(S)-PD-148903-药物合成数据库

【药物名称】(S)-PD-148903

化学结构式(Chemical Structure):

参考文献No.	48851
标题:	Method for treating Parkinson's disease by administering (-)-5-keto-2-N,N-di-N-propylamino-tetrahydrotetralin
作者:	Wise, L.D.; Wikstrom, H.V.; Wustrow, D.J.; Meltzer, L.T.; Dijkstra, D.; Venhuis, B.J. (Pfizer Inc.)
来源:	WO 0128977

合成路线图解说明: Mannich reaction of 1,3-cyclohexanedione (I) with paraformaldehyde and dipropylamine affords intermediate (II) which, without isolation is condensed with acetone under Robinson annulation conditions, to produce the bicyclic amino ketone (III). Enamine reduction in (III) using NaBH3CN in AcOH gives a racemic amine, which is resolved via formation of the corresponding diastereoisomeric salts with (-)-ditoluyltartaric acid, and finally isolated as the hydrochloride salt.

参考文献No.	672305
标题:	A new type of prodrug of catecholamines: An opportunity to improve the treatment of Parkinson's disease
作者:	Venhuis, B.J.; Rodenhuis, N.; Wikstrom, H.V.; Wustrow, D.J.; Meltzer, L.T.; Wise, L.D.; Johnson, S.J.; Pugsley, T.A.; Sundell, S.; Dijkstra, D.
来源:	J Med Chem 2002,45(12),2349

合成路线图解说明: Mannich reaction of 1,3-cyclohexanedione (I) with paraformaldehyde and dipropylamine affords intermediate (II) which, without isolation is condensed with acetone under Robinson annulation conditions, to produce the bicyclic amino ketone (III). Enamine reduction in (III) using NaBH3CN in AcOH gives a racemic amine, which is resolved via formation of the corresponding diastereoisomeric salts with (-)-ditoluyltartaric acid, and finally isolated as the hydrochloride salt.