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项目整合精选>>>Buspirone hydrochloride, APC-6003(oral), APC-6002(topical), MJ-9022-1, Buspimen, Bespar, Narol, BuSpar
Buspirone hydrochloride, APC-6003(oral), APC-6002(topical), MJ-9022-1, Buspimen, Bespar, Narol, BuSpar
丁螺旋酮盐酸盐 丁螺环酮 Chemical Name: 8-[4-[4-(2-Pyrimidinyl)piperazin-1-yl]butyl]-8-azaspiro[4.5]decane-7,9-dione monohydrochloride
CAS No. 33386-08-2, 36505-84-7 (free base)
项目整合开发状态: Launched-1985
项目研究机构: Bristol-Myers Squibb (Originator), Almirall Prodesfarma (Licensee), Meiji Seika (Licensee), Menarini (Licensee), Elan Transdermal Technologies (Codevelopment)
合成路线:The condensation of 1-(2-pyrimidinyl)piperazine (I) with 3-chloro-1-cyanopropane (II) by means of Na2CO3 in n-butanol gives 4-(2-pyrimidinyl)-1-(3-cyanopropyl)piperazine (III).This product is reduced with LiAlH4 or with H2 and Raney-Ni yielding 4-(2-pyrimidinyl)-1-(4-aminobutyl)piperazine (IV),which is finally condensed with 8-oxaspiro[4.5]decane-7,9-dione-(3,3-tetramethylene-glutaric anhydride) (V) in pyridine.
📌 参考资料/链接：
参考文献标题:Buspirone
文献作者:Castar,J.; Thorpe,P.
参考来源:Drugs Fut 1976,1(9),409
📄 详细内容
合成路线:The condensation of 1-(2-pyrimidinyl)piperazine (I) with 3-chloro-1-cyanopropane (II) by means of Na2CO3 in n-butanol gives 4-(2-pyrimidinyl)-1-(3-cyanopropyl)piperazine (III).This product is reduced with LiAlH4 or with H2 and Raney-Ni yielding 4-(2-pyrimidinyl)-1-(4-aminobutyl)piperazine (IV),which is finally condensed with 8-oxaspiro[4.5]decane-7,9-dione-(3,3-tetramethylene-glutaric anhydride) (V) in pyridine.
参考文献标题:Psychosedative agents.2.8-(4-substituted-1-piperazinylalkyl)-8-azaspiro-[4,5]decane-7,9-diones
文献作者:Allen,L.E.; Ferguson,H.C.; Kissel,J.W.
参考来源:J Med Chem 1972,15(5),477-479
合成路线:The condensation of 1-(2-pyrimidinyl)piperazine (I) with 3-chloro-1-cyanopropane (II) by means of Na2CO3 in n-butanol gives 4-(2-pyrimidinyl)-1-(3-cyanopropyl)piperazine (III).This product is reduced with LiAlH4 or with H2 and Raney-Ni yielding 4-(2-pyrimidinyl)-1-(4-aminobutyl)piperazine (IV),which is finally condensed with 8-oxaspiro[4.5]decane-7,9-dione-(3,3-tetramethylene-glutaric anhydride) (V) in pyridine.
参考文献标题:N-(Heteroarcyclic)piperazizylalkylazaspiroalkanediones
文献作者:Wu,Y.H.; et al.
参考来源:DE 2057845; FR 2073406; GB 1332194; US 3717634
产品链接: CAS No. 33386-08-2›› 产品链接: CAS No.36505-84-7››