HKI-9924154
Chemical Name: (2S,5R,6R)-6-[2(R)-[2-[N-(2,3-Diacetoxybenzoyl)-N-[4-(2,3-diacetoxybenzamido)butyl]amino]acetamido]-2-phenylacetamido]-3,3-dimethyl-7-oxo-4-thia-1-azabicyclo[3.2.0]heptane-2-carboxylic acid
项目整合开发状态: Preclinical
项目研究机构: Gr黱enthal (Originator), Hans Kn鰈l Institute Natural Prod. Res. (Originator)
合成路线:Reductive condensation of 1,4-butanediamine (I) with glyoxylic acid (II) affords 3,8-diazaoctanoic acid (III).Subsequent acylation of diamino acid (III) with 2,3-diacetoxybenzoyl chloride (IV) provides diamide (V).After activation of (V) as the corresponding mixed anhydride with either methyl or isobutyl chloroformate,condensation with ampicillin (VI) yields the title compound.
📌 参考资料/链接：
参考文献标题:Catecholate beta-lactam conjugates,method for producing the same and the use thereof
文献作者:Berg,A.; Heinisch,L.; M鰈lmann,U.; Wittmann,S.; Scherlitz-Hofmann,I.; Stoiber,T.(Gr黱enthal GmbH)
参考来源:DE 10111160; WO 0270016
📄 详细内容
合成路线:Reductive condensation of 1,4-butanediamine (I) with glyoxylic acid (II) affords 3,8-diazaoctanoic acid (III).Subsequent acylation of diamino acid (III) with 2,3-diacetoxybenzoyl chloride (IV) provides diamide (V).After activation of (V) as the corresponding mixed anhydride with either methyl or isobutyl chloroformate,condensation with ampicillin (VI) yields the title compound.
参考文献标题:RF-2691A
文献作者:
参考来源:Drug Data Rep 1995,17(9),867