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US 2002/0120072 A1Published application
Polymers based on N-carbamyl-N'-dimethysilyl methyl-piperazine traceless linkers for the solid phase synthesis of phenyl based libraries
AssigneeBoehringer Ingelheim Pharma GmbH & Co. KG
InventorsEnzo Cereda, Carlo Maria Pellegrini, Monica Quai, Walter Barbaglia
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Abstract
The present invention relates to polymers characterized by novel silicon linkers based on the carbamyl piperazine moiety, methods of preparing these polymers and their use in the solid phase synthesis of compounds or libraries of compounds embracing a phenyl ring in their structure.
Claims8
1) A compound of formula (I)
- 28
- wherein
- Resin denotes polystyrene, optionally cross linked with divinyl benzene or polyethylenglycol;
- R1 denotes hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl C1-C6-alkoxy, halogen, NO2 or CF3;
- R2 denotes a group selected from hydroxy, amino, and formyl, being optionally protected by a suitable protective group,
- or
- a 5 or 6 membered saturated or unsaturated nitrogen heterocycle, optionally containing one or two additional heteroatoms selected from the group consisting of oxygen, nitrogen and sulfur, and being optionally substituted by a group selected from C1-C6-alkyl, C1-C6-alkoxy, halogen, NO2 and a suitable protective group.
4 more elements
6) A compound of formula (IV)
- 29
- wherein
- R1 denotes hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl C1-C6-alkoxy, halogen, NO2 or CF3;
- and
- R2 denotes a group selected from hydroxy, amino, and formyl, being optionally protected by a suitable protective group.
2 more elements
8) A compound of formula (I′)
- 30
- wherein Resis denotes polystyrene, optionally cross linked with divinyl benzene or polyethylenglycol;
- R1 denotes hydrogen, C1-C6-alkyl, C2-C6-alkenyl, C2-C6-alkynyl C1-C6-alkoxy, halogen, NO2 or CF3;
- and
- R3 denotes a group selected from —O—CO—C1-C4-alkyl, —N(C1-C4-alykl)2, —NH—CO—C1-C4-alkyl, —NH—CO—OC1-C4-alkyl, —NH—CO—NH—C1-C4-alkyl, —COOH, —COOC1-C4-alkyl and —CONHC1-C4-alkyl and —CH2OH.
2 more elements
Dependencies are inferred from the claim text.