发明授权
- 专利标题: Synthesis of 4-amino-pyrimidines scaffolds
- 专利标题(中): 合成4-氨基 - 嘧啶支架
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申请号: US12522929申请日: 2008-01-07
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公开(公告)号: US08198443B2公开(公告)日: 2012-06-12
- 发明人: Werner Bonrath , Ralph Haerter , Reinhard Karge , Ulla Letinois
- 申请人: Werner Bonrath , Ralph Haerter , Reinhard Karge , Ulla Letinois
- 申请人地址: NL Heerlen
- 专利权人: DSM IP Assets B.V.
- 当前专利权人: DSM IP Assets B.V.
- 当前专利权人地址: NL Heerlen
- 代理机构: Nixon & Vanderhye P.C.
- 优先权: EP07001136 20070119
- 国际申请: PCT/EP2008/000320 WO 20080107
- 国际公布: WO2008/087021 WO 20080724
- 主分类号: C07D239/02
- IPC分类号: C07D239/02
摘要:
Process for the manufacture of a compound of the structure (I) with R1=hydrogen, alkyl (C1-C10, linear, cyclic or branched, aliphatic or aromatic), NR′R″ (wherein R′ and R″ are independently selected from H, alkyl [C1-C10, linear, cyclic or branched, aliphatic or aromatic] and R2=CH2R3 wherein R3 is selected from NHR1′″ (with R′″=C(O)H, C(O)CH3, C(O)alkyl, CH2C6H2(OMe)3 or other saponifiable residues), alkyl (C1-C10, linear, cyclic or branched) aromatic residues, heteroaryl residues, substituted aryl residues, e.g. 3,4,5-trimethoxy-phenyl) wherein 1 equivalent of an α-formyl-propionitrile salt is reacted with 0.75 to 2 equivalents of an acetamidine salt in the presence of a Lewis acid.
公开/授权文献
- US20100016591A1 SYNTHESIS OF 4-AMINO-PYRIMIDINES SCAFFOLDS 公开/授权日:2010-01-21
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