Hapten Synthesis for (+)-6-(2-Chlorophenyl)-3-cyclopropanecarbonyl-8,11-dimethyl-2,3,4,5-tetrahydro-8H-pyrido[4', 3' : 4,5]thieno[3,2-f]triazolo[4,3-a][1,4]diazepine(E6123)

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(+)-6-(2-Chlorophenyl)-3-cyclopropanecarbonyl-8,11-dimethyl-2,3,4,5-tetrahydro-8H-pyrido[4', 3' : 4,5]thieno-[3,2-f]triazolo[4,3-a][1,4]diazepine (E1623) is a very potent platelet-activating factor (PAF) receptor antagonist and shows potent anti-PAF activities at the microgram level in a variety of animal models. In order to examine the pharmacokinetics of E6123 at low doses, estabilishment of a radioimmunoassay is required. On the basis of the metabolic pattern of E6123,we synthesized 6-{2-chloro-4-(3-carboxypropyl)phenyl}-3-cyclopropanecarbonyl-8,11-dimethyl-2,3,4,5-tetrahydro-8H-pyrido[4', 3' : 4,5]thieno[3,2-f][1,2,4]triazolo[4,3-a][1,4]diazepine 22 as a potential hapten. In the synthesis of 22,we developed butynyl carbamate as a piperidine ring N-protecting group to prevent possible side reaction, namely oxidation of the methylene at position 2. This protecting group is stable under usual basic and acidic conditions.
公益社団法人日本薬学会の論文
1992-03-25