Synthesis of dolastatin 10

Details Synthesis of dolastatin 10 Synthesis of dolastatin 10

1989-01-27

1990-12-18

Lee, Lester L.

Chemistry: natural resins or derivatives; peptides or proteins;

Peptides of 3 to 100 amino acid residues

4 to 5 amino acid residues in defined sequence

C07K 510, C07K 706

Patent

active

049787446

ABSTRACT:
A complicated but extremely important scheme of synthesis has been developed for synthesizing, dolaisoleuine, dolaproine, dolaphenine and dolavaline from readily available starting materials such as Z-(S,S)isoleucine, S-phenylalaline, S-phenylalaninol, S-prolinol, S-mandelate, and S-valine. The requisite amino acids have been combined using several peptide coupling procedures to create pharmaceutically pure dolastatin 10.

REFERENCES:
patent: 4414205 (1983-11-01), Pettit
patent: 4486414 (1984-12-01), Pettit
The Isolation and Structure of a Remarkable Marine Animal Antineoplastic Constituent: Dolastatin 10.sup.1a, Pettit et al., JACS vol. 109, No. 22, (1987).

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