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US 6,639,023 B1Granted
Fluorophenyl resin compounds
AssigneeAventis Pharmaceuticals Inc.
InventorsJoseph M. Salvino, Robert D. Groneberg, John E. Airey, Gregory B. Poli, Gerard M. McGeehan, Richard F. Labaudiniere, François-Frédéric Clerc, Daniel Noël André Bezard
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Abstract
This invention is directed to a fluorophenyl resin compound, to methods of its preparation; and to its use in the solid phase synthesis of amides, peptides, hydroxamic acids, amines, urethanes, carbonates carbamates, sulfonamides and α-substituted carbonyl compounds.
Claims68
A fluorophenyl resin compound of formula
- wherein
- is a solid support;
- A is selected from
- L is a chemical bond,
- m is 1 to 5;
- p is 0, 1 or 2;
- B is F, OW or SO2Z;
- D is CH or N;
- W is hydrogen, tripyrrolidinophosphonium, C(O)V, C(O)Ra, C(O)NRbRc, C(O)Ora, SO2Ra or
- V is Cl or imidazol-1-yl;
- Y is O or NR3;
- Z is Cl, —OH, ORa or NRaRi;
- Ra and Rf are independently aliphatic or aromatic;
- Rb and Rc are independently H, aliphatic or aromatic, or Rb and Rc, taken together with the N atom through which they are attached, form an azaheterocyclyl or azaheterocyclenyl;
- Ri is CH2Rf;
- R0, R1 and R2 are a ring system substituent, or R0 and R1 taken together with the adjacent carbon atoms through which they are linked form a 6 membered aryl or 5 to 6 membered heteroaryl;
- R3 is H or lower alkyl;
- R4, R5, R6 and R7 are independently ring system substituents, or R4 and R5 taken together with the carbon atoms through which they are linked form a 6 membered aryl or 5 to 6 membered heteroaryl;
- and
- R11 and R12 are independently alkyl, heteroaryl, or aryl.
17 more elements
Dependencies are inferred from the claim text.