On July 2, 2009, Manoharan, Muthiah; Rajeev, Kallanthottathil G.; Jayaraman, Muthusamy; Narayanannair, Jayaprakash K. published a patent.Name: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate The title of the patent was Preparation of oligonucleotide-folate conjugates. And the patent contained the following:
The invention provides an iRNA agent having at least one monomer with the structure shown in formula I, where A and B are each independently O, imino groups, or S; X, Y are independently H, a protecting group, a phosphate, phosphodiester, activated phosphate or phosphite group, phosphoramidite, a solid support, -P(Z’)(Z”)O-nucleoside, -P(Z’)(Z”O)-oligonucleotide, a lipid, a PEG, a steroid, a polymer, -P(Z’)(Z”)O-L6-Q’-L7-OP(Z”’)(Z””)O-oligonucleotide, a nucleotide, or an oligonucleotide (Y may also be a lipophile); R is folate, a folate analog or mimic or a folate receptor-binding ligand; L6, L7 are independently -(CH2)n-, -CR’R”(CH2)n-, -(CH2)nCR’R”-, -(CH2CH2O)mCH2CH2-, or -(CH2CH2O)mCH2CH2NH-; Q’ is NH, O, S, CH2, CO2, CONH, NHCH(Ra)CO-, -COCH(Ra)NH-, CO, etc.; Ra is H or an amino acid side chain; R’, R” are independently H, Me, OH, SH, NH2, alkyl- or dialkylamino; Z’, Z”, Z”’, and Z”” are independently O or S; n is 1-20; and m is 0-50. The synthesis and biol. properties of oligonucleotide-folate conjugates are described. An example describes the synthesis of folate conjugate monomer II (CPG = controlled pore glass long-chain alkylamine, DMTr = 4,4′-dimethoxytrityl). A figure shows the in vivo targeting of folate-conjugated siRNAs. The experimental process involved the reaction of (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate(cas: 53838-27-0).Name: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate
The Article related to folate oligonucleotide conjugate preparation antitumor, Amino Acids, Peptides, and Proteins: Poly(Amino Acids) and Peptides and other aspects.Name: (S)-5-tert-Butyl 1-methyl 2-aminopentanedioate
Referemce:
Ester – Wikipedia,
Ester – an overview | ScienceDirect Topics