Method of synthesizing dendrimeric amphiphile

A method for synthesizing amphiphilic dendrimers, comprising:

• (a) reacting a compound of formula (IIb) with at least one diamino carboxylate having two protecting group for replacing Y on the compound of formula (IIb) to develop branched skeletons and modifying the terminal groups of the branched skeleton with functional moieties to obtain a compound of formula (IIIb),
• wherein M is a solid support material;
• X is amino carboxylate;
• Y is a protection group to protect the N-terminal of X;
• K is a moiety with branched diamine;
• B and B′ are K(2n−1)Z2n, wherein n is 0 to 5 and Z is a functional moiety comprising H, amino acids, peptides, acids, sugars, targeting ligands, imaging molecules, therapeutic agents, or peptidomimetic molecules;
• provided that B is not the same as B′, at least one of Z, K or n of B is different from B′;
• (b) reacting the compound of formula (IIIb) with nitrite in a polar solvent to obtain a compound of formula (IVb) having a benzotriazole structure,
• and
• (c) reacting the compound of formula (IVb) with one amine having hydrophobic residues in a mixed solution containing a hydrophilic solvent and a hydrophobic solvent to obtain a compound of formula (Vb),
• wherein R′ comprises amino groups having hydrophobic residues;
• or reacting at least two compounds of formula (IVb) with corresponding di- or multi-amine having hydrophobic residues in a mixed solution containing a hydrophilic solvent and a hydrophobic solvent to obtain a compound of formula (Vb′),
• wherein R″ comprises branched di- or multi-amino amino groups having hydrophobic residues, and n>1.