F-10981-药物合成数据库

【药物名称】F-10981

化学结构式(Chemical Structure):

参考文献No.	35577
标题:	Novel benzodioxanes and 1-(2H)-benzopyranes, their preparation and their use as medicine
作者:	Vidaluc, J.-L.; Imberg, T.; Marien, M.; Briley, M. (Pierre Fabre M閐icament)
来源:	WO 9802435

合成路线图解说明: Condensation of 2-(1-benzyl-4-piperidinyl)ethyl amine (I) with phenyl isocyanate (II) provided the corresponding urea (III), which was debenzylated by hydrogenolysis over Pd/C to afford the secondary amine (IV). Subsequent Mannich reaction of (IV) with 4-chromanone (V) and paraformaldehyde produced the (chromanylmethyl)piperidine (VI). After ketone reduction of (IV) by means of NaBH4, the resulting alcohol (VII) was dehydrated in refluxing 6 N HCl to furnish the target chromene.

参考文献No.	527416
标题:	Modulation of the benzodioxane heterocycle in a novel series of potent alpha2 adrenoceptor antagonists
作者:	Mayer, P.; et al.
来源:	217th ACS Natl Meet (March 21 1999, Anaheim) 1999,Abst MEDI 112

合成路线图解说明: Condensation of 2-(1-benzyl-4-piperidinyl)ethyl amine (I) with phenyl isocyanate (II) provided the corresponding urea (III), which was debenzylated by hydrogenolysis over Pd/C to afford the secondary amine (IV). Subsequent Mannich reaction of (IV) with 4-chromanone (V) and paraformaldehyde produced the (chromanylmethyl)piperidine (VI). After ketone reduction of (IV) by means of NaBH4, the resulting alcohol (VII) was dehydrated in refluxing 6 N HCl to furnish the target chromene.