1,4-Epoxy-1,3-butadiene（CAS 110-00-9）中间体

应用背景（按来源药适应症）

心脏和血管疾病阿托伐他汀/氢氯噻嗪/阿司匹林/依那普利高血压阿托伐他汀/氢氯噻嗪/阿司匹林/依那普利高脂血症阿托伐他汀/氢氯噻嗪/阿司匹林/依那普利心脏病阿托伐他汀/氢氯噻嗪/阿司匹林/依那普利高脂血症阿托伐他汀锶蛛网膜下腔出血阿托伐他汀锶高血压阿托伐他汀锶不宁腿综合征罗替高汀帕金森病罗替高汀物质相关性障碍罗替高汀药物相关的副作用和不良反应罗替高汀组织粘连罗替高汀术后疼痛罗替高汀

来源药（使用该中间体的合成路线）

品种	梯队	到期年
阿托伐他汀/氢氯噻嗪/阿司匹林/依那普利Atorvastatin/Hydrochlorothiazide/Aspirin/Enalapril	Tier C · 观察 / 贸易	-
阿托伐他汀锶Atorvastatin strontium	Tier C · 观察 / 贸易	-
罗替高汀Rotigotine	Tier C · 观察 / 贸易	-

合成路线中的位置（上下游链）

按路线登记顺序排列，左→右为合成方向；高亮为当前 CAS，其余可点击跳转对应档案。

阿托伐他汀/氢氯噻嗪/阿司匹林/依那普利优化路线步数：11总收率：25g(Atorvastatin-017)

1,4-Epoxy-1,3-butadiene→(2E)-1,1,4,4-Tetramethoxybut-2-ene→2,2-Dimethoxyacetaldehyde→Nitrocarbol→tert-Butyl 4-bromo-3-oxobutanoate→1,1-Dimethoxy-3-nitropropan-2-ol→(1E)-3,3-Dimethoxy-1-nitroprop-1-ene→(2E)-3-Nitroprop-2-enal→Bromido(4-tert-butoxy-2,4-dioxobutyl)zinc→tert-Butyl (5S,6E)-5-hydroxy-7-nitro-3-oxohept-6-enoate→4-Methylene-2-oxetanone→tert-Butyl (3R,5S,6E)-3,5-dihydroxy-7-nitrohept-6-enoate→2-Propanone→tert-Butyl [(4R,6S)-2,2-dimethyl-6-[(E)-2-nitroethenyl]-1,3-dioxan-4-yl]acetate→(4R,6R)-6-(2-Aminoethyl)-2,2-dimethyl-1,3-Dioxane-4-acetic acid 1,1-dimethylethyl ester

阿托伐他汀锶优化路线步数：11总收率：25g(Atorvastatin-017)

1,4-Epoxy-1,3-butadiene→(2E)-1,1,4,4-Tetramethoxybut-2-ene→2,2-Dimethoxyacetaldehyde→Nitrocarbol→tert-Butyl 4-bromo-3-oxobutanoate→1,1-Dimethoxy-3-nitropropan-2-ol→(1E)-3,3-Dimethoxy-1-nitroprop-1-ene→(2E)-3-Nitroprop-2-enal→Bromido(4-tert-butoxy-2,4-dioxobutyl)zinc→tert-Butyl (5S,6E)-5-hydroxy-7-nitro-3-oxohept-6-enoate→4-Methylene-2-oxetanone→tert-Butyl (3R,5S,6E)-3,5-dihydroxy-7-nitrohept-6-enoate→2-Propanone→tert-Butyl [(4R,6S)-2,2-dimethyl-6-[(E)-2-nitroethenyl]-1,3-dioxan-4-yl]acetate→(4R,6R)-6-(2-Aminoethyl)-2,2-dimethyl-1,3-Dioxane-4-acetic acid 1,1-dimethylethyl ester

罗替高汀优化路线步数：9总收率：128 mg

2-(thiophen-2-yl)ethyl 4-methylbenzenesulfonate→(S)-6-(propylamino)-5,6,7,8-tetrahydronaphthalen-1-ol→1-chloro-3-methoxybenzene→furan→5-methoxy-1,4-dihydro-1,4-epoxynaphthalene→N-benzylpropan-1-amine→(1S,2S)-2-(benzyl(propyl)amino)-5-methoxy-1,2-dihydronaphthalen-1-ol→(1S,2S)-2-(benzyl(propyl)amino)-5-methoxy-1,2,3,4-tetrahydronaphthalen-1-ol→(1S,2S)-5-methoxy-2-(propylamino)-1,2,3,4-tetrahydronaphthalen-1-ol→tert-butyl ((1S,2S)-1-hydroxy-5-methoxy-1,2,3,4-tetrahydronaphthalen-2-yl)(propyl)carbamate→(3aS,9bR)-6-methoxy-3-propyl-3a,4,5,9b-tetrahydronaphtho[2,1-d]oxazol-2(3H)-one→(S)-5-methoxy-N-propyl-1,2,3,4-tetrahydronaphthalen-2-amine

本站可供应的对应中间体

同 CAS 多家在售供应横向对比；价格区间为供应方挂牌口径，实价以询价确认为准。

供应商	产品	价格区间	最小起订	货期	资质
Qualified Partner — East China API Works	5-Methoxy-2-tetralone Pharmaceutical Intermediates	询价	询价	询价	—
Unibest Nantong cGMP Site	(S)-2-AMINO-5-METHOXYTETRALIN HYDROCHLORIDE Pharmaceutical Intermediates	询价	询价	询价	—
Unibest Taizhou GMP-like Site	(S)-2-Amino-5-methoxytetralin Hydrochloride Pharmaceutical Intermediates	询价	询价	询价	—
Qualified Partner — East China API Works	(S)-1,2,3,4-Tetrahydro-5-methoxy-N-propyl-2-naphthalenamine hydrochloride Pharmaceutical Intermediates	询价	询价	询价	—
Unibest Nantong cGMP Site	(S)-2-Amino-5-methoxytetralin (S)-mandelate Pharmaceutical Intermediates	询价	询价	询价	—