Invention Grant
- Patent Title: Reagents and methods for the beta-keto amide synthesis of a synthetic precursor to immunological adjuvant E6020
- Patent Title (中): β-酮酰胺合成免疫佐剂E6020合成前体的试剂和方法
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Application No.: US12338517Application Date: 2008-12-18
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Publication No.: US07919643B2Publication Date: 2011-04-05
- Inventor: Bruce DeCosta , Francis G. Fang , James E. Foy , Lynn Hawkins , Charles Lemelin , Xiang Niu , Kuo-Ming Wu
- Applicant: Bruce DeCosta , Francis G. Fang , James E. Foy , Lynn Hawkins , Charles Lemelin , Xiang Niu , Kuo-Ming Wu
- Applicant Address: JP
- Assignee: Eisai R & D Management Co., Ltd.
- Current Assignee: Eisai R & D Management Co., Ltd.
- Current Assignee Address: JP
- Agency: Nixon Peabody LLP
- Agent Jeffrey L. Costellia
- Main IPC: C07F9/02
- IPC: C07F9/02
Abstract:
This invention relates to the synthesis for a precursor of E6020, compound 26, via a β-keto amide alcohol intermediate, compound 22. The synthesis reacts compound 22 with compound 25 and the resultant intermediate is oxidized to produce compound 26, the precursor to E6020. Compounds 22 and 25, and their crystalline forms, represent separate embodiments of the invention. The invention also relates to compounds of formulas (3) and (4) and processes for their preparation. The β-keto amide alcohol intermediate compound 22 is a compound of formula (3). Compound 25 is a compound of formula (4).
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