Thiocylating reagents and intermediates, thiopeptides, and...

Details Thiocylating reagents and intermediates, thiopeptides, and... Thiocylating reagents and intermediates, thiopeptides, and...

C - Chemistry, Metallurgy

07

K

C07K 5/04 (2006.01) C07C 237/04 (2006.01) C07C 327/42 (2006.01) C07D 207/16 (2006.01) C07D 209/26 (2006.01) C07D 233/64 (2006.01) C07D 235/26 (2006.01) C07D 311/88 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07K 5/02 (2006.01) C07K 5/09 (2006.01) C07K 5/093 (2006.01) C07K 5/103 (2006.01) C07K 14/66 (2006.01) A61K 38/00 (2006.01)

Patent

CA 2059647

Thioacylating reagents are provided for the introduction of thioamide bonds into growing peptides represented by struc- ture (I), where the substituents are disclosed herein. Intermediate precursors for preparing these thioacylating reagents are also provided. A process for preparing the thioacylating reagents and the intermediate precursors is further provided. Thiopeptides, and salts thereof, that exhibit pharmacological utility are provided and are represented by formula (II), wherein R1, R3, R4, X and n are as defined herein. Methods for preparing these thiopeptides from solution and solid phase syntheses, utilizing the thioacylating reagents disclosed herein, are also provided.

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