Preparation of lysine based macromolecular highly branched homogeneous compound

Claim 1

Process of producing a macromolecule which comprises: (A) an initiation stage wherein at least one source unit(S) is combined with at least one lysine unit by: (1) blocking the two amino groups of lysine by conversion of each to a t-butyloxyurethane group; thus protecting these amino groups against reaction with the carboxyl group; (2) blocking the free carboxyl group of the obtained diurethane, N,N'-(di(t-butyloxycarbonyl) lysine, by conversion thereof to an inert N-substituted amide of said carboxyl group, inert toward amino groups; (3) liberating the two lysine amino groups by hydrolysis of the two urethane groups whereby the t-butyloxycarbonyl groups are removed and decomposed to t-butanol and carbon dioxide; thus freeing the two amino groups and obtaining a Compound I; (B) a first growth stage wherein two lysine units (M) are linked to the lysine unit of Compound I by: (1) blocking the two amino groups of the lysine unit in Compound I as in step (A) (1) above by conversion of each to a t-butyloxy urethane group; (2) forming a Compound (II) by converting the free carboxyl group of the N,N'-di(t-butyloxycarbonyl) lysine, obtained in step (B) (1) above, to a carboxyl derivative reactive with amino groups; (3) contacting the diamino-containing Compound (I), obtained in step (A)(3) above, with the reactive carboxyl derivative, Compound (II) of step (B)(2) above, to form the linkage --CONH-- and thereby link the lysine unit (M) of Compound I via its two amino groups to each of two diurethane lysine units (M) of Compound II via their carboxyl groups; and then liberating the four blocked amino groups by hydrolysis of the four urethane groups as in step (A)(3) above thereby forming Compound III; (C) as a third stage, repeating the steps, as in the preceding stage, of blocking the lysine amino groups; coverting the carboxyls of such blocked lysines to a reactive derivative Compound II; and linking four of these Compound II molecules via their reactive carboxyl derivative, to the four amino groups in each molecule of Compound III; and then liberating the eight amino groups of the four newly added lysine units to form Compound IV; (D) repeating at least once more, the set of growth steps of stage (C) above, thereby at each new stage increasing by a factor of essentially 2, the number of lysine units contained in the resulting macromolecule.