本文报道了在乙炔基苯并恶唑啉酮-乙腈络合物(EBX-MeCN)存在下,由O-烷基异羟肟酸立体合成顺式-β- N-烷氧基酰胺乙烯基苯并恶唑烷(顺式-β - N -RO-酰胺-VBXs)。反应在温和的条件下进行,所述条件包括水性溶剂,温和的碱和室温。该反应容许各种衍生自羧酸的O-烷基异羟肟酸,例如氨基酸,药物和天然产物。还使用氧化氘作为氘源合成了乙烯基双氘化的顺式-β - N -MeO-酰胺-VBXs。缬氨酸衍生的顺式将-β - N - MeO-酰胺-VBX立体定向衍生为异羟肟酸衍生的顺式-酰胺,而不会失去立体选择性或降低氘/氢比。
Compositions Having Antimycrobial Activity Including a Hydroxamate or a Hydroxamate and a Hydroxlyamine
申请人:Kohn Harold
公开号:US20080249181A1
公开(公告)日:2008-10-09
Antimycorbacterial compositions are disclosed comprising at least one hydroxamate or at least one hydroxamate and at least one hydroxylamine. The preferred ratio of hydroxamate to hydroxylamines is about 100:1 to about 1:1. A method for inhibiting mycobacterial growth is also disclosed comprising the step of administering the compositions of this invention to an animal including a human.
(cis-β-N-RO-amide-VBXs) from O-alkyl hydroxamic acids in the presence of an ethynyl benziodoxolone–acetonitrile complex (EBX–MeCN) is reported herein. The reaction was performed under mild conditions including an aqueous solvent, a mild base, and room temperature. The reaction tolerated various O-alkyl hydroxamic acids derived from carboxylicacids, such as amino acids, pharmaceuticals, and natural products
本文报道了在乙炔基苯并恶唑啉酮-乙腈络合物(EBX-MeCN)存在下,由O-烷基异羟肟酸立体合成顺式-β- N-烷氧基酰胺乙烯基苯并恶唑烷(顺式-β - N -RO-酰胺-VBXs)。反应在温和的条件下进行,所述条件包括水性溶剂,温和的碱和室温。该反应容许各种衍生自羧酸的O-烷基异羟肟酸,例如氨基酸,药物和天然产物。还使用氧化氘作为氘源合成了乙烯基双氘化的顺式-β - N -MeO-酰胺-VBXs。缬氨酸衍生的顺式将-β - N - MeO-酰胺-VBX立体定向衍生为异羟肟酸衍生的顺式-酰胺,而不会失去立体选择性或降低氘/氢比。