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阿尼芬净
Tier C · 观察 / 贸易Anidulafungin
辉瑞
原研
2006
首批上市
-
到期年（公开口径）
无销量数据
峰值销售
化学药
类型
靶点：1,3-beta-glucan synthase
商品名：Ecalta、Eraxis
适应症（已批准）：念珠菌病、念珠菌血症
各地区研发/上市状态
美国
批准上市
2006-02-17
欧盟
批准上市
2007-09-20
中国
临床一期
2019-08-08
日本
-
合成路线与中间体11 routes
原研路线 × 1优化路线（非专利）× 9工艺路线 × 1
路线按「原研路线 → 优化路线 / 工艺路线（非专利）」排序。每条路线附本站自绘的路线流程图（中间体 → 原料药）与中间体表（编号 / CAS / 英文名），可直接用于供应商开发与询价。流程图由本站依据已授权的结构化数据自行渲染，未使用任何第三方路线图。
原研Route 1步骤 4 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ANID-001 | 63619-51-2在售 | 4-bromo-4'-(pentyloxy)-1,1'-biphenyl |
| ANID-002 | 619-44-3在售 | methyl 4-iodobenzoate |
| ANID-003 | 158937-30-5在售 | methyl 4''-(pentyloxy)-[1,1':4',1''-terphenyl]-4-carboxylate |
| ANID-004 | 158938-08-0在售 | 4''-(pentyloxy)-[1,1':4',1''-terphenyl]-4-carboxylic acid |
| ANID-005 | 95-95-4在售 | 2,4,5-trichlorophenol |
| ANID-006 | 158937-65-6在售 | 2,4,5-trichlorophenyl 4''-(pentyloxy)-[1,1':4',1''-terphenyl]-4-carboxylate |
| ANID-007 | 79411-15-7在售 | (2R,6S,9S,11R,12R,14aS,15S,16S,20S,23S,25aS)-9-amino-23-((1S,2S)-1,2-dihydroxy-2-(4-hydroxyphenyl)ethyl)-2,11,12,15-tetrahydroxy-6,20-bis((R)-1-hydroxyethyl)-16-methylhexadecahydro-1H-dipyrrolo[2,1-c:2',1'-l][1,4,7,10,13,16]hexaazacyclohenicosine-5,8,14,19,22,25(9H,25aH)-hexaone |
优化Route 3步骤 6 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ANID-011 | 54651-05-7在售 | 4(R),5(R)-Dihydroxy-N2-[1-oxo-9(Z),12(Z)-octadecadienyl]-L-ornithyl-L-threonyl-4(R)-hydroxy-L-prolyl-4(S)-hydroxy-4-(4-hydroxyphenyl)-L-threonyl-L-threonyl-3(S)-hydroxy-4(S)-methyl-L-proline N-6.1-C-1.6-lactam |
| ANID-007 | 79411-15-7在售 | (2R,6S,9S,11R,12R,14aS,15S,16S,20S,23S,25aS)-9-Amino-23-[1(S),2(S)-dihydroxy-2-(4-hydroxyphenyl)ethyl]-2,11,12,15-tetrahydroxy-6,20-bis[1(R)-hydroxyethyl]-16-methylhexadecahydro-1H-dipyrrolo[2,1-c:2',1'-l][1,4,7,10,13,16]hexaazacyclohenicosine-5,8,14,19,22,25(9H,25aH)-hexone |
| ANID-006 | 158937-65-6在售 | 4''-(Pentyloxy)-p-terphenyl-4-carboxylic acid 2,4,5-trichlorophenyl ester |
| ANID-001 | 63619-51-2在售 | 4'-Bromobiphenyl-4-yl pentyl ether |
| ANID-005 | 95-95-4在售 | 2,4,5-Trichlorophenol |
| ANID-012 | 158937-25-8在售 | 4'-(Pentyloxy)biphenyl-4-ylboronic acid |
| ANID-002 | 619-44-3在售 | Methyl 4-iodobenzoate |
| ANID-003 | 158937-30-5在售 | 4''-(Pentyloxy)-p-terphenyl-4-carboxylic acid methyl ester |
| ANID-004 | 158938-08-0在售 | 4''-(Pentyloxy)-p-terphenyl-4-carboxylic acid |
优化Route 5步骤 5 · 总收率 14.6g (ANID-008)
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ANID-015 | 106-37-6在售 | 1,4-Dibromobenzene |
| ANID-016 | 4612-26-4在售 | 1,4-Phenylenediboronic acidd |
| ANID-017 | 30752-18-2在售 | 4-Bromophenyl pentyl ether |
| ANID-018 | 51934-41-9在售 | Ethyl 4-iodobenzoate |
| ANID-019 | 5798-75-4在售 | 4-Bromobenzoic acid ethyl ester |
| ANID-020 | 1448812-89-2在售 | Ethyl 4''-(pentyloxy)-1,1':4',1''-terphenyl-4-carboxylate |
| ANID-021 | 364358-99-6在售 | 4-Ethoxycarbonylphenylmagnesium bromide |
| ANID-022 | 6324-15-8在售 | 4-Bromophenyl tosylate |
| ANID-023 | 1645290-73-8在售 | Ethyl 4'-[(4-methylbenzene-1-sulfonyl)oxy][1,1'-biphenyl]-4-carboxylate |
| ANID-024 | 115171-02-3在售 | 4-Pentoxyphenylmagnesium bromide |
| ANID-004 | 158938-08-0在售 | 4''-(Pentyloxy)-p-terphenyl-4-carboxylic acid |
优化Route 6步骤 2 · 总收率 100mg (Anidulafungin)
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ANID-015 | 1903773-46-5在售 | 4,6-Dimethoxy-1,3,5-triazin-2-yl 3(4)-(pentyloxy)[1(1),2(1):2(4),3(1)-terphenyl]-1(4)-carboxylate |
| ANID-016 | 1029890-89-8在售 | (2R,6S,9S,11R,12R,14aS,15S,16S,20S,23S,25aS)-9-Amino-23-[(1S,2S)-1,2-dihydroxy-2-(4-hydroxyphenyl)ethyl]-2,11,12,15-tetrahydroxy-6,20-bis[(1R)-1-hydroxyethyl]-16-methylhexadecahydro-1H-dipyrrolo[2,1-c:2',1'-l][1,4,7,10,13,16]hexaazacyclohenicosine-5,8,14,19,22,25(9H,25aH)-hexone hydrogen chloride |
| ANID-007 | 79411-15-7在售 | (2R,6S,9S,11R,12R,14aS,15S,16S,20S,23S,25aS)-9-Amino-23-[1(S),2(S)-dihydroxy-2-(4-hydroxyphenyl)ethyl]-2,11,12,15-tetrahydroxy-6,20-bis[1(R)-hydroxyethyl]-16-methylhexadecahydro-1H-dipyrrolo[2,1-c:2',1'-l][1,4,7,10,13,16]hexaazacyclohenicosine-5,8,14,19,22,25(9H,25aH)-hexone |
| ANID-004 | 158938-08-0在售 | 4''-(Pentyloxy)-p-terphenyl-4-carboxylic acid |
优化Route 8步骤 9 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ANID-020 | 90600-20-7在售 | (S)-N-Boc-allylglycine |
| ANID-021 | 107-11-9在售 | Allylamine |
| ANID-022 | 1152110-39-8在售 | tert-Butyl [(2S)-1-oxo-1-[(prop-2-en-1-yl)amino]pent-4-en-2-yl]carbamate |
| ANID-023 | 1443528-89-9在售 | tert-Butyl [(3S)-2-oxo-1,2,3,4-tetrahydropyridin-3-yl]carbamate |
| ANID-024 | 1443528-80-0在售 | tert-Butyl [(3S,5R,6R)-5,6-dihydroxy-2-oxopiperidin-3-yl]carbamate |
| ANID-025 | - | (4R,5R)-N2-(tert-Butoxycarbonyl)-4,5-dihydroxy-L-ornithine |
| ANID-026 | - | (4R,5R)-N2-(tert-Butoxycarbonyl)-N5-[[(9H-fluoren-9-yl)oxy]carbonyl]-4,5-dihydroxy-L-ornithine |
| ANID-027 | - | (4R,5R)-4,5-Bis(acetyloxy)-N2-(tert-butoxycarbonyl)-N5-[[(9H-fluoren-9-yl)oxy]carbonyl]-L-ornithine |
| ANID-028 | - | Resin bound (4R,5R)-4,5-bis(acetyloxy)-N2-(tert-butoxycarbonyl)-N5-[[(9H-fluoren-9-yl)oxy]carbonyl]-L-ornithine |
| ANID-029 | - | (3S,4S)-N-Fmoc-3-acetoxy-4-methyl-L-proline |
| ANID-030 | - | 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 |
| ANID-031 | - | O-Acetyl-N-[[(9H-fluoren-9-yl)oxy]carbonyl]-L-threonine |
| ANID-032 | - | 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 |
优化Route 9步骤 5 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ANID-032 | - | 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 |
| ANID-033 | - | (4S)-O-Acetyl-4-(acetyloxy)-4-[4-(acetyloxy)phenyl]-N-[[(9H-fluoren-9-yl)oxy]carbonyl]-L-threonine |
| ANID-034 | - | Resin bound N5-[O-acetyl-N-[[(9H-fluoren-9-yl)methoxy]carbonyl]-L-threonyl-(4R)-4-(acetyloxy)-L-prolyl-(4S)-O-acetyl-4-(acetyloxy)-4-[4-(acetyloxy)phenyl]-L-threonyl-O-acetyl-L-threonyl-(3S,4S)-3-(acetyloxy)-4-methyl-L-prolyl]-(4R,5R)-4,5-bis(acetyloxy)-N2-(tert-butoxycarbonyl)-L-ornithine |
| ANID-035 | - | Resin bound N5-[(4S)-O-acetyl-4-(acetyloxy)-4-[4-(acetyloxy)phenyl]-N-[[(9H-fluoren-9-yl)oxy]carbonyl]-L-threonyl-O-acetyl-L-threonyl-(3S,4S)-3-(acetyloxy)-4-methyl-L-prolyl]-(4R,5R)-4,5-bis(acetyloxy)-N2-(tert-butoxycarbonyl)-L-ornithine |
| ANID-036 | 178860-12-3在售 | (4R)-4-(Acetyloxy)-1-[[(9H-fluoren-9-yl)methoxy]carbonyl]-L-proline |
| ANID-037 | - | Resin bound N5-[(4R)-4-(acetyloxy)-1-[[(9H-fluoren-9-yl)methoxy]carbonyl]-L-prolyl-(4S)-O-acetyl-4-(acetyloxy)-4-[4-(acetyloxy)phenyl]-L-threonyl-O-acetyl-L-threonyl-(3S,4S)-3-(acetyloxy)-4-methyl-L-prolyl]-(4R,5R)-4,5-bis(acetyloxy)-N2-(tert-butoxycarbonyl)-L-ornithine |
| ANID-038 | 181817-14-1在售 | O-Acetyl-N-[[(9H-fluoren-9-yl)methoxy]carbonyl]-L-threonine |
| ANID-039 | - | N5-[O-Acetyl-L-threonyl-(4R)-4-(acetyloxy)-L-prolyl-(4S)-O-acetyl-4-(acetyloxy)-4-[4-(acetyloxy)phenyl]-L-threonyl-O-acetyl-L-threonyl-(3S,4S)-3-(acetyloxy)-4-methyl-L-prolyl]-(4R,5R)-4,5-bis(acetyloxy)-N2-(tert-butoxycarbonyl)-L-ornithine |
| ANID-040 | 1443528-87-7在售 | (2R,6S,9S,11R,12R,14aS,15S,16S,20S,23S,25aS)-6,20-Bis[(1R)-1-(acetyloxy)ethyl]-9-amino-23-[(1S,2S)-1,2-bis(acetyloxy)-2-[4-(acetyloxy)phenyl]ethyl]-16-methyl-5,8,14,19,22,25-hexaoxotetracosahydro-1H-dipyrrolo[2,1-c:2',1'-l][1,4,7,10,13,16]hexaazacyclohenicosine-2,11,12,15-tetrayl tetraacetate |
优化Route 10步骤 2 · 总收率 /
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ANID-040 | 1443528-87-7在售 | (2R,6S,9S,11R,12R,14aS,15S,16S,20S,23S,25aS)-6,20-Bis[(1R)-1-(acetyloxy)ethyl]-9-amino-23-[(1S,2S)-1,2-bis(acetyloxy)-2-[4-(acetyloxy)phenyl]ethyl]-16-methyl-5,8,14,19,22,25-hexaoxotetracosahydro-1H-dipyrrolo[2,1-c:2',1'-l][1,4,7,10,13,16]hexaazacyclohenicosine-2,11,12,15-tetrayl tetraacetate |
| ANID-004 | 158938-08-0在售 | 4''-(Pentyloxy)-p-terphenyl-4-carboxylic acid |
| ANID-041 | 1443528-88-8在售 | (2R,6S,9S,11R,12R,14aS,15S,16S,20S,23S,25aS)-6,20-Bis[(1R)-1-(acetyloxy)ethyl]-23-[(1S,2S)-1,2-bis(acetyloxy)-2-[4-(acetyloxy)phenyl]ethyl]-16-methyl-5,8,14,19,22,25-hexaoxo-9-[[3(4)-(pentyloxy)[1(1),2(1):2(4),3(1)-terphenyl]-1(4)-carbonyl]amino]tetracosahydro-1H-dipyrrolo[2,1-c:2',1'-l][1,4,7,10,13,16]hexaazacyclohenicosine-2,11,12,15-tetrayl tetraacetate |
| ANID-042 | 166663-25-8在售 | (11aS,25aS)-N-[9(S)-[1(S),2(S)-Dihydroxy-2-(4-hydroxyphenyl)ethyl]-1(S),13(R),22(R),23(R)-tetrahydroxy-6(S),17(S)-bis[1(R)-hydroxyethyl]-2(S)-methyl-5,8,11,16,19,25-hexaoxoperhydrodipyrrolo[2,1-c:2',1'-l][1,4,7,10,13,16]hexaazacycloheneicosin-20(S)-yl]-4''-pentyloxy-p-terphenyl-4-carboxamide |
优化Route 11步骤 4 · 总收率 27.9g (ANID-033)
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ANID-043 | 1443528-83-3在售 | (2S,3E)-2-[[(Benzyloxy)carbonyl]amino]-4-[4-(benzyloxy)phenyl]but-3-enoic acid |
| ANID-044 | 1894196-63-4在售 | (4S)-N-[(Benzyloxy)carbonyl]-4-[4-(benzyloxy)phenyl]-4-hydroxy-L-threonine |
| ANID-045 | 106454-67-5在售 | 4(S)-Hydroxy-4-(4-hydroxyphenyl)-L-threonine |
| ANID-046 | - | (4S)-N-[[(9H-Fluoren-9-yl)oxy]carbonyl]-4-hydroxy-4-(4-hydroxyphenyl)-L-threonine |
| ANID-033 | - | (4S)-O-Acetyl-4-(acetyloxy)-4-[4-(acetyloxy)phenyl]-N-[[(9H-fluoren-9-yl)oxy]carbonyl]-L-threonine |
工艺Route 4步骤 4 · 总收率 7.6kg (Anidulafungin)
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ANID-008 | 289706-68-9在售 | 2-[4-Pentyloxyphenyl]-1,3,2-dioxaborolane |
| ANID-009 | 5731-12-4在售 | 4-(4-Iodophenyl)benzoic acid |
| ANID-013 | 2592-95-2在售 | 1H-1,2,3-Benzotriazol-1-ol |
| ANID-014 | 220115-71-9在售 | 1-(4''-(Pentyloxy)-p-terphenyl-4-ylcarbonyloxy)-1H-benzotriazole |
| ANID-007 | 79411-15-7在售 | (2R,6S,9S,11R,12R,14aS,15S,16S,20S,23S,25aS)-9-Amino-23-[1(S),2(S)-dihydroxy-2-(4-hydroxyphenyl)ethyl]-2,11,12,15-tetrahydroxy-6,20-bis[1(R)-hydroxyethyl]-16-methylhexadecahydro-1H-dipyrrolo[2,1-c:2',1'-l][1,4,7,10,13,16]hexaazacyclohenicosine-5,8,14,19,22,25(9H,25aH)-hexone |
| ANID-012 | 158937-25-8在售 | 4'-(Pentyloxy)biphenyl-4-ylboronic acid |
| ANID-002 | 619-44-3在售 | Methyl 4-iodobenzoate |
| ANID-004 | 158938-08-0在售 | 4''-(Pentyloxy)-p-terphenyl-4-carboxylic acid |
RouteRoute 2步骤 3 · 总收率 7.6kg (Anidulafungin)
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ANID-008 | 289706-68-9在售 | 2-(4-(pentyloxy)phenyl)-1,3,2-dioxaborolane |
| ANID-009 | 5731-12-4在售 | 4'-iodo-[1,1'-biphenyl]-4-carboxylic acid |
| ANID-004 | 158938-08-0在售 | 4''-(pentyloxy)-[1,1':4',1''-terphenyl]-4-carboxylic acid |
| ANID-010 | - | (1H-benzo[d][1,2,3]triazol-1-yl)(4''-(pentyloxy)-[1,1':4',1''-terphenyl]-4-yl)methanone |
| ANID-007 | 79411-15-7在售 | (2R,6S,9S,11R,12R,14aS,15S,16S,20S,23S,25aS)-9-amino-23-((1S,2S)-1,2-dihydroxy-2-(4-hydroxyphenyl)ethyl)-2,11,12,15-tetrahydroxy-6,20-bis((R)-1-hydroxyethyl)-16-methylhexadecahydro-1H-dipyrrolo[2,1-c:2',1'-l][1,4,7,10,13,16]hexaazacyclohenicosine-5,8,14,19,22,25(9H,25aH)-hexaone |
RouteRoute 7步骤 1 · 总收率 550g(ANID-004)
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ANID-017 | 619-58-9在售 | 4-Iodobenzoic acid |
| ANID-018 | 99770-93-1在售 | Cyclic bis(tetramethylethylene) ester p-Benzenediboronic acid |
| ANID-019 | 116223-55-3在售 | 1-Iodo-4-(pentyloxy)benzene |
| ANID-004 | 158938-08-0在售 | 4''-(Pentyloxy)-p-terphenyl-4-carboxylic acid |
常见问题（FAQ）
阿尼芬净的适应症有哪些？
已批准的适应症包括：念珠菌病、念珠菌血症。
阿尼芬净的专利什么时候到期？
阿尼芬净的专利到期年暂无公开口径，本页会在数据管道核实后更新。
阿尼芬净有几条合成路线？
本站收录 11 条合成路线，最短路线 1 步、总收率 550g(ANID-004)。每条路线的中间体均带登记编号与 CAS 号。
阿尼芬净的关键中间体在哪里可以采购？
阿尼芬净的多条路线中间体已挂接 CAS 档案，其中 41 个 CAS 已有优贝德（Unibest）供应网络在售报价，可在本页路线表中直接查看并询价。
如何获取阿尼芬净中间体的报价？
在本页选择目标中间体的 CAS 进入档案页，或在询价页直接提交需求；CAS 会自动带入供需撮合流程，由供应网络反馈报价。
数据来源：多源数据交叉核实（仅结构化字段） · 2026-09-24