Malonic acid derivatives and methods for their synthesis

Details Malonic acid derivatives and methods for their synthesis Malonic acid derivatives and methods for their synthesis

1987-07-16

1990-04-03

Gray, Bruce

Organic compounds -- part of the class 532-570 series

Organic compounds

Carboxylic acid esters

560154, 560190, 560 55, C07C17565

Patent

active

049142267

ABSTRACT:
The present invention refers to a new class of malonic acid derivatives of general formula I ##STR1## wherein R.sup.1 and R.sup.2, each independently, represent hydrogen or a carboxyl protecting group, and the residue R corresponds to the side-chain of the amino acids lysine, ornithine, tyrosine, cysteine, asparatic acid and glutamic acid wherein the additional functionalities are suitably protected. The new compounds of the present invention are useful for preparing analogues of biologically active peptides wherein the direction of some amide bonds in which the amino acids lysine, ornithine, tyrosine, cysteine, aspartic acid or glutamic acid are involved, has been reversed.

REFERENCES:
patent: 3013069 (1961-12-01), Wilkinson et al.
patent: 4439360 (1984-03-01), Verdini et al.
patent: 4499079 (1985-02-01), Gordon et al.
patent: 4816560 (1989-03-01), Verdini et al.
Sheppard, "Peptide Synthesis," Comprehensive Organic Chemistry, Pergamon Press, Oxford, pp. 321-334 (1985).
Kritzler et al., Chemical Abstracts, vol. 61, No. 580h (1964).
Hayashi, Chemical Abstracts, vol. 55, No. 7304e (1961).
Oda et al., Chemical Abstracts, vol. 59, No. 3806g (1963).
Cohen, Chemical Abstracts, vol. 81, No. 63234x (1974).

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