专利号:US-8987493-B2 优先权日:2010-05-20 标题 :Process for synthesis of silane dipeptide analogs 发明人:SIEBURTH SCOTT MCNEILL; BO YINGJIAN 权利人:SIEBURTH SCOTT MCNEILL; BO YINGJIAN; Temple University—Of the Commonwealth System of Higher Education 摘要:The invention provides a method of preparing silane dipeptide analogs, comprising the steps of treating a solution of a substituted 1,2-oxasilolane with lithium metal to form a solution of the dilithium salt of a substituted 3-hydroxypropylsilanol, and reacting the solution of the dilithium salt of the substituted 3-hydroxypropylsilanol with a substituted enamine.
专利号:US-6172226-B1 优先权日:1993-12-22 标 题:Synthons for the synthesis and deprotection of peptide nucleic acids under mild conditions 发明人:COULL JAMES M; EGHOLM MICHAEL; HODGE RICHARD P; ISMAIL MOHAMED; RAJUR S B 权利人:PERSEPTIVE BIOSYSTEMS INC 摘要:A method is disclosed for preparing novel PNA synthons having protecting groups capable of removal under mild conditions. The PNA synthons are prepared by coupling novel N-substituted nucleobase intermediates having carbamate protection of the exocyclic amino group of the heterocycle to an amino protected backbone or an amino protected backbone ester of the amino acid N-(2-aminoethyl)-glycine. By the method of this invention, the resultant PNA synthons can have orthogonal protection of the carbamate protected nucleobase and the amino protected backbone. The PNA synthons are useful in the synthesis of peptide nucleic acids (PNAs) and other oligomers such as PNA-DNA chimeras, and may be used in automated synthesizers. Novel compositions of matter are also disclosed. In addition, a guanine PNA synthon having selective carbamate protection of the exocyclic 2-amino group with the C6 carbonyl group unprotected is disclosed.
专利号:US-7038037-B2 优先权日:2002-06-20 标题 :Method for sequential support-bound synthesis of conjugated oligomeric compounds 发明人:MAIER MARTIN A; GUZAEV ANDREI P; MANOHARAN MUTHIAH 权利人:ISIS PHARMACEUTICALS INC 摘要:A sequential support-bound synthesis method is disclosed for preparing a conjugated oligomeric compound, preferably a PNA-peptide conjugate or an oligonucleotide-peptide conjugate, using a bridging molecule having at least two N-protecting amino groups. A conjugated oligomeric compound for therapeutic or prophylactic delivery is also disclosed.
专利号:US-2005256324-A1 优先权日:2004-05-10 标 题:Synthesis of amino acid keto-epoxides 发明人:LAIDIG GUY J; RADEL PEGGY A; SMYTH MARK S 权利人:PROTEOLIX INC 摘要:This invention relates to methods for the preparation of amino acid keto-epoxides. Specifically, allylic ketones are stereoselectively converted to the desired keto epoxides.
专利号:EP-1756079-A2 优先权日:2004-05-17 标 题:Synthesis of amino acid keto-epoxides 发明人:LAIDIG GUY J; RADEL PEGGY A; SMYTH MARK S 权利人:PROTEOLIX INC 摘要:This invention relate to methods for the preparation of amino acid keto-epoxides according to scheme (I). Specifically, allylic ketones are stereoselectively converted to the desired keto epoxides.
专利号:US-7402670-B2 优先权日:2004-09-30 标 题:Synthesis by chiral diamine-mediated asymmetric alkylation 发明人:DENG XIAOHU; MANI NEELAKANDHA 权利人:JANSSEN PHARMACEUTICA NV 摘要:Chiral synthesis from an achiral starting material by chiral diamine-mediated, such as sparteine-mediated, intermolecular asymmetric alkylation with a strained cyclic ether in the presence of a Lewis acid.