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The Synthesis of a Dopamine D 2 Partial Agonist for the Treatment of Schizophrenia
期刊名称： Organic Process Rearch & Development
参谋部伴侣度假村作者： Magano, Javier,Acciacca, Alison,Akin, Anne,Collman, Benjamin M.,Conway,
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智慧工程Brian,Waldo, Michael,Chen, Michael H.,Mennen, Kenneth E.
涨价 英文decursive年份： 2009年
调酒培训学校
期号： 第3期
关键词： Duranta repens;triterpene saponins;durantanin IV and V;brine
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摘要：The synthesis of the phosphoric acid salt of dopamine D2 partial agonist 2-{4-[4-(7-fluoro-naphthalen-1-yl)-piperazin-1-yl]-butoxy}-5,6,7,9-tetrahydro-1,7,9-triaza-benzocyclohepten-8-one (1) is reported. The most prominent feature of the molecule is a ven-membered ring urea functionality that 原产地
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has been prepared via an efficient one-pot, three-step transformation. The original synthesis from the Medicinal Chemistry group provided precursor 13 in 10 steps and 2% overall yield, required four chromatographies and employed unsafe reagents such as 2-iodoxybenzoic acid (IBX) and HClO4. The optimized synthetic route for the preparation of phosphate salt 1 consists of 12 linear steps with a 10% overall yield. Safer and more robust reaction conditions have been developed with only one required chromatography. Another key step in the
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