Allylamine（CAS 107-11-9）中间体

应用背景（按来源药适应症）

念珠菌病阿尼芬净念珠菌血症阿尼芬净真菌感染阿尼芬净腹膜炎阿尼芬净脓肿阿尼芬净呼吸道感染阿尼芬净侵袭性念珠菌病醋酸瑞扎芬净念珠菌病醋酸瑞扎芬净念珠菌血症醋酸瑞扎芬净卡氏肺囊虫感染醋酸瑞扎芬净侵袭性真菌感染醋酸瑞扎芬净曲霉菌属感染醋酸瑞扎芬净高磷血症碳酸司维拉姆慢性肾功能不全碳酸司维拉姆肾病碳酸司维拉姆终末期肾脏病碳酸司维拉姆肾功能不全碳酸司维拉姆甲状旁腺功能亢进症碳酸司维拉姆

来源药（使用该中间体的合成路线）

品种	梯队	到期年
阿尼芬净Anidulafungin	Tier C · 观察 / 贸易	-
醋酸瑞扎芬净Rezafungin acetate	Tier C · 观察 / 贸易	-
碳酸司维拉姆Sevelamer Carbonate	Tier B · 提前布局	-

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。

阿尼芬净优化路线步数：9总收率：/

(S)-N-Boc-allylglycine→Allylamine→tert-Butyl [(2S)-1-oxo-1-[(prop-2-en-1-yl)amino]pent-4-en-2-yl]carbamate→tert-Butyl [(3S)-2-oxo-1,2,3,4-tetrahydropyridin-3-yl]carbamate→tert-Butyl [(3S,5R,6R)-5,6-dihydroxy-2-oxopiperidin-3-yl]carbamate→(4R,5R)-N2-(tert-Butoxycarbonyl)-4,5-dihydroxy-L-ornithine→(4R,5R)-N2-(tert-Butoxycarbonyl)-N5-[[(9H-fluoren-9-yl)oxy]carbonyl]-4,5-dihydroxy-L-ornithine→(4R,5R)-4,5-Bis(acetyloxy)-N2-(tert-butoxycarbonyl)-N5-[[(9H-fluoren-9-yl)oxy]carbonyl]-L-ornithine→Resin bound (4R,5R)-4,5-bis(acetyloxy)-N2-(tert-butoxycarbonyl)-N5-[[(9H-fluoren-9-yl)oxy]carbonyl]-L-ornithine→(3S,4S)-N-Fmoc-3-acetoxy-4-methyl-L-proline→Resin bound N5-[(3S,4S)-3-(acetyloxy)-1-[[(9H-fluoren-9-yl)oxy]carbonyl]-4-methyl-L-prolyl]-(4R,5R)-4,5-bis(acetyloxy)-N2-(tert-butoxycarbonyl)-L-ornithine→O-Acetyl-N-[[(9H-fluoren-9-yl)oxy]carbonyl]-L-threonine→Resin bound N5-[O-acetyl-N-[[(9H-fluoren-9-yl)oxy]carbonyl]-L-threonyl-(3S,4S)-3-(acetyloxy)-4-methyl-L-prolyl]-(4R,5R)-4,5-bis(acetyloxy)-N2-(tert-butoxycarbonyl)-L-ornithine

醋酸瑞扎芬净优化路线步数：9总收率：/

(S)-N-Boc-allylglycine→Allylamine→tert-Butyl [(2S)-1-oxo-1-[(prop-2-en-1-yl)amino]pent-4-en-2-yl]carbamate→tert-Butyl [(3S)-2-oxo-1,2,3,4-tetrahydropyridin-3-yl]carbamate→tert-Butyl [(3S,5R,6R)-5,6-dihydroxy-2-oxopiperidin-3-yl]carbamate→(4R,5R)-N2-(tert-Butoxycarbonyl)-4,5-dihydroxy-L-ornithine→(4R,5R)-N2-(tert-Butoxycarbonyl)-N5-[[(9H-fluoren-9-yl)oxy]carbonyl]-4,5-dihydroxy-L-ornithine→(4R,5R)-4,5-Bis(acetyloxy)-N2-(tert-butoxycarbonyl)-N5-[[(9H-fluoren-9-yl)oxy]carbonyl]-L-ornithine→Resin bound (4R,5R)-4,5-bis(acetyloxy)-N2-(tert-butoxycarbonyl)-N5-[[(9H-fluoren-9-yl)oxy]carbonyl]-L-ornithine→(3S,4S)-N-Fmoc-3-acetoxy-4-methyl-L-proline→Resin bound N5-[(3S,4S)-3-(acetyloxy)-1-[[(9H-fluoren-9-yl)oxy]carbonyl]-4-methyl-L-prolyl]-(4R,5R)-4,5-bis(acetyloxy)-N2-(tert-butoxycarbonyl)-L-ornithine→O-Acetyl-N-[[(9H-fluoren-9-yl)oxy]carbonyl]-L-threonine→Resin bound N5-[O-acetyl-N-[[(9H-fluoren-9-yl)oxy]carbonyl]-L-threonyl-(3S,4S)-3-(acetyloxy)-4-methyl-L-prolyl]-(4R,5R)-4,5-bis(acetyloxy)-N2-(tert-butoxycarbonyl)-L-ornithine→3(4)-(Pentyloxy)-N-[(2R,6S,9S,11R,12R,14aS,15S,16S,20S,23S,25aS)-2,11,12,15-tetrahydroxy-6,20-bis[(1R)-1-hydroxyethyl]-23-[(4S,5S)-5-(4-hydroxyphenyl)-2-phenyl-1,3,2-dioxaborolan-4-yl]-16-methyl-5,8,14,19,22,25-hexaoxotetracosahydro-1H-dipyrrolo[2,1-c:2',1'-l][1,4,7,10,13,16]hexaazacyclohenicosin-9-yl][1(1),2(1):2(4),3(1)-terphenyl]-1(4)-carboxamide

碳酸司维拉姆优化路线步数：3总收率：452 g

2-(chloromethyl)oxirane→5-((3-((4-(aminomethyl)-2-methylhexyl)amino)-2-hydroxypropyl)amino)-2-ethyl-4-methylpentan-1-aminium chloride→prop-2-en-1-amine→(E)-2,2'-(diazene-1,2-diyl)bis(2-methylpropanamide) dihydrochloride→5-((3-((4-(aminomethyl)-2-methylhexyl)amino)-2-hydroxypropyl)amino)-2-ethyl-4-methylpentan-1-aminium

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供应商	产品	价格区间	最小起订	货期	资质	操作
Qualified Partner — East China API Works	4-(4'-Pentoxy-4-biphenylyl)benzoic acid Pharmaceutical Intermediates	询价	询价	询价	—
Unibest Nantong cGMP Site	1-(Diphenylmethyl)-3-hydroxyazetidine Pharmaceutical Intermediates	询价	询价	询价	—