Butenafine hydrochloride, 501 cream(combination with betamethasone dipropionate), KP-363, Volley, Mentax, -Drug Synthesis Database

【结构式】

【药物名称】Butenafine hydrochloride, 501 cream(combination with betamethasone dipropionate), KP-363, Volley, Mentax

【化学名称】N-Methyl-N-(4-tert-butylbenzyl)-1-naphthylmethylamine hydrochloride
　　　　　　4-tert-Butyl-N-methyl-N-(1-napthylmethyl)benzylamine hydrochloride

【CA登记号】101827-46-7, 101828-21-1 (free base)

【分子式】C₂₃H₂₈ClN

【分子量】353.93931

【开发单位】Kaken (Originator), Bertek (Licensee), Schering-Plough (Licensee), UCB (Licensee), Hisamitsu (Formulation)

【药理作用】Antifungal Agents, ANTIINFECTIVE THERAPY

合成路线1 合成路线2

合成路线1

By condensation of N-methyl-1-naphthylmethylamine (I) with 4-(tert-butyl)benzyl bromide (II) by means of Na2CO3 in DMF, followed by acidification with HCl in ethanol.

参考文献中间体

【1】 Arai, K.; Arita, M.; Sedino, T.; Komoto, N.; Hirose, S. (Mitsui Toatsu Chem.; Inc.); Benzylamine derivatives, process for production thereof, and use thereof. EP 0221781 .
【2】 Prous, J.; Castaner, J.; KP-363. Drugs Fut 1989, 14, 4, 315.

中间体序号	中间体编号	品名	CAS号	分子式	供应商	用于合成
(I)	10108	N-Methyl(1-naphthyl)methanamine; N-Methyl-N-(1-naphthylmethyl)amine; 1-Methyl-1-naphthalenemethylamine	65473-13-4	C₁₂H₁₃N	详情	详情
(II)	20588	1-(bromomethyl)-4-(tert-butyl)benzene	18880-00-7	C₁₁H₁₅Br	详情	详情

合成路线2

By condensation of 1-(chloromethyl)naphthalene (I) with N-(4-tert-butylbenzyl)-N-methylamine (II) by means of sodium carbonate in hot DMF.

参考文献中间体

【1】 Maeda, T.; Koshikawa, S.; Yamamoto, T.; Sasaki, K.; Yokoo, M.; Amemiya, K.; Hashimoto, R.; Arika, T.; Takase, M. (Kaken Pharmaceutical Co., Ltd.); Amine derivs. and fungicides containing the same. US 5021458 .

中间体序号	中间体编号	品名	CAS号	分子式	供应商	用于合成
(I)	27408	1-(Chloromethyl)naphthalene	86-52-2	C₁₁H₉Cl	详情	详情
(II)	40524	[4-(tert-butyl)phenyl]-N-methylmethanamine; N-[4-(tert-butyl)benzyl]-N-methylamine		C₁₂H₁₉N	详情	详情

Extended Information