专利号:US-7067622-B2 优先权日:2001-06-25 标题 :Method of the solid phase synthesis of pyrrole-imidazole polyamide 发明人:SUGIYAMA HIROSHI; IIDA HIROKAZU; SAITO ISAO; SAITO TAKASHI 权利人:JAPAN SCIENCE & TECH AGENCY 摘要:It is intended to provide a method of producing a pyrrole-imidazole polyamide whereby a longer pyrrole-imidazole polyamide can be conveniently synthesized and a peptide (protein) can be easily transferred. According to this method, a pyrrole-imidazole polyamide having a carboxylate group which can be excised from a solid phase carrier at its end, makes it possible to directly transfer various functional groups and can exactly distinguish DNA sequences can be efficiently produced. A method of synthesizing a pyrrole-imidazole polyamide characterized by performing automatic synthesis by the solid phase Fmoc method with the used of a peptide synthesizer; a pyrrole-imidazole polyamide having a carboxyl group at its end obtained by this method; a pyrrole-imidazole polyamide having a DNA alkylation agent transferred into the carboxyl group at the end of the above-described pyrrole-imidazole polyamide; and a sequence-specific DNA alkylation method characterized by using the above compound.
专利号:US-2024425461-A1 优先权日:2023-06-13 标题 :Preparation process of intermediate, synthesis process of amino imidazole carboxylate ester and hplc purity measure method 发明人:DUAN JIANXIN; LU ZHAOQIANG; FAN JINWEI; HUANG QUNHUI; ZHANG YANJUN; CHEN WEISU; QIN WEI 权利人:ASCENTAWITS PHARMACEUTICALS LTD 摘要:This invention relates to a process for preparing an intermediate of aminoimidazole carboxylate, a process for synthesizing aminoimidazole carboxylate and an HPLC method for determining purity. The process of preparing the intermediate of aminoimidazole carboxylate comprises subjecting a compound of formula I-2 and a formate as the reactants to a first-step reaction in a benzene solvent and at a temperature of −5° C.−5° C., with the addition of a solution of sodium alkoxide in such a way that the temperature of the reaction solution is not higher than 5° C., to obtain the intermediate of aminoimidazole carboxylate or a mixture comprising a compound of formula I-3, i.e., the intermediate of aminoimidazole carboxylate. By using a sodium alkoxide reagent, as a comparatively safe alternative to NaH and potassium tert-butoxide which are prone to cause fire hazards or explosions and are not suitable for use in large-scale production, the process of the present application can ensure smooth progression of the reaction to the product and effectively improve the overall safety of the reaction without noticeably impairing the reaction efficiency.
专利号:CN-116789558-A 优先权日:2022-03-18 标题:Preparation method of intermediate, synthesis method of amino imidazole carboxylate and HPLC (high performance liquid chromatography) purity detection method
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