rivaroxaban
Xarelto · Bayer / J&J · DOAC 抗凝
明确不做（太卷）门槛 2.5/5
- US LOE
- 2026 (EU)
- 备注
- —
- 准备期
- 0 年
- 年销售
- ~$7B
- 关键中间体
- 1 个
门槛构成
卷度最高EU 已到期
明确不做
2026 EU 已到期，DMF/产能高度饱和，卷度最高。
关键中间体链
本目录已覆盖 0/1利伐沙班胺（446292-10-0）446292-10-0 ✓ 药渡核验药渡节点 RIVA-048
报价成熟，已卷
依据：RIVA-048 = (S)-4-(4-(5-(aminomethyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one，即利伐沙班的噁唑烷酮-苄胺关键中间体；CAS 与片段名自带值一致，且已由药渡路线数据二次确认
未在目录中匹配 → 潜在新增供应机会
药渡合成路线 · 中间体全表仅结构化数据（编号 / CAS / 分子式），路线由本站自行渲染
6 条路线 · 48 个节点 · 去重 CAS 46 个利伐沙班RivaroxabandrugId 71237064568445696785
原研路线 · 9 步 · 总收率 2.00% · 文献 WO2013053739A1 / WO2014155259A2优化路线 · 6 步 · 总收率 23.7 g · 文献 WO2004060887A1 / US8106192B2优化路线 · 9 步 · 总收率 79 mg · 文献 WO2011080341A1 / US2012283434A1优化路线 · 5 步 · 总收率 3.34 g · 文献 WO2013046211A1 / US6362334B1优化路线 · 9 步 · 总收率 2.25 g · 文献 WO2013105100A1优化路线 · 6 步 · 文献 WO2014170908A1
| 编号 | CAS 号 | 分子式 | 分子量 | 英文名 / 结构描述 |
|---|---|---|---|---|
| RIVA-001 | 141-43-5 | C2H7NO | 61.08 | 2-aminoethan-1-ol |
| RIVA-002 | 79-04-9 | C2H2Cl2O | 112.94 | 2-chloroacetyl chloride |
| RIVA-003 | 药渡未登记 | C6H9Cl2NO3 | 214.05 | 2-(2-chloroacetamido)ethyl 2-chloroacetate |
| RIVA-004 | 6320-16-7 | C4H8ClNO2 | 137.56 | 2-chloro-N-(2-hydroxyethyl)acetamide |
| RIVA-005 | 109-11-5 | C4H7NO2 | 101.1 | morpholin-3-one |
| RIVA-006 | 350-46-9 | C6H4FNO2 | 141.1 | 1-fluoro-4-nitrobenzene |
| RIVA-007 | 446292-04-2 | C10H10N2O4 | 222.2 | 4-(4-nitrophenyl)morpholin-3-one |
| RIVA-008 | 438056-69-0 | C10H12N2O2 | 192.21 | 4-(4-aminophenyl)morpholin-3-one |
| RIVA-009 | 161596-47-0 | C11H9NO3 | 203.19 | (S)-2-(oxiran-2-ylmethyl)isoindoline-1,3-dione |
| RIVA-010 | 446292-07-5 | C21H21N3O5 | 395.41 | (R)-2-(2-hydroxy-3-((4-(3-oxomorpholino)phenyl)amino)propyl)isoindoline-1,3-dione |
| RIVA-011 | 446292-08-6 | C22H19N3O6 | 421.4 | (S)-2-((2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidin-5-yl)methyl)isoindoline-1,3-dione |
| RIVA-012 | 1430407-73-0 | C16H19N3O8 | 381.34 | (S)-4-(4-(5-(aminomethyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one oxalate |
| RIVA-013 | 42518-98-9 | C5H2Cl2OS | 181.04 | 5-chlorothiophene-2-carbonyl chloride |
| RIVA-014 | 7283-96-7 | C5H3ClOS | 146.59 | 5-chlorothiophene-2-carbaldehyde |
| RIVA-015 | 24065-33-6 | C5H3ClO2S | 162.59 | 5-chlorothiophene-2-carboxylic acid |
| RIVA-016 | 209849-99-0 | C3H10ClNO2 | 127.57 | (S)-3-aminopropane-1,2-diol hydrochloride |
| RIVA-017 | 721401-51-0 | C8H10ClNO3S | 235.69 | (S)-5-chloro-N-(2,3-dihydroxypropyl)thiophene-2-carboxamide |
| RIVA-018 | 721401-52-1 | C8H9BrClNO2S | 298.58 | (S)-N-(3-bromo-2-hydroxypropyl)-5-chlorothiophene-2-carboxamide |
| RIVA-019 | 721401-53-2 | C18H20ClN3O4S | 409.89 | (R)-5-chloro-N-(2-hydroxy-3-((4-(3-oxomorpholino)phenyl)amino)propyl)thiophene-2-carboxamide |
| RIVA-020 | 122-98-5 | C8H11NO | 137.18 | 2-(phenylamino)ethan-1-ol |
| RIVA-021 | 29518-11-4 | C10H11NO2 | 177.2 | 4-phenylmorpholin-3-one |
| RIVA-022 | 501-53-1 | C8H7ClO2 | 170.59 | benzyl carbonochloridate |
| RIVA-023 | 1313613-18-1 | C18H18N2O4 | 326.35 | benzyl (4-(3-oxomorpholino)phenyl)carbamate |
| RIVA-024 | 60456-26-0 | C7H12O3 | 144.17 | (R)-oxiran-2-ylmethyl butyrate |
| RIVA-025 | 1117893-60-3 | C14H16N2O5 | 292.29 | (R)-4-(4-(5-(hydroxymethyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one |
| RIVA-026 | 1117893-61-4 | C15H18N2O7S | 370.38 | (R)-(2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidin-5-yl)methyl methanesulfonate |
| RIVA-027 | 75-64-9 | C4H11N | 73.14 | 2-methylpropan-2-amine |
| RIVA-028 | 1313613-19-2 | C18H25N3O4 | 347.41 | (S)-4-(4-(5-((tert-butylamino)methyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one |
| RIVA-029 | 1313613-21-6 | C23H26ClN3O5S | 491.99 | (S)-N-(tert-butyl)-5-chloro-N-((2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidin-5-yl)methyl)thiophene-2-carboxamide |
| RIVA-030 | 67843-74-7 | C3H5ClO | 92.52 | (S)-2-(chloromethyl)oxirane |
| RIVA-031 | 100-52-7 | C7H6O | 106.12 | benzaldehyde |
| RIVA-032 | 224323-52-8 | C10H12ClNO | 197.66 | (S,E)-1-(benzylideneamino)-3-chloropropan-2-ol |
| RIVA-033 | 34839-13-9 | C3H9Cl2NO | 146.02 | (S)-1-amino-3-chloropropan-2-ol hydrochloride |
| RIVA-034 | 1384257-81-1 | C8H9Cl2NO2S | 254.13 | (S)-5-chloro-N-(3-chloro-2-hydroxypropyl)thiophene-2-carboxamide |
| RIVA-035 | 药渡未登记 | C10H11Cl2NO3S | 296.17 | (S)-1-chloro-3-(5-chlorothiophene-2-carboxamido)propan-2-yl acetate |
| RIVA-036 | 16495-04-8 | C17H20O5S | 336.4 | (S)-3-(benzyloxy)-2-hydroxypropyl 4-methylbenzenesulfonate |
| RIVA-037 | 1018979-25-3 | C19H22O6S | 378.44 | (S)-1-(benzyloxy)-3-(tosyloxy)propan-2-yl acetate |
| RIVA-038 | 1447919-68-7 | C22H26N2O5 | 398.45 | (R)-1-(benzyloxy)-3-((4-(3-oxomorpholino)phenyl)amino)propan-2-yl acetate |
| RIVA-039 | 1447919-69-8 | C23H25ClN2O6 | 460.91 | (R)-1-(benzyloxy)-3-((chlorocarbonyl)(4-(3-oxomorpholino)phenyl)amino)propan-2-yl acetate |
| RIVA-040 | 1117893-59-0 | C21H22N2O5 | 382.41 | (R)-4-(4-(5-((benzyloxy)methyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one |
| RIVA-041 | 1424942-80-2 | C21H22N2O7S | 446.47 | (R)-(2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidin-5-yl)methyl 4-methylbenzenesulfonate |
| RIVA-042 | 1424942-78-8 | C21H23N3O4 | 381.43 | (S)-4-(4-(5-((benzylamino)methyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one |
| RIVA-043 | 1429333-90-3 | C26H24ClN3O5S | 526.0 | (S)-N-benzyl-5-chloro-N-((2-oxo-3-(4-(3-oxomorpholino)phenyl)oxazolidin-5-yl)methyl)thiophene-2-carboxamide |
| RIVA-044 | 681225-50-3 | C3H6ClN3O | 135.55 | (S)-1-azido-3-chloropropan-2-ol |
| RIVA-045 | 127182-48-3 | C3H5N3O | 99.09 | (S)-2-(azidomethyl)oxirane |
| RIVA-046 | 1429334-05-3 | C13H17N5O3 | 291.31 | (R)-4-(4-((3-azido-2-hydroxypropyl)amino)phenyl)morpholin-3-one |
| RIVA-047 | 1349248-79-8 | C14H15N5O4 | 317.3 | (R)-4-(4-(5-(azidomethyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one |
| RIVA-048 | 446292-10-0 | C14H17N3O4 | 291.3 | (S)-4-(4-(5-(aminomethyl)-2-oxooxazolidin-3-yl)phenyl)morpholin-3-one |
数据来源：药渡（Pharmacodia）授权账号，仅取结构化字段；本方未使用药渡的路线图（webImg）—— 其图形带水印，属第三方著作权内容，转载需授权。本表由本站依据数据自行渲染。 标注「药渡未登记」者，为药渡该节点 CAS 字段为空，非本站遗漏。
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准备期 0 年 · 不足 3 年
US LOE 2026 (EU)
市场关 · 峰值销售可进
≈$7B · 优先档（≥$3B）
公开口径 ~$7B
供给关 · 稀缺程度不进
供给拥挤 · 明确不做
梯队判定：明确不做（太卷）
技术关 · 门槛不进
门槛 2.5/5 · 不足
卷度最高 · EU 已到期
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