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1. 发明申请

WO2012109256A3 FORMATION OF N-PROTECTED BIS-3,6-(4-AMINOALKYL) -2,5,DIKETOPIPERAZINE 审中-公开
标题翻译：形成N-保护的BIS-3,6-（4-氨基二甲基）-2,5，二酮类
公开(公告)号：WO2012109256A3
公开(公告)日：2013-01-24
申请号：PCT/US2012024160
申请日：2012-02-07
申请人： MANNKIND CORP , FREEMAN JOHN J , STAMPER ADRIENNE , HEITMANN MELISSA
发明人： FREEMAN JOHN J , STAMPER ADRIENNE , HEITMANN MELISSA
IPC分类号： C07D241/08 , B01J31/02 , C07C229/00
CPC分类号： C07D241/08 , B01J31/0225 , B01J31/0258 , B01J31/0259 , B01J2231/40
摘要： 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.
摘要翻译：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

WO2012109256A2 FORMATION OF N-PROTECTED BIS-3,6-(4-AMINOALKYL) -2,5,DIKETOPIPERAZINE 审中-公开
标题翻译：形成N-保护的BIS-3,6-（4-氨基二甲基）-2,5，二酮类
公开(公告)号：WO2012109256A2
公开(公告)日：2012-08-16
申请号：PCT/US2012/024160
申请日：2012-02-07
申请人： MANNKIND, CORP , FREEMAN, John, J. , STAMPER, Adrienne , HEITMANN, Melissa
发明人： FREEMAN, John, J. , STAMPER, Adrienne , HEITMANN, Melissa
IPC分类号： C07D241/08 , C07C229/00 , B01J31/02
CPC分类号： C07D241/08 , B01J31/0225 , B01J31/0258 , B01J31/0259 , B01J2231/40
摘要： 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.
摘要翻译：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。

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