Synthesis and dopamine receptor selectivity of the benzyltetrahydroisoquinoline, (R)-(+)-nor-roefractine.
Synthesis and dopamine receptor selectivity of the benzyltetrahydroisoquinoline, (R)-(+)-nor-roefractine.
复制标题
苄基四氢异喹啉 (R)-( )-nor-roefratine 的合成和多巴胺受体选择性。
DOI：
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发表时间：
1998
影响因子：
5.1
通讯作者：
D. Cortes
中科院分区：
文献类型：
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作者：
N. Cabedo;P. Protais;B. Cassels;D. Cortes
(R)-(以（S）-N-CBZ-脯氨酰氧基硼氢化钠为还原剂，通过Bischler-Napieralski法合成了（+）-nor-Roefractine（1）。化合物1能够从其在大鼠纹状体中的特异性结合位点置换[3 H]-雷氯必利（D2多巴胺受体选择性配体），其选择性相对于[3 H]-SCH 23390（D1多巴胺受体选择性配体）。
(R)-(+)-nor-Roefractine (1) was synthesized by the Bischler-Napieralski route, using asymmetric reduction of the 1, 2-didehydro precursor imine with sodium (S)-N-CBZ-prolinyloxyborohydride. Compound 1 was able to displace [3H]-raclopride (a D2 dopamine receptor-selective ligand) from its specific binding sites in rat striatum with selectivity vs [3H]-SCH23390 (D1 dopamine receptor-selective ligand).