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瑞舒伐他汀钙
Tier B · 提前布局Rosuvastatin Calcium
盐野义制药株式会社
原研
2002
首批上市
-
到期年（公开口径）
$7.05B ▲
峰值销售
化学药
类型
靶点：HMGCR
商品名：可定、冠脂妥、Crestor
适应症（已批准）：纯合子家族性高胆固醇血症、杂合子家族性高胆固醇血症、高脂蛋白血症Ⅲ型、动脉粥样硬化、II型高脂蛋白血症、高胆固醇血症、血脂障碍
各地区研发/上市状态
美国
批准上市
2003-08-12
欧盟
批准上市
2002-11-06
中国
批准上市
2006-12-27
日本
批准上市
2005-01-19
生产该 API 的工厂3
口径：平台供应网络（富通询价明细 + 产品主档）中登记生产该品种的工厂（在产口径），按报价活跃度排序；快照不含成本与客户信息。
已收录 3 家在产工厂名单，登录后可见（工厂信息不对未登录访客展示）。
登录查看工厂名单 →合成路线与中间体5 routes
原研路线 × 1优化路线（非专利）× 3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 10 · 总收率 162 mg
ROSU-001459-57-4ROSU-0027152-15-0ROSU-003122930-45-4ROSU-004—ROSU-005147118-27-2ROSU-006147118-28-3ROSU-007147118-30-7ROSU-008147118-37-4ROSU-009147118-35-2ROSU-010147118-38-5ROSU-011147118-39-6ROSU-012147118-40-9ROSU-013147098-18-8API · 瑞舒伐他汀钙
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ROSU-001 | 459-57-4 | 4-fluorobenzaldehyde |
| ROSU-002 | 7152-15-0 | ethyl 4-methyl-3-oxopentanoate |
| ROSU-003 | 122930-45-4 | (Z)-ethyl 2-(4-fluorobenzylidene)-4-methyl-3-oxopentanoate |
| ROSU-004 | - | (methyleneamino)(methylthio)methanamine |
| ROSU-005 | 147118-27-2 | ethyl 4-(4-fluorophenyl)-6-isopropyl-2-(methylthio)pyrimidine-5-carboxylate |
| ROSU-006 | 147118-28-3 | ethyl 4-(4-fluorophenyl)-6-isopropyl-2-(methylsulfonyl)pyrimidine-5-carboxylate |
| ROSU-007 | 147118-30-7 | ethyl 4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidine-5-carboxylate |
| ROSU-008 | 147118-37-4 | N-(4-(4-fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide |
| ROSU-009 | 147118-35-2 | methyl (R)-3-((tert-butyldimethylsilyl)oxy)-5-oxo-6-(triphenyl-l5-phosphanylidene)hexanoate |
| ROSU-010 | 147118-38-5 | methyl (R,E)-3-((tert-butyldimethylsilyl)oxy)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-5-oxohept-6-enoate |
| ROSU-011 | 147118-39-6 | methyl (R,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3-hydroxy-5-oxohept-6-enoate |
| ROSU-012 | 147118-40-9 | methyl (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate |
| ROSU-013 | 147098-18-8 | sodium (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate |
优化Route 2步骤 10 · 总收率 /
ROSU-014714963-27-6ROSU-015866088-06-4ROSU-016866088-07-5ROSU-017866088-08-6ROSU-018116563-00-9ROSU-019866114-13-8ROSU-020289042-10-0ROSU-021866088-09-7ROSU-022—ROSU-023—ROSU-024503610-43-3API · 瑞舒伐他汀钙
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ROSU-014 | 714963-27-6 | (4R,6S)-6-(chloromethyl)tetrahydro-2H-pyran-2,4-diol |
| ROSU-015 | 866088-06-4 | (2S,4R)-2-(chloromethyl)-6-methoxytetrahydro-2H-pyran-4-ol |
| ROSU-016 | 866088-07-5 | (2S,4R)-4-(benzyloxy)-2-(chloromethyl)-6-methoxytetrahydro-2H-pyran |
| ROSU-017 | 866088-08-6 | ((2S,4R)-4-(benzyloxy)-6-methoxytetrahydro-2H-pyran-2-yl)methyl acetate |
| ROSU-018 | 116563-00-9 | ((2S,4R)-4-(benzyloxy)-6-methoxytetrahydro-2H-pyran-2-yl)methanol |
| ROSU-019 | 866114-13-8 | (2S,4R)-4-(benzyloxy)-6-methoxytetrahydro-2H-pyran-2-carbaldehyde |
| ROSU-020 | 289042-10-0 | N-(5-((diphenylphosphoryl)methyl)-4-(4-fluorophenyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide |
| ROSU-021 | 866088-09-7 | N-(5-((E)-2-((2S,4R)-4-(benzyloxy)-6-methoxytetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide |
| ROSU-022 | - | N-(4-(4-fluorophenyl)-5-((E)-2-((2S,4R)-4-hydroxy-6-methoxytetrahydro-2H-pyran-2-yl)vinyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide |
| ROSU-023 | - | N-(5-((E)-2-((2S,4R)-4,6-dihydroxytetrahydro-2H-pyran-2-yl)vinyl)-4-(4-fluorophenyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide |
| ROSU-024 | 503610-43-3 | N-(4-(4-fluorophenyl)-5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide |
优化Route 3步骤 12 · 总收率 50 g
ROSU-008147118-37-4ROSU-013147098-18-8ROSU-025141942-85-0ROSU-026141942-82-7ROSU-027105876-28-6ROSU-0281644395-21-0ROSU-0291644395-22-1ROSU-030908274-86-2ROSU-03179-22-1ROSU-032908274-87-3ROSU-0331779-49-3ROSU-034908274-88-4ROSU-035676256-39-6ROSU-036615556-96-2ROSU-037355806-00-7API · 瑞舒伐他汀钙
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ROSU-008 | 147118-37-4 | N-(4-(4-fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide |
| ROSU-013 | 147098-18-8 | sodium (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate |
| ROSU-025 | 141942-85-0 | ethyl (R)-4-cyano-3-hydroxybutanoate |
| ROSU-026 | 141942-82-7 | ethyl (R)-3-((tert-butyldimethylsilyl)oxy)-4-cyanobutanoate |
| ROSU-027 | 105876-28-6 | (R)-3-((tert-butyldimethylsilyl)oxy)-4-cyanobutanoic acid |
| ROSU-028 | 1644395-21-0 | tert-butyl (R)-3-((tert-butyldimethylsilyl)oxy)-4-cyanobutanoate |
| ROSU-029 | 1644395-22-1 | tert-butyl (R)-5-amino-3-((tert-butyldimethylsilyl)oxy)-5-oxopentanoate |
| ROSU-030 | 908274-86-2 | (R)-5-(tert-butoxy)-3-((tert-butyldimethylsilyl)oxy)-5-oxopentanoic acid |
| ROSU-031 | 79-22-1 | methyl carbonochloridate |
| ROSU-032 | 908274-87-3 | (S)-(R)-5-(tert-butoxy)-3-((tert-butyldimethylsilyl)oxy)-5-oxopentanoic (ethyl carbonic) anhydride |
| ROSU-033 | 1779-49-3 | methyltriphenylphosphonium bromide |
| ROSU-034 | 908274-88-4 | tert-butyl (R)-3-((tert-butyldimethylsilyl)oxy)-5-oxo-6-(triphenyl-l5-phosphanylidene)hexanoate |
| ROSU-035 | 676256-39-6 | tert-butyl (R,E)-3-((tert-butyldimethylsilyl)oxy)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-5-oxohept-6-enoate |
| ROSU-036 | 615556-96-2 | tert-butyl (R,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3-hydroxy-5-oxohept-6-enoate |
| ROSU-037 | 355806-00-7 | tert-butyl (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxyhept-6-enoate |
优化Route 4步骤 7 · 总收率 4.38 g
ROSU-008147118-37-4ROSU-03179-22-1ROSU-0331779-49-3ROSU-03891424-40-7ROSU-0393886-69-9ROSU-040121331-25-7ROSU-04191424-38-3ROSU-0421360110-92-4ROSU-0431360110-94-6ROSU-0441456783-25-7ROSU-0451456783-26-8API · 瑞舒伐他汀钙
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ROSU-008 | 147118-37-4 | N-(4-(4-fluorophenyl)-5-formyl-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide |
| ROSU-031 | 79-22-1 | methyl carbonochloridate |
| ROSU-033 | 1779-49-3 | methyltriphenylphosphonium bromide |
| ROSU-038 | 91424-40-7 | 4-((tert-butyldimethylsilyl)oxy)dihydro-2H-pyran-2,6(3H)-dione |
| ROSU-039 | 3886-69-9在售 | (R)-1-phenylethan-1-amine |
| ROSU-040 | 121331-25-7 | (S)-3-((tert-butyldimethylsilyl)oxy)-5-oxo-5-(((R)-1-phenylethyl)amino)pentanoic acid |
| ROSU-041 | 91424-38-3 | (S)-3-((tert-butyldimethylsilyl)oxy)-5-oxo-5-(((R)-1-phenylethyl)amino)pentanoic (methyl carbonic) anhydride |
| ROSU-042 | 1360110-92-4 | (R)-3-((tert-butyldimethylsilyl)oxy)-5-oxo-N-((R)-1-phenylethyl)-6-(triphenyl-l5-phosphanylidene)hexanamide |
| ROSU-043 | 1360110-94-6 | (R,E)-3-((tert-butyldimethylsilyl)oxy)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-5-oxo-N-((R)-1-phenylethyl)hept-6-enamide |
| ROSU-044 | 1456783-25-7 | (R,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3-hydroxy-5-oxo-N-((R)-1-phenylethyl)hept-6-enamide |
| ROSU-045 | 1456783-26-8 | (3R,5S,E)-7-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)-3,5-dihydroxy-N-((R)-1-phenylethyl)hept-6-enamide |
工艺Route 5步骤 8 · 总收率 1.67 kg
ROSU-001459-57-4ROSU-020289042-10-0ROSU-024503610-43-3ROSU-04642558-54-3ROSU-04757-13-6ROSU-048488798-36-3ROSU-049488798-37-4ROSU-0501184-85-6ROSU-051289042-11-1ROSU-052147118-36-3ROSU-053799842-07-2ROSU-055172405-02-6ROSU-056—API · 瑞舒伐他汀钙
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ROSU-001 | 459-57-4 | 4-fluorobenzaldehyde |
| ROSU-020 | 289042-10-0 | N-(5-((diphenylphosphoryl)methyl)-4-(4-fluorophenyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide |
| ROSU-024 | 503610-43-3 | N-(4-(4-fluorophenyl)-5-((E)-2-((2S,4R)-4-hydroxy-6-oxotetrahydro-2H-pyran-2-yl)vinyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide |
| ROSU-046 | 42558-54-3 | methyl 4-methyl-3-oxopentanoate |
| ROSU-047 | 57-13-6 | urea |
| ROSU-048 | 488798-36-3 | methyl 4-(4-fluorophenyl)-6-isopropyl-2-oxo-1,2,3,4-tetrahydropyrimidine-5-carboxylate |
| ROSU-049 | 488798-37-4 | methyl 4-(4-fluorophenyl)-2-hydroxy-6-isopropylpyrimidine-5-carboxylate |
| ROSU-050 | 1184-85-6 | N-methylmethanesulfonamide |
| ROSU-051 | 289042-11-1 | methyl 4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidine-5-carboxylate |
| ROSU-052 | 147118-36-3 | N-(4-(4-fluorophenyl)-5-(hydroxymethyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide |
| ROSU-053 | 799842-07-2 | N-(5-(bromomethyl)-4-(4-fluorophenyl)-6-isopropylpyrimidin-2-yl)-N-methylmethanesulfonamide |
| ROSU-055 | 172405-02-6 | tert-butyl (4S,6S)-6-formyl-2,2-dimethyl-1,3-dioxane-4-carboxylate |
| ROSU-056 | - | tert-butyl (4S,6S)-6-((E)-2-(4-(4-fluorophenyl)-6-isopropyl-2-(N-methylmethylsulfonamido)pyrimidin-5-yl)vinyl)-2,2-dimethyl-1,3-dioxane-4-carboxylate |
常见问题（FAQ）
瑞舒伐他汀钙的适应症有哪些？
已批准的适应症包括：纯合子家族性高胆固醇血症、杂合子家族性高胆固醇血症、高脂蛋白血症Ⅲ型、动脉粥样硬化、II型高脂蛋白血症、高胆固醇血症、血脂障碍。
瑞舒伐他汀钙的专利什么时候到期？
瑞舒伐他汀钙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。
瑞舒伐他汀钙有几条合成路线？
本站收录 5 条合成路线，最短路线 7 步、总收率 4.38 g。每条路线的中间体均带登记编号与 CAS 号。
瑞舒伐他汀钙的关键中间体在哪里可以采购？
瑞舒伐他汀钙的多条路线中间体已挂接 CAS 档案，其中 1 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。
如何获取瑞舒伐他汀钙中间体的报价？
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