专利号:US-6683189-B1 优先权日:1996-02-26 标 题 :Method for the synthesis of pyrrole and imidazole carboxamides on a solid support 发明人:DERVAN PETER B; BAIRD ELDON 权利人:CALIFORNIA INST OF TECHN 摘要:The present invention describes a novel method for the solid phase synthesis of polyamides containing imidazole and pyrrole carboxamides. The polyamides are prepared on a solid support from aromatic carboxylic acids and aromatic amines with high stepwise coupling yields (>99%), providing milligram quantities of highly pure polyamides. The present invention also describes the synthesis of analogs of the natural products Netropsin and Distamycin A, two antiviral antibiotics. The present invention also describes a novel method for the solid phase synthesis of imidazole and pyrrole carboxamide polyamide-oligonucleotide conjugates. This methodology will greatly increase both the complexity and quantity of minor-groove binding polyamides and minor-groove binding polyamide-oligonucleotide conjugates which can be synthesized and tested.
专利号:US-10189803-B2 优先权日:2008-02-22 标题 :Synthesis of therapeutic and diagnostic drugs centered on regioselective and stereoselective ring opening of aziridinium ions 发明人:CHONG HYUN-SOON 权利人:CHONG HYUN SOON; ILLINOIS INSTITUTE OF TECH 摘要:Stereoselective and regioselective synthesis of compounds via nucleophilic ring opening reactions of aziridinium ions for use in stereoselective and regioselective synthesis of therapeutic and diagnostic compounds.
专利号:WO-0058264-A1 优先权日:1999-03-26 标 题:Method for the synthesis of non-symmetrical dtpa compounds 发明人:ACHILEFU SAMUEL I; SRINIVASAN ANANTHACHARI 权利人:MALLINCKRODT INC; ACHILEFU SAMUEL I; SRINIVASAN ANANTHACHARI 摘要:The synthesis of compounds of formula (XIV) wherein each R4 is an alkyl group having 1 to 15 carbon atoms, and R6 is a linking moiety having 1 to 10 carbon atoms, is disclosed. These compounds are useful intermediates in the synthesis of compounds of formula (X). These compounds are useful in the preparation of nuclear pharmaceuticals such as those used for tumor imaging or tumor therapy.
专利号:WO-0102339-A1 优先权日:1999-07-01 标题 :Versatile method for the synthesis of iso-dtpa 发明人:ACHILEFU SAMUEL I 权利人:MALLINCKRODT INC; ACHILEFU SAMUEL I 摘要:The synthesis of compounds of formula (XII) is disclosed. These compounds are useful intermediates in the synthesis of compounds of formulae (XI) and (X). These compounds are useful in the preparation of nuclear pharmaceuticals such as those used for tumor imaging or tumor therapy.
专利号:WO-0058267-A1 优先权日:1999-03-26 标 题 :Enhanced selectivity in the synthesis of dtpa esters fom diethylenetriamine 发明人:ACHILEFU SAMUEL I 权利人:MALLINCKRODT INC; SRINIVASAN ANANTHACHARI; ACHILEFU SAMUEL I 摘要:The synthesis of compounds of formula (XI) is disclosed. These compounds are useful intermediates in the synthesis of compounds of formula (X). These compounds are useful in the preparation of nuclear pharmaceuticals such as those used for tumor imaging or tumor therapy.
专利号:EP-1085020-B1 优先权日:1999-09-17 标题 :Synthesis of peptide nucleic acids 发明人:BATZ HANS-GEORG; HANSEN HENRIK FRYDENLUND; OERUM HENRIK; KOCH TROELS; KOFOED THOMAS 权利人:PNA DIAGNOSTICS APS APPLIED BI 摘要:Protected diaminopurines can be used in the synthesis of nucleic acid binding compounds containing diaminepurine in place of other nucleobases. A method for the synthesis of protected diaminopurines is disclosed which is convenient for incorporating modified diaminopurines into monomers or into oligomers for the preparation of nucleic acid binding compounds.
[参考文献]: Toru Masaka, Et Al. Synthesis Of Vip-Lipopeptide Using A New Linker To Modify Liposomes: Towards The Development Of A Drug Delivery System For Active Targeting. Chem Pharm Bull (Tokyo). 2013;61(11):1184-7.
合成参考文献
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