【药物名称】EP-1052
化学结构式(Chemical Structure):
参考文献No.56839
标题:14-Membered macrolides derived from leucomycins
作者:Or, Y.S.; Wang, J.; Lazarova, T.; Binet, S. (Enanta Pharmaceuticals, Inc.)
来源:US 6440942; WO 0260912
合成路线图解说明:

Ring contraction of the 16-membered lactone skeleton of josamycin (I) to the 14-membered lactone (III) is accomplished by olefin metathesis in the presence of Nolan catalyst (II) and 1-hexene. Subsequent deacetylation of (III) employing K2CO3 in MeOH gives rise to the title compound.

合成路线图解说明:

In a closely related procedure, leucomycin A1 (I) is subjected to olefin metathesis in the presence of Nolan catalyst (II) and 1-hexene to furnish the title compound.

参考文献No.694152
标题:Synthesis and biological evaluation of a new class of 14-membered ring macrolide antibiotics
作者:Binet, S.M.; Evans, J.; Haley, T.; Napper, A.; Phan, L.; Or, Y.; Lazarova, T.I.
来源:42nd Intersci Conf Antimicrob Agents Chemother (Sept 27 2002, San Diego) 2002,Abst F-1665
合成路线图解说明:

Ring contraction of the 16-membered lactone skeleton of josamycin (I) to the 14-membered lactone (III) is accomplished by olefin metathesis in the presence of Nolan catalyst (II) and 1-hexene. Subsequent deacetylation of (III) employing K2CO3 in MeOH gives rise to the title compound.

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