DBO-83

1H-2-苯并吡喃-5,6-二醇,1-(氨基甲基)-3,4-二氢-3-(羟甲基)-,(1R,3S)-Chemical Name: 3-Chloro-6-(3,8-diazabicyclo[3.2.1]oct-3-yl)pyridazine dihydrochloride
CAS No. 195211-53-1
项目整合开发状态: Preclinical
项目研究机构: Universit?degli Studi di Firenze (Originator), Universit?degli Studi di Milano (Originator)
合成路线:3-Benzyl-3,8-diazabicyclo[3.2.1]octane (I) was protected at the N8 position with di tert-butyl dicarbonate in CH2Cl2,and carbamate (II) was then debenzylated by catalytic hydrogenolysis over Pd/C.The resulting bicyclic amine (III) was condensed with 3,6-dichloropyridazine (IV) in the presence of Et3N to give the Boc-protected intermediate (V),which was finally deprotected with HCl in Et2O.
📌 参考资料/链接:
参考文献标题:Mono- and disubstituted-3,8-diazabicyclo[3.2.1]octane derivatives as analgesics structurally related to epibatidine: Synthesis,activity,and modeling
文献作者:Barlocco,D.; Cignarella,G.; Tondi,D.; Vianello,P.; Villa,S.; Bartolini,A.; Ghelardini,C.; Galeotti,N.; Anderson,D.J.; Kuntzweiler,T.A.; Colombo,D.; Toma,L.
参考来源:J Med Chem 1998,41(5),674

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