新产品编号:872191

Chemical Name: N-Decanoyl-L-tryptophyl-L-asparaginyl-L-aspartyl-L-threonyl-glycyl-N5-(1H-imidazol-2-ylmethyl)-L-ornithyl-L-aspartyl-D-alanyl-L-aspartyl-glycyl-D-seryl-threo-3-methyl-L-glutamyl-3-anthraniloyl-L-alanine C-1.13-O-2.4-lactone
CAS No. 345645-14-9
项目整合开发状态: Preclinical
项目研究机构: Cubist (Originator)
合成路线:Daptomycin (I) was obtained as a fermentation product from Streptomyces roseosporus.Selective acylation of (I) at the lysine side-chain amino group by means of N-Boc-tryptophan activated as either the pentafluorophenyl (II) or the p-nitrophenyl ester (III) furnished the corresponding tryptophan amide (IV).

合成路线:The N-Boc group of (IV) was then removed by treatment with trifluoroacetic acid in the presence of thioanisole or in the presence of ethanedithiol and triethylsilane to furnish the desired lipodepsipeptide.

合成路线:The title compound is prepared by reductive alkylation of daptomycin (I) with 2 imidazolecarboxaldehyde (II) in the presence of NaBH(OAc)3 in DMF.