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OBTAINING N-PROTECTED BIS-3,6-(4-AMINOALKYL)-2,5-DIKETOPIPERAZINE

机译:获得N保护的BIS-3,6-(4-氨基烷基)-2,5-二酮哌嗪

摘要

FIELD: chemistry.;SUBSTANCE: invention relates to a method for synthesis of 3,6-bis-[N-protected aminoalkyl]-2,5-diketopiperazine. Method involves heating a mixture of amino acids of general formula I in presence of catalyst in an organic solvent. Said catalyst is phosphorus pentoxide, which is present in concentration of 20 mol% to 50 mol% with respect to concentration of amino acids; n equals 2 or 3; PG represents trifluoroacetyl, and said solvent is selected from a group consisting of dimethylacetamide, N-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme and ethyldiglyme. Invention also relates to a method for synthesis of 3,6-bis-4-(N-trifluoroacetyl)aminobutyl-2,5-diketopiperazine, which involves heating a mixture of ε-trifluoroacetyl-L-lysine in presence of phosphorus pentoxide in N-methyl-2-pyrrolidone to temperature from 150 to 175 °C for 0.25–5 h, wherein concentration of phosphorus pentoxide ranges from approximately 20 mol% to approximately 35 mol% of concentration of ε-trifluoroacetyl-L-lysine, and slaking said mixture with a second solvent.;EFFECT: disclosed methods ensure high output of reaction.;8 cl, 4 tbl, 3 dwg, 10 ex
机译:发明领域本发明涉及一种3,6-双-[N-保护的氨基烷基] -2,5-二酮哌嗪的合成方法。方法包括在有机溶剂中在催化剂的存在下加热通式I的氨基酸的混合物。所述催化剂是五氧化二磷,其相对于氨基酸的浓度以20mol%至50mol%的浓度存在。 n等于2或3; PG代表三氟乙酰基,并且所述溶剂选自二甲基乙酰胺,N-甲基-2-吡咯烷酮,二甘醇二甲醚,乙基二甘醇二甲醚,脯氨酸二甲醚和乙基二甘醇二甲醚。本发明还涉及一种合成3,6-双-4-(N-三氟乙酰基)氨基丁基-2,5-二酮哌嗪的方法,该方法包括在五氧化二磷存在下在N中加热ε-三氟乙酰基-L-赖氨酸的混合物。 -甲基-2-吡咯烷酮在150至175°C的温度下静置0.25-5小时,其中五氧化二磷的浓度为ε-三氟乙酰基-L-赖氨酸浓度的约20摩尔%至约35摩尔%,与第二种溶剂混合;效果:所公开的方法可确保高产量的反应; 8 cl,4 tbl,3 dwg,10 ex

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