Resin-linker combination for the solid-phase synthesis of peptid

Details Resin-linker combination for the solid-phase synthesis of peptid Resin-linker combination for the solid-phase synthesis of peptid

1988-05-02

1989-05-16

Kight, John

Synthetic resins or natural rubbers -- part of the class 520 ser

Synthetic resins

Mixing of two or more solid polymers; mixing of solid...

5253333, C08F 1208, C08F 818, C08F11208

Patent

active

048310840

ABSTRACT:
The present invention relates to a novel polymeric carrier, a process for its production and its use for the preparation of peptides and their intermediates. The process comprises reacting chloromethylated polystyrene (cross-linked with divinylbenzene) with a 4-hydroxy-2-substituted-benzyl alcohol (linker), attaching .alpha.-amino acids with amino and side-chain protection to the carrier thus obtained, and building up a peptide according to the method known in the field of solid phase peptide synthesis (SPPS). The method allows removal of intermediates or final products under extremely mild acidic conditions giving products in high state of purity and yield. The 2-substituent consists of an electron donating group, such as methoxy.

REFERENCES:
patent: 4085261 (1978-04-01), Patchornik et al.
patent: 4173693 (1979-11-01), Au et al.
patent: 4446284 (1984-05-01), Parker
patent: 4725568 (1988-02-01), Parker et al.
R. B. Merrifield, J. Amer. Chem. Soc., 85, 2149-2154, (1963).
R. C. Sheppard et al., Inter. J. Pept. Prot. Res., 20, 451-454, (1982).
S. S. Wang, J. Amer. Chem. Soc., 95, 1328-1333, (1972).
K. D. Kopple, "Peptides and Amino Acids", (W. A. Benjamin, Inc., N.Y., 1963), pp. 4-7.
J. Meienhofer et al., Int. J. Pept. Prot. Res., 13, 35-42, (1979).
E. Kaiser et al., Anal. Biochem., 34, 595-598, (1970).

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