发明名称 |
Crystalline peptide epoxy ketone protease inhibitors and the synthesis of amino acid keto-epoxides |
摘要 |
The invention relates to crystalline peptide keto epoxide compounds, methods of their preparation, and related pharmaceutical compositions. This invention also relates to methods for the preparation of amino acid keto-epoxides. Specifically, allylic ketones are stereoselectively converted to the desired keto epoxides. |
申请公布号 |
US8921583(B2) |
申请公布日期 |
2014.12.30 |
申请号 |
US201313757113 |
申请日期 |
2013.02.01 |
申请人 |
Onyx Therapeutics, Inc. |
发明人 |
Phiasivongsa Pasit;Sehl Louis C.;Fuller William Dean;Laidig Guy J. |
分类号 |
C07D303/00;C07D301/03;C07K1/107;C07K1/30;C07C51/41;C07K5/107;C07K5/103;C07D303/36;C07C53/18;C07D301/00;A61K38/00 |
主分类号 |
C07D303/00 |
代理机构 |
Marshall, Gerstein & Borun LLP |
代理人 |
Marshall, Gerstein & Borun LLP |
主权项 |
1. A method for the preparation of a crystalline compound of Formula (III), wherein X is trifluorocetate, comprising (i) preparing a solution of a compound of Formula (IV) in an organic solvent, wherein PG is a suitable protecting group(ii) adding trifluoroacetic acid; (iii) bringing the solution to supersaturation to cause formation of crystals; and (iv) isolating the crystals, wherein said crystalline compound has 2θ values of 8.84; 15.18; 15.32;16.20; 16.82; 17.66; 18.26; 19.10; 21.20; 22.58; 23.06; 23.52; 25.32; 26.58; 28.60; 30.08; 30.48; 30.84; 32.20; 36.14; and 37.12. |
地址 |
South San Francisco CA US |