【药物名称】
化学结构式(Chemical Structure):
参考文献No.668958
标题:Synthesis of (1S,2R)-1-phenyl-2-[(S)-1-aminopropyl]-N, N-diethylcyclopropanecarboxamide (PPDC) derivatives modified at the carbamoyl moiety as a new class of NMDA receptor antagonists
作者:Kazuta, Y.; Tsujita, R.; Ogawa, K.; Hokonohara, T.; Yamashita, K.; Morino, K.; Matsuda, A.; Shuto, S.
来源:Bioorg Med Chem 2002,10(6),1777
合成路线图解说明:

The title compound is synthesized from the optically active lactone (I). Aluminum chloride-catalyzed aminolysis of (I) with dipropylamine affords the hydroxy amide (II). Subsequent Swern oxidation of the alcohol function of (II) leads to aldehyde (III). Addition of ethylmagnesium bromide to aldehyde (III) then stereoselectively provides the (S)-alcohol adduct (IV). Introduction of an azido group in (IV) by using a Mitsunobu-type reaction leads to configuration-retained azide (V). This is finally reduced to the desired amine by catalytic hydrogenation in the presence of Pd/C

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