Invention Grant
US09458188B2 Efficient peptide couplings and their use in the synthesis and isolation of a cyclopenta (G) quinazoline trisodium salt
有权
高效的肽偶联及其在合成和分离环戊烷(G)喹唑啉三钠盐中的应用
- Patent Title: Efficient peptide couplings and their use in the synthesis and isolation of a cyclopenta (G) quinazoline trisodium salt
- Patent Title (中): 高效的肽偶联及其在合成和分离环戊烷(G)喹唑啉三钠盐中的应用
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Application No.: US13996618Application Date: 2011-12-19
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Publication No.: US09458188B2Publication Date: 2016-10-04
- Inventor: James Alan Kerschen , Alexander James Bridges , Milind D. Choubal , Sean Mark Dalziel , Thomas Elliott Jacks , Andrew S. Thompson , James Robert Zeller
- Applicant: James Alan Kerschen , Alexander James Bridges , Milind D. Choubal , Sean Mark Dalziel , Thomas Elliott Jacks , Andrew S. Thompson , James Robert Zeller
- Applicant Address: GB London
- Assignee: BTG INTERNATIONAL LIMITED
- Current Assignee: BTG INTERNATIONAL LIMITED
- Current Assignee Address: GB London
- Agency: Tarolli, Sundheim, Covell & Tummino LLP
- International Application: PCT/US2011/065752 WO 20111219
- International Announcement: WO2012/087888 WO 20120628
- Main IPC: C07F7/02
- IPC: C07F7/02 ; C07K1/08 ; C07F7/18 ; C07K5/02 ; C07C271/20 ; C07D403/12 ; C07F7/10 ; C07K1/10 ; C07K1/16 ; C07K1/36 ; C07D239/90

Abstract:
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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