct (II) [resin polymer]-[linker-Z-E.sup.1-S.sup.1].sub.n in the presence of a suitable Pd catalyst with a phosphinate (III) A.sup.1-O--(PHO)A.sup..quadrature. (III) with substitution of the group S.sup.1 to give the compound (IV) [resin polymer]-[linker-Z-E.sup.1-P(H)(.dbd.O)--OA.sup.1 (IV) and cleaving the compound (I) after derivatization reactions on the resin from the resin-linker adduct. The invention also provides the intermediate steps and resin-linked intermediate compounds, and also the substance libraries obtained.
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