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伏环孢素
Tier C · 观察 / 贸易Voclosporin
Aurinia
原研
2021
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：Calcineurin
商品名：Luveniq、Voclera、Orelvo、Lupkynis
适应症（已批准）：狼疮肾炎
各地区研发/上市状态
美国
批准上市
2021-01-22
欧盟
批准上市
2022-09-15
中国
临床三期
2013-10-21
日本
批准上市
2024-09-24
合成路线与中间体6 routes
原研路线 × 0优化路线（非专利）× 6工艺路线 × 0
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。
优化Route 1步骤 2 · 总收率 /
Voclosporin-00159865-13-3Voclosporin-002—Voclosporin-003—Voclosporin-004121584-52-9Voclosporin-005—API · 伏环孢素
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| Voclosporin-001 | 59865-13-3 | Cyclo{-[4-( E)-but-2-enyl- N,4-dimethyl- L-threonyl]-L-homoalanyl-(N-methylglycyl)-( N-methyl-L-leucyl)-L-valyl-( N-me-thyl- L-leucyl)-L-alanyl- D-alanyl-(N-methyl-L-leucyl)-( N-methyl-L-leucyl)-(N-methyl-L-valyl)-} |
| Voclosporin-002 | - | (1R,2R,4E)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methylhex-4-en-1-ylacetate |
| Voclosporin-003 | - | (1R,2R,4E)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methylhex-4-en-1-ylbenzoate |
| Voclosporin-004 | 121584-52-9 | Cyclo[[3(R)-acetoxy-N2,4(R)-dimethyl-6-oxo-L-norleucyl]-L-2-aminobutyryl-N-methyl-G-N-methyl-LV-N-methyl-LAa-N-methyl-L-N-methyl-L-N-methyl-V] |
| Voclosporin-005 | - | (1R,2R)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methyl-4-oxobutylbenzoate |
优化Route 2步骤 2 · 总收率 9.6g(Voclosporin (Free))
Voclosporin-004121584-52-9Voclosporin-005—Voclosporin-006—Voclosporin-007515814-02-5Voclosporin-008—Voclosporin-009—Voclosporin-010—API · 伏环孢素
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| Voclosporin-004 | 121584-52-9 | Cyclo[[3(R)-acetoxy-N2,4(R)-dimethyl-6-oxo-L-norleucyl]-L-2-aminobutyryl-N-methyl-G-N-methyl-LV-N-methyl-LAa-N-methyl-L-N-methyl-L-N-methyl-V] |
| Voclosporin-005 | - | (1R,2R)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methyl-4-oxobutylbenzoate |
| Voclosporin-006 | - | Triphenyl(prop-2-en-1-yl)phosphoniumbromide |
| Voclosporin-007 | 515814-02-5 | (1R,2R,4E)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methylhepta-4,6-dien-1-ylacetate |
| Voclosporin-008 | - | (1R,2R,4E)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methylhepta-4,6-dien-1-ylbenzoate |
| Voclosporin-009 | - | [Phenyl(prop-2-en-1-yl)phosphoroso]benzene |
| Voclosporin-010 | - | Dimethylallylphosphonate |
优化Route 3步骤 3 · 总收率 10.51g(Voclosporin (Free))
Voclosporin-011603-35-0Voclosporin-002—Voclosporin-012138957-22-9Voclosporin-013514854-23-0API · 伏环孢素
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| Voclosporin-011 | 603-35-0 | Phosphorustriphenyl |
| Voclosporin-002 | - | (1R,2R,4E)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methylhex-4-en-1-ylacetate |
| Voclosporin-012 | 138957-22-9 | (1R,2R,4E)-6-bromo-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-bis(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methylhex-4-en-1-ylacetate |
| Voclosporin-013 | 514854-23-0 | [(2E,5R,6R)-6-(acetyloxy)-6-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-bis(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-5-methylhex-2-en-1-yl]triphenylphosphoniumbromide |
优化Route 4步骤 2 · 总收率 14.09g(Voclosporin (Free))
Voclosporin-004121584-52-9Voclosporin-01479309-68-5Voclosporin-015—API · 伏环孢素
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| Voclosporin-004 | 121584-52-9 | Cyclo[[3(R)-acetoxy-N2,4(R)-dimethyl-6-oxo-L-norleucyl]-L-2-aminobutyryl-N-methyl-G-N-methyl-LV-N-methyl-LAa-N-methyl-L-N-methyl-L-N-methyl-V] |
| Voclosporin-014 | 79309-68-5 | trimethyl[(1E)-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)prop-1-en-1-yl]silane |
| Voclosporin-015 | - | (1R,2R,4R,5R)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-ethyl-14,32-diisopropyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-4-hydroxy-2-methyl-5-(trimethylsilyl)hept-6-en-1-ylacetate |
优化Route 5步骤 2 · 总收率 4.92g(Voclosporin-004)
Voclosporin-00159865-13-3Voclosporin-002—Voclosporin-004121584-52-9API · 伏环孢素
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| Voclosporin-001 | 59865-13-3 | Cyclo{-[4-( E)-but-2-enyl- N,4-dimethyl- L-threonyl]-L-homoalanyl-(N-methylglycyl)-( N-methyl-L-leucyl)-L-valyl-( N-me-thyl- L-leucyl)-L-alanyl- D-alanyl-(N-methyl-L-leucyl)-( N-methyl-L-leucyl)-(N-methyl-L-valyl)-} |
| Voclosporin-002 | - | (1R,2R,4E)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methylhex-4-en-1-ylacetate |
| Voclosporin-004 | 121584-52-9 | Cyclo[[3(R)-acetoxy-N2,4(R)-dimethyl-6-oxo-L-norleucyl]-L-2-aminobutyryl-N-methyl-G-N-methyl-LV-N-methyl-LAa-N-methyl-L-N-methyl-L-N-methyl-V] |
优化Route 6步骤 2 · 总收率 40mg(Voclosporin (Free))
Voclosporin-004121584-52-9Voclosporin-01613361-64-3Voclosporin-007515814-02-5API · 伏环孢素
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| Voclosporin-004 | 121584-52-9 | Cyclo[[3(R)-acetoxy-N2,4(R)-dimethyl-6-oxo-L-norleucyl]-L-2-aminobutyryl-N-methyl-G-N-methyl-LV-N-methyl-LAa-N-methyl-L-N-methyl-L-N-methyl-V] |
| Voclosporin-016 | 13361-64-3 | 3-(Trimethylsilyl)propyne |
| Voclosporin-007 | 515814-02-5 | (1R,2R,4E)-1-[(2S,5S,11S,14S,17S,20S,23R,26S,29S,32S)-5-Ethyl-1,7,10,16,20,23,25,28,31-nonamethyl-11,17,26,29-tetrakis(2-methylpropyl)-3,6,9,12,15,18,21,24,27,30,33-undecaoxo-14,32-di(propan-2-yl)-1,4,7,10,13,16,19,22,25,28,31-undecaazacyclotritriacontan-2-yl]-2-methylhepta-4,6-dien-1-ylacetate |
常见问题（FAQ）
伏环孢素的适应症有哪些？
已批准的适应症包括：狼疮肾炎。
伏环孢素的专利什么时候到期？
伏环孢素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。
伏环孢素有几条合成路线？
本站收录 6 条合成路线，最短路线 2 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
伏环孢素的关键中间体在哪里可以采购？
伏环孢素路线中的中间体均已建立 CAS 档案，可直接按 CAS 发起询价，需求会进入供应网络撮合池。
如何获取伏环孢素中间体的报价？
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） · 2026-10-22