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    • 1. 发明申请
    • FORMATION OF N-PROTECTED BIS-3,6-(4-AMINOALKYL) -2,5,DIKETOPIPERAZINE
    • 形成N-保护的BIS-3,6-(4-氨基二甲基)-2,5,二酮类
    • WO2012109256A3
    • 2013-01-24
    • PCT/US2012024160
    • 2012-02-07
    • MANNKIND CORPFREEMAN JOHN JSTAMPER ADRIENNEHEITMANN MELISSA
    • FREEMAN JOHN JSTAMPER ADRIENNEHEITMANN MELISSA
    • C07D241/08B01J31/02C07C229/00
    • C07D241/08B01J31/0225B01J31/0258B01J31/0259B01J2231/40
    • The disclosed embodiments detail improved methods for the synthesis of diketopiperazines from amino acids. In particular improved methods for the cyclocondensation and purification of N-protected 3,6-(aminoalkyl)-2,5-diketopiperazines from N-protected amino acids. Disclosed embodiments describe methods for the synthesis of 3,6-bis-[N-protected aminoalkyl]-2,5-diketopiperazine comprising heating a mixture of an amino acid in the presence of a catalyst in an organic solvent. The catalyst is selected from the group comprising sulfuric acid, phosphoric acid, p-toluenesulfonic acid, 1 -propylphosphonic acid cyclic anhydride, tributyl phosphate, phenyl phosphonic acid and phosphorous pentoxide among others. The solvent is selected from the group comprising: dimethylacetamide, N-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme, ethyldiglyme, m-cresol, p-cresol, o-cresol, xylenes, ethylene glycol and phenol among others.
    • 所公开的实施方案详细描述了从氨基酸合成二酮哌嗪的改进方法。 特别是用于由N-保护的氨基酸环化缩合和纯化N-保护的3,6-(氨基烷基)-2,5-二酮哌嗪的改进方法。 公开的实施方案描述了合成3,6-双[N-保护的氨基烷基] -2,5-二酮哌嗪的方法,包括在催化剂存在下在有机溶剂中加热氨基酸的混合物。 催化剂选自硫酸,磷酸,对甲苯磺酸,1-丙基膦酸环状酸酐,磷酸三丁酯,苯基膦酸和五氧化二磷等。 溶剂选自二甲基乙酰胺,N-甲基-2-吡咯烷酮,二甘醇二甲醚,甘醇二甲醚,丙二醇,乙基二甘醇二甲醚,间甲酚,对甲酚,邻甲酚,二甲苯,乙二醇和苯酚等。
    • 2. 发明申请
    • FORMATION OF N-PROTECTED BIS-3,6-(4-AMINOALKYL) -2,5,DIKETOPIPERAZINE
    • 形成N-保护的BIS-3,6-(4-氨基二甲基)-2,5,二酮类
    • WO2012109256A2
    • 2012-08-16
    • PCT/US2012/024160
    • 2012-02-07
    • MANNKIND, CORPFREEMAN, John, J.STAMPER, AdrienneHEITMANN, Melissa
    • FREEMAN, John, J.STAMPER, AdrienneHEITMANN, Melissa
    • C07D241/08C07C229/00B01J31/02
    • C07D241/08B01J31/0225B01J31/0258B01J31/0259B01J2231/40
    • The disclosed embodiments detail improved methods for the synthesis of diketopiperazines from amino acids. In particular improved methods for the cyclocondensation and purification of N-protected 3,6-(aminoalkyl)-2,5-diketopiperazines from N-protected amino acids. Disclosed embodiments describe methods for the synthesis of 3,6-bis-[N-protected aminoalkyl]-2,5-diketopiperazine comprising heating a mixture of an amino acid in the presence of a catalyst in an organic solvent. The catalyst is selected from the group comprising sulfuric acid, phosphoric acid, p-toluenesulfonic acid, 1 -propylphosphonic acid cyclic anhydride, tributyl phosphate, phenyl phosphonic acid and phosphorous pentoxide among others. The solvent is selected from the group comprising: dimethylacetamide, N-methyl-2-pyrrolidone, diglyme, ethyl glyme, proglyme, ethyldiglyme, m-cresol, p-cresol, o-cresol, xylenes, ethylene glycol and phenol among others.
    • 所公开的实施方案详细描述了从氨基酸合成二酮哌嗪的改进方法。 特别是用于由N-保护的氨基酸环化缩合和纯化N-保护的3,6-(氨基烷基)-2,5-二酮哌嗪的改进方法。 公开的实施方案描述了合成3,6-双[N-保护的氨基烷基] -2,5-二酮哌嗪的方法,包括在催化剂存在下在有机溶剂中加热氨基酸的混合物。 催化剂选自硫酸,磷酸,对甲苯磺酸,1-丙基膦酸环状酸酐,磷酸三丁酯,苯基膦酸和五氧化二磷等。 溶剂选自二甲基乙酰胺,N-甲基-2-吡咯烷酮,二甘醇二甲醚,甘醇二甲醚,丙二醇,乙基二甘醇二甲醚,间甲酚,对甲酚,邻甲酚,二甲苯,乙二醇和苯酚等。