发明申请
US20130345423A1 EFFICIENT PEPTIDE COUPLINGS AND THEIR USE IN THE SYNTHESIS AND ISOLATION OF A CYCLOPENTA (G) QUINAZOLINE TRISODIUM SALT
有权
有效肽联合物及其在环孢菌素(G)喹唑啉三氯盐酸盐的合成和分离中的应用
- 专利标题: EFFICIENT PEPTIDE COUPLINGS AND THEIR USE IN THE SYNTHESIS AND ISOLATION OF A CYCLOPENTA (G) QUINAZOLINE TRISODIUM SALT
- 专利标题(中): 有效肽联合物及其在环孢菌素(G)喹唑啉三氯盐酸盐的合成和分离中的应用
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申请号: US13996618申请日: 2011-12-19
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公开(公告)号: US20130345423A1公开(公告)日: 2013-12-26
- 发明人: James Alan Kershen , Thomas Elliott Jacks , Andrew S. Thompson , Alexander James Bridges , Milind D. Choubal , Sean Mark Dalziel , James Robert Zeller
- 申请人: James Alan Kershen , Thomas Elliott Jacks , Andrew S. Thompson , Alexander James Bridges , Milind D. Choubal , Sean Mark Dalziel , James Robert Zeller
- 申请人地址: US CA San Franscisco
- 专利权人: Onyx Pharmaceutical, Inc.
- 当前专利权人: Onyx Pharmaceutical, Inc.
- 当前专利权人地址: US CA San Franscisco
- 国际申请: PCT/US11/65752 WO 20111219
- 主分类号: C07K1/08
- IPC分类号: C07K1/08 ; C07K1/16 ; C07D403/12 ; C07F7/10 ; C07C271/20 ; C07K1/10 ; C07K1/36
摘要:
A new method for the synthesis of L-Glutamyl-γ-D-Glutamic acid and its use in the synthesis of (2R)-((4S)-carboxy-4-(4,N-(((6S)-2-(hydroxymethyl)-4-oxo-3,4,7,8-tetrahydro-3H-cyclopenta[g]quinazolin-6-yl)-N-(prop-2-ynyl)amino)benzamido)butanamido)pentanedioic acid, 1 are provided. Also provided is an efficient method for the isolation and purification of the trisodium salt of the abovementioned acid, 2, in a form suitable for long term storage and use in a parenteral dosing form.
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