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丙酸氟替卡松
Tier C · 观察 / 贸易Fluticasone Propionate
葛兰素史克
原研
1990
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:GR、PLA2G4A
商品名:Flonase、Flutide、Flixotide/Flovent、辅舒拿、Cutivate、Flixotide、Flovent
适应症(已批准):鼻塞、过敏性鼻炎、鼻息肉、鼻炎、扁平苔藓、红疹、接触性皮炎、盘状红斑狼疮
各地区研发/上市状态
美国
批准上市
1990-12-14
欧盟
临床三期
1999-11-01
中国
批准上市
2000-06-16
日本
批准上市
2001-10-02
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 5 · 总收率 3.6 g (Fluticasone propionate)
FLUTI-00128416-82-2FLUTI-00280473-92-3FLUTI-00380474-45-9FLUTI-00480486-69-7FLUTI-00580474-67-5Fluticasone propionate90566-53-3API · 丙酸氟替卡松
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| FLUTI-001 | 28416-82-2 | (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxylic acid |
| FLUTI-002 | 80473-92-3 | (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carbothioic S-acid |
| FLUTI-003 | 80474-45-9 | (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-17-(propionyloxy)-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carbothioic S-acid |
| FLUTI-004 | 80486-69-7 | (6S,8S,9R,10S,11S,13S,14S,16R,17R)-17-(((chloromethyl)thio)carbonyl)-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl propionate |
| FLUTI-005 | 80474-67-5 | (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11-hydroxy-17-(((iodomethyl)thio)carbonyl)-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl propionate |
| Fluticasone propionate | 90566-53-3 | - |
优化Route 2步骤 6 · 总收率 83.5 g (Fluticasone propionate)
FLUTI-00128416-82-2FLUTI-00380474-45-9FLUTI-0061744-65-6FLUTI-00765429-42-7FLUTI-00816420-13-6FLUTI-009105638-31-1FLUTI-0101351451-82-5API · 丙酸氟替卡松
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| FLUTI-001 | 28416-82-2 | (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11,17-dihydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxylic acid |
| FLUTI-003 | 80474-45-9 | (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-17-(propionyloxy)-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carbothioic S-acid |
| FLUTI-006 | 1744-65-6 | (6S,8S,9R,10S,11S,13S,14S,16R,17R)-17-acetyl-6,9-difluoro-11,17-dihydroxy-10,13,16-trimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one |
| FLUTI-007 | 65429-42-7 | (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-17-(propionyloxy)-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxylic acid |
| FLUTI-008 | 16420-13-6 | dimethylcarbamothioic chloride |
| FLUTI-009 | 105638-31-1 | (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-17-(propionyloxy)-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carboxylic dimethylcarbamic thioanhydride |
| FLUTI-010 | 1351451-82-5 | 2-(((6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-17-(propionyloxy)-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carbonyl)thio)acetic acid |
优化Route 3步骤 5 · 总收率 0.041 g (Fluticasone propionate)
FLUTI-00380474-45-9FLUTI-0115292-43-3FLUTI-0121414857-52-5FLUTI-0131414857-53-6FLUTI-0141414857-54-7FLUTI-0151414857-56-9API · 丙酸氟替卡松
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| FLUTI-003 | 80474-45-9 | (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-17-(propionyloxy)-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carbothioic S-acid |
| FLUTI-011 | 5292-43-3 | tert-butyl 2-bromoacetate |
| FLUTI-012 | 1414857-52-5 | (6S,9R,10S,11S,13S,16R,17R)-17-(((2-(tert-butoxy)-2-oxoethyl)thio)carbonyl)-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl propionate |
| FLUTI-013 | 1414857-53-6 | (6S,9R,10S,11S,13S,16R,17R)-17-(((2-(tert-butoxy)-2-oxoethyl)thio)carbonyl)-6,9-difluoro-10,13,16-trimethyl-3-oxo-11-(2,2,2-trifluoroacetoxy)-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl propionate |
| FLUTI-014 | 1414857-54-7 | 2-(((6S,9R,10S,11S,13S,16R,17R)-6,9-difluoro-10,13,16-trimethyl-3-oxo-17-(propionyloxy)-11-(2,2,2-trifluoroacetoxy)-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carbonyl)thio)acetic acid |
| FLUTI-015 | 1414857-56-9 | (6S,9R,10S,11S,13S,16R,17R)-6,9-difluoro-17-(((fluoromethyl)thio)carbonyl)-10,13,16-trimethyl-3-oxo-11-(2,2,2-trifluoroacetoxy)-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-17-yl propionate |
优化Route 4步骤 2 · 总收率 0.4 g (Fluticasone propionate)
FLUTI-00380474-45-9FLUTI-0101351451-82-5FLUTI-01679-08-3API · 丙酸氟替卡松
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| FLUTI-003 | 80474-45-9 | (6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-17-(propionyloxy)-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carbothioic S-acid |
| FLUTI-010 | 1351451-82-5 | 2-(((6S,8S,9R,10S,11S,13S,14S,16R,17R)-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-3-oxo-17-(propionyloxy)-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthrene-17-carbonyl)thio)acetic acid |
| FLUTI-016 | 79-08-3 | 2-bromoacetic acid |
优化Route 5步骤 2 · 总收率 72.9 g (FLUT-015)
FLUTI-017—FLUTI-018—FLUTI-019—API · 丙酸氟替卡松
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| FLUTI-017 | - | (6S,9R,10S,11S,13S,16R,E)-6,9-difluoro-11-hydroxy-10,13,16-trimethyl-17-(1-((trimethylsilyl)oxy)ethylidene)-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one |
| FLUTI-018 | - | (6S,9R,10S,11S,13S,16R,17R)-6,9-difluoro-11,17-dihydroxy-10,13,16-trimethyl-17-(2-((trimethylsilyl)oxy)acetyl)-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one |
| FLUTI-019 | - | (6S,9R,10S,11S,13S,16R,17R)-6,9-difluoro-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13,16-trimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one |
优化Route 6步骤 6 · 总收率 254.5 mg (FLUT-027)
FLUTI-023—FLUTI-02437413-91-5FLUTI-025—FLUTI-026—FLUTI-027—FLUTI-02050-24-8FLUTI-021—FLUTI-022108-24-7API · 丙酸氟替卡松
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| FLUTI-023 | - | (Z)-1-((8S,10S,13S,14S)-10,13-dimethyl-3-oxo-7,8,12,13,15,16-hexahydro-3H-cyclopenta[a]phenanthren-17(6H,10H,14H)-ylidene)-2-oxoethyl acetate |
| FLUTI-024 | 37413-91-5 | 2-((8S,10S,13S,14S)-10,13-dimethyl-3-oxo-6,7,8,10,12,13,14,15-octahydro-3H-cyclopenta[a]phenanthren-17-yl)-2-oxoethyl acetate |
| FLUTI-025 | - | 2-((8S,9R,10S,11S,13S,14S)-9-bromo-11-(formyloxy)-10,13-dimethyl-3-oxo-6,7,8,9,10,11,12,13,14,15-decahydro-3H-cyclopenta[a]phenanthren-17-yl)-2-oxoethyl acetate |
| FLUTI-026 | - | 2-((4aS,4bS,5aS,6aS,9aS,9bS)-4a,6a-dimethyl-2-oxo-2,4a,5a,6,6a,9,9a,9b,10,11-decahydrocyclopenta[1,2]phenanthro[4,4a-b]oxiren-7-yl)-2-oxoethyl acetate |
| FLUTI-027 | - | 2-((4aS,4bS,5aS,6aS,7R,8R,9aS,9bS)-7-hydroxy-4a,6a,8-trimethyl-2-oxo-2,4a,5a,6,6a,7,8,9,9a,9b,10,11-dodecahydrocyclopenta[1,2]phenanthro[4,4a-b]oxiren-7-yl)-2-oxoethyl acetate |
| FLUTI-020 | 50-24-8 | (8S,9S,10R,11S,13S,14S,17R)-11,17-dihydroxy-17-(2-hydroxyacetyl)-10,13-dimethyl-6,7,8,9,10,11,12,13,14,15,16,17-dodecahydro-3H-cyclopenta[a]phenanthren-3-one |
| FLUTI-021 | - | (Z)-2-((8S,10S,13S,14S)-10,13-dimethyl-3-oxo-7,8,12,13,15,16-hexahydro-3H-cyclopenta[a]phenanthren-17(6H,10H,14H)-ylidene)-2-hydroxyacetaldehyde |
| FLUTI-022 | 108-24-7 | acetic anhydride |
常见问题(FAQ)
丙酸氟替卡松的适应症有哪些?
已批准的适应症包括:鼻塞、过敏性鼻炎、鼻息肉、鼻炎、扁平苔藓、红疹、接触性皮炎、盘状红斑狼疮。
丙酸氟替卡松的专利什么时候到期?
丙酸氟替卡松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。
丙酸氟替卡松有几条合成路线?
本站收录 6 条合成路线,最短路线 2 步、总收率 0.4 g (Fluticasone propionate)。每条路线的中间体均带登记编号与 CAS 号。
丙酸氟替卡松的关键中间体在哪里可以采购?
丙酸氟替卡松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。
如何获取丙酸氟替卡松中间体的报价?
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) · 2026-09-27