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依普利酮
Tier C · 观察 / 贸易Eplerenone
辉瑞
原研
2002
首批上市
-
到期年（公开口径）
$0.23B ▲
峰值销售
化学药
类型
靶点：MR
商品名：Selara、Inspra、EPLERENONEANDA、Elecor
适应症（已批准）：高血压、心脏衰竭
各地区研发/上市状态
美国
批准上市
2002-09-27
欧盟
临床二期
2007-01-01
中国
批准上市
2021-04-09
日本
批准上市
2007-07-31
合成路线与中间体5 routes
原研路线 × 1优化路线（非专利）× 4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。
原研Route 1步骤 6 · 总收率 44.3 g
EPLE-001192569-17-8EPLE-00275-86-5EPLE-003192704-52-2EPLE-004192704-54-4EPLE-005192704-56-6EPLE-006192704-58-8EPLE-00795716-70-4API · 依普利酮
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EPLE-001 | 192569-17-8 | (10R,11R,13S,17R)-11-hydroxy-10,13-dimethyl-1,3',4',8,9,10,11,12,13,14,15,16-dodecahydro-5'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2H)-dione |
| EPLE-002 | 75-86-5 | 2-hydroxy-2-methylpropanenitrile |
| EPLE-003 | 192704-52-2 | (2R,5'R,7'R,10'R,11'R,13'S)-18'-amino-11'-hydroxy-10',13'-dimethyl-3',5-dioxo-1',2',3',4,5,6',7',8',9',10',11',12',13',14',15',16'-hexadecahydro-3H,5'H-spiro[furan-2,17'-[4,7](metheno)cyclopenta[a]phenanthrene]-5'-carbonitrile |
| EPLE-004 | 192704-54-4 | (2R,5'S,7'R,10'R,11'R,13'S)-11'-hydroxy-10',13'-dimethyl-3',5,18'-trioxohexadecahydro-3H-spiro[furan-2,17'-[4,7]methanocyclopenta[a]phenanthrene]-5'(2'H)-carbonitrile |
| EPLE-005 | 192704-56-6 | methyl (7R,10R,11R,13S,17R)-11-hydroxy-10,13-dimethyl-3,5'-dioxo-1,2,3,4',5',6,7,8,9,10,11,12,13,14,15,16-hexadecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-7-carboxylate |
| EPLE-006 | 192704-58-8 | methyl (7R,10R,11R,13S,17R)-10,13-dimethyl-11-((methylsulfonyl)oxy)-3,5'-dioxo-1,2,3,4',5',6,7,8,9,10,11,12,13,14,15,16-hexadecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-7-carboxylate |
| EPLE-007 | 95716-70-4 | methyl (7R,10S,13S,17R)-10,13-dimethyl-3,5'-dioxo-1,2,3,4',5',6,7,8,10,12,13,14,15,16-tetradecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-7-carboxylate |
优化Route 2步骤 5 · 总收率 7.45 g
EPLE-00795716-70-4EPLE-00895716-71-5EPLE-00995716-72-6EPLE-010188988-15-0EPLE-01195716-74-8API · 依普利酮
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EPLE-007 | 95716-70-4 | methyl (7R,10S,13S,17R)-10,13-dimethyl-3,5'-dioxo-1,2,3,4',5',6,7,8,10,12,13,14,15,16-tetradecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-7-carboxylate |
| EPLE-008 | 95716-71-5 | (10R,13S,17R)-10,13-dimethyl-1,3',4',8,10,12,13,14,15,16-decahydro-5'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2H)-dione |
| EPLE-009 | 95716-72-6 | (7R,10S,13S,17R)-10,13-dimethyl-3,5'-dioxo-1,2,3,4',5',6,7,8,10,12,13,14,15,16-tetradecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-7-carbonitrile |
| EPLE-010 | 188988-15-0 | (7R,10S,13S,17R)-3-hydroxy-10,13-dimethyl-5'-oxo-1,2,3,4',5',6,7,8,10,12,13,14,15,16-tetradecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-7-carbaldehyde |
| EPLE-011 | 95716-74-8 | (7R,10S,13S,17R)-10,13-dimethyl-3,5'-dioxo-1,2,3,4',5',6,7,8,10,12,13,14,15,16-tetradecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-7-carboxylic acid |
优化Route 3步骤 7 · 总收率 /
EPLE-00795716-70-4EPLE-00895716-71-5EPLE-01195716-74-8EPLE-012534-22-5EPLE-013610785-40-5EPLE-014109-53-5EPLE-015610785-41-6EPLE-016—EPLE-017610785-45-0API · 依普利酮
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EPLE-007 | 95716-70-4 | methyl (7R,10S,13S,17R)-10,13-dimethyl-3,5'-dioxo-1,2,3,4',5',6,7,8,10,12,13,14,15,16-tetradecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-7-carboxylate |
| EPLE-008 | 95716-71-5 | (10R,13S,17R)-10,13-dimethyl-1,3',4',8,10,12,13,14,15,16-decahydro-5'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2H)-dione |
| EPLE-011 | 95716-74-8 | (7R,10S,13S,17R)-10,13-dimethyl-3,5'-dioxo-1,2,3,4',5',6,7,8,10,12,13,14,15,16-tetradecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-7-carboxylic acid |
| EPLE-012 | 534-22-5 | 2-methylfuran |
| EPLE-013 | 610785-40-5 | (7R,8R,10S,13S,14S,17R)-10,13-dimethyl-7-(5-methylfuran-2-yl)-1,3',4',6,7,8,10,12,13,14,15,16-dodecahydro-5'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2H)-dione |
| EPLE-014 | 109-53-5 | 2-methyl-1-(vinyloxy)propane |
| EPLE-015 | 610785-41-6 | (7R,8R,10S,13S,14S,17R)-10,13-dimethyl-7-((E)-4-oxopent-2-enoyl)-1,3',4',6,7,8,10,12,13,14,15,16-dodecahydro-5'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2H)-dione |
| EPLE-016 | - | (7R,8R,10S,13S,14S,17R)-7-(2-hydroxy-2-methoxyacetyl)-10,13-dimethyl-1,3',4',6,7,8,10,12,13,14,15,16-dodecahydro-5'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2H)-dione |
| EPLE-017 | 610785-45-0 | (1'R,2R,3a'R,7a'R,9a'S,12a'S,12b'R)-7a',9a'-dimethyl-1',3,4,6',7',7a',9',9a',11',12',12a',12b'-dodecahydro-2'H,5H-spiro[furan-2,10'-[1,3a]methanobenzo[b]indeno[5,4-d]oxepine]-2',5,5'(4'H)-trione |
优化Route 4步骤 5 · 总收率 /
EPLE-001192569-17-8EPLE-00895716-71-5EPLE-017610785-45-0EPLE-018209253-91-8EPLE-0191263102-65-3EPLE-020115464-59-0EPLE-0211263102-67-5API · 依普利酮
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EPLE-001 | 192569-17-8 | (10R,11R,13S,17R)-11-hydroxy-10,13-dimethyl-1,3',4',8,9,10,11,12,13,14,15,16-dodecahydro-5'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2H)-dione |
| EPLE-008 | 95716-71-5 | (10R,13S,17R)-10,13-dimethyl-1,3',4',8,10,12,13,14,15,16-decahydro-5'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2H)-dione |
| EPLE-017 | 610785-45-0 | (1'R,2R,3a'R,7a'R,9a'S,12a'S,12b'R)-7a',9a'-dimethyl-1',3,4,6',7',7a',9',9a',11',12',12a',12b'-dodecahydro-2'H,5H-spiro[furan-2,10'-[1,3a]methanobenzo[b]indeno[5,4-d]oxepine]-2',5,5'(4'H)-trione |
| EPLE-018 | 209253-91-8 | (10R,11R,13S,17R)-10,13-dimethyl-3,5'-dioxo-1,2,3,4',5',8,9,10,11,12,13,14,15,16-tetradecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-11-yl methanesulfonate |
| EPLE-019 | 1263102-65-3 | (1'R,2R,3a'R,7a'R,9a'S)-7a',9a'-dimethyl-1',3,4,6',7',7a',9',9a',11',12',12a',12b'-dodecahydro-2'H,5H-spiro[furan-2,10'-[1,3a]methanobenzo[b]indeno[5,4-d]oxepine]-5,5'(4'H)-dione |
| EPLE-020 | 115464-59-0 | 3-methyl-3-(trifluoromethyl)dioxirane |
| EPLE-021 | 1263102-67-5 | (1'R,2R,2'S,3a'R,7a'R,9a'S)-2'-hydroxy-7a',9a'-dimethyl-1',3,4,6',7',7a',9',9a',11',12',12a',12b'-dodecahydro-2'H,5H-spiro[furan-2,10'-[1,3a]methanobenzo[b]indeno[5,4-d]oxepine]-5,5'(4'H)-dione |
优化Route 5步骤 6 · 总收率 3.06 g
EPLE-001192569-17-8EPLE-005192704-56-6EPLE-006192704-58-8EPLE-00795716-70-4EPLE-0221398078-03-9EPLE-023209253-72-5API · 依普利酮
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| EPLE-001 | 192569-17-8 | (10R,11R,13S,17R)-11-hydroxy-10,13-dimethyl-1,3',4',8,9,10,11,12,13,14,15,16-dodecahydro-5'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2H)-dione |
| EPLE-005 | 192704-56-6 | methyl (7R,10R,11R,13S,17R)-11-hydroxy-10,13-dimethyl-3,5'-dioxo-1,2,3,4',5',6,7,8,9,10,11,12,13,14,15,16-hexadecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-7-carboxylate |
| EPLE-006 | 192704-58-8 | methyl (7R,10R,11R,13S,17R)-10,13-dimethyl-11-((methylsulfonyl)oxy)-3,5'-dioxo-1,2,3,4',5',6,7,8,9,10,11,12,13,14,15,16-hexadecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-7-carboxylate |
| EPLE-007 | 95716-70-4 | methyl (7R,10S,13S,17R)-10,13-dimethyl-3,5'-dioxo-1,2,3,4',5',6,7,8,10,12,13,14,15,16-tetradecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-7-carboxylate |
| EPLE-022 | 1398078-03-9 | (7R,8R,9S,10R,11R,13S,14S,17R)-11-hydroxy-10,13-dimethyl-7-(nitromethyl)-1,3',4',6,7,8,9,10,11,12,13,14,15,16-tetradecahydro-5'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-3,5'(2H)-dione |
| EPLE-023 | 209253-72-5 | (7R,8S,9S,10R,11R,13S,14S,17R)-11-hydroxy-10,13-dimethyl-3,5'-dioxo-1,2,3,4',5',6,7,8,9,10,11,12,13,14,15,16-hexadecahydro-3'H-spiro[cyclopenta[a]phenanthrene-17,2'-furan]-7-carboxylic acid |
常见问题（FAQ）
依普利酮的适应症有哪些？
已批准的适应症包括：高血压、心脏衰竭。
依普利酮的专利什么时候到期？
依普利酮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。
依普利酮有几条合成路线？
本站收录 5 条合成路线，最短路线 5 步、总收率 7.45 g。每条路线的中间体均带登记编号与 CAS 号。
依普利酮的关键中间体在哪里可以采购？
依普利酮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。
如何获取依普利酮中间体的报价？
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） · 2026-10-04