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艾托格列净
Tier C · 观察 / 贸易Ertugliflozin
辉瑞
原研
2017
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:SGLT2
商品名:捷诺妥、Steglatro
适应症(已批准):二型糖尿病
各地区研发/上市状态
美国
批准上市
2017-12-19
欧盟
批准上市
2018-03-21
中国
批准上市
2020-07-29
日本
-
合成路线与中间体4 routes
原研路线 × 1优化路线(非专利)× 2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 13 · 总收率 60 mg

| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ERTU-001 | 2280-44-6在售 | (3R,4S,5S,6R)-6-(hydroxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetraol |
| ERTU-002 | 54606-68-7在售 | ((2R,3R,4S,5R)-6-(allyloxy)-3,4,5-tris(benzyloxy)tetrahydro-2H-pyran-2-yl)methanol |
| ERTU-003 | 1210344-25-4在售 | ((3S,4S,5R)-6-(allyloxy)-3,4,5-tris(benzyloxy)tetrahydro-2H-pyran-2,2-diyl)dimethanol |
| ERTU-004 | 2746-25-0在售 | 1-(bromomethyl)-4-methoxybenzene |
| ERTU-005 | 1210344-28-7在售 | (3S,4S,5R)-6-(allyloxy)-3,4,5-tris(benzyloxy)-2,2-bis(((4-methoxybenzyl)oxy)methyl)tetrahydro-2H-pyran |
| ERTU-006 | 1210344-29-8在售 | (3R,4S,5S)-3,4,5-tris(benzyloxy)-6,6-bis(((4-methoxybenzyl)oxy)methyl)tetrahydro-2H-pyran-2-ol |
| ERTU-007 | 1210344-30-1在售 | (3R,4S,5S)-3,4,5-tris(benzyloxy)-6,6-bis(((4-methoxybenzyl)oxy)methyl)tetrahydro-2H-pyran-2-one |
| ERTU-008 | 6638-79-5在售 | N,O-dimethylhydroxylamine hydrochloride |
| ERTU-009 | 1210344-31-2在售 | (2R,3S,4S)-2,3,4-tris(benzyloxy)-5-hydroxy-N-methoxy-6-((4-methoxybenzyl)oxy)-5-(((4-methoxybenzyl)oxy)methyl)-N-methylhexanamide |
| ERTU-010 | 461432-23-5在售 | 4-bromo-1-chloro-2-(4-ethoxybenzyl)benzene |
| ERTU-011 | 1210344-39-0在售 | (4S,5S)-3,4,5-tris(benzyloxy)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6,6-bis(((4-methoxybenzyl)oxy)methyl)tetrahydro-2H-pyran-2-ol |
| ERTU-012 | 1210763-25-9在售 | ((2S,3S)-2,3,4-tris(benzyloxy)-5-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6,8-dioxabicyclo[3.2.1]octan-1-yl)methanol |
优化Route 3步骤 16 · 总收率 491 mg

| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ERTU-019 | 14131-84-1在售 | (3aS,4S,6R,6aS)-6-((R)-2,2-dimethyl-1,3-dioxolan-4-yl)-2,2-dimethyltetrahydrofuro[3,4-d][1,3]dioxol-4-ol |
| ERTU-020 | 108678-46-2在售 | tert-butyl(((3aS,4R,6R,6aS)-6-((R)-2,2-dimethyl-1,3-dioxolan-4-yl)-2,2-dimethyltetrahydrofuro[3,4-d][1,3]dioxol-4-yl)oxy)dimethylsilane |
| ERTU-021 | 111000-75-0在售 | (R)-1-((3aS,4R,6R,6aS)-6-((tert-butyldimethylsilyl)oxy)-2,2-dimethyltetrahydrofuro[3,4-d][1,3]dioxol-4-yl)ethane-1,2-diol |
| ERTU-022 | 111000-76-1在售 | (3aS,4S,6R,6aS)-6-((tert-butyldimethylsilyl)oxy)-2,2-dimethyltetrahydrofuro[3,4-d][1,3]dioxole-4-carbaldehyde |
| ERTU-023 | 1233481-95-2在售 | 2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-1,3-dithiane |
| ERTU-024 | 1233481-96-3在售 | (R)-((3aS,4R,6R,6aS)-6-((tert-butyldimethylsilyl)oxy)-2,2-dimethyltetrahydrofuro[3,4-d][1,3]dioxol-4-yl)(2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-1,3-dithian-2-yl)methanol |
| ERTU-025 | 1233481-98-5在售 | (3aS,4S,6R,6aS)-6-((R)-(2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-1,3-dithian-2-yl)(hydroxy)methyl)-2,2-dimethyltetrahydrofuro[3,4-d][1,3]dioxol-4-ol |
| ERTU-026 | 1233481-99-6在售 | (3aS,6R,6aS)-6-((R)-(2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-1,3-dithian-2-yl)(hydroxy)methyl)-3a-(hydroxymethyl)-2,2-dimethyltetrahydrofuro[3,4-d][1,3]dioxol-4-ol |
| ERTU-027 | 1233482-00-2在售 | (1R,2R)-1-((S)-5,5-bis(hydroxymethyl)-2,2-dimethyl-1,3-dioxolan-4-yl)-2-(2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-1,3-dithian-2-yl)ethane-1,2-diol |
| ERTU-028 | 6342-60-5在售 | 2-chloro-5-methylbenzoic acid |
| ERTU-029 | 103-73-1在售 | ethoxybenzene |
| ERTU-030 | 1275583-49-7在售 | (2-chloro-5-methylphenyl)(4-ethoxyphenyl)methanone |
| ERTU-031 | 1275583-51-1在售 | (5-(bromomethyl)-2-chlorophenyl)(4-ethoxyphenyl)methanone |
| ERTU-032 | 1275583-52-2在售 | 4-(bromomethyl)-1-chloro-2-(4-ethoxybenzyl)benzene |
| ERTU-033 | 1518795-13-5在售 | 4-chloro-3-(4-ethoxybenzyl)benzyl acetate |
| ERTU-034 | 1275583-53-3在售 | (4-chloro-3-(4-ethoxybenzyl)phenyl)methanol |
| ERTU-035 | 1275583-54-4在售 | 4-chloro-3-(4-ethoxybenzyl)benzaldehyde |
| ERTU-036 | 109-80-8在售 | propane-1,3-dithiol |
优化Route 4步骤 14 · 总收率 5.26 g

| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ERTU-037 | 59531-24-7在售 | (2R,3R,4S,5R,6R)-3,4,5-tris(benzyloxy)-6-((benzyloxy)methyl)tetrahydro-2H-pyran-2-ol |
| ERTU-038 | 13096-62-3在售 | (3R,4S,5R,6R)-3,4,5-tris(benzyloxy)-6-((benzyloxy)methyl)tetrahydro-2H-pyran-2-one |
| ERTU-039 | 109-01-3在售 | 1-methylpiperazine |
| ERTU-040 | 1431329-04-2在售 | (2R,3S,4R,5R)-2,3,4,6-tetrakis(benzyloxy)-5-hydroxy-1-(4-methylpiperazin-1-yl)hexan-1-one |
| ERTU-041 | 1520112-88-2在售 | (2R,3S,4S)-2,3,4,6-tetrakis(benzyloxy)-1-(4-methylpiperazin-1-yl)hexane-1,5-dione |
| ERTU-042 | 53064-79-2在售 | iodomethyl pivalate |
| ERTU-043 | - | (3S,4S,5R)-3,4,5-tris(benzyloxy)-2-((benzyloxy)methyl)-2-hydroxy-6-(4-methylpiperazin-1-yl)-6-oxohexyl pivalate |
| ERTU-044 | - | (2R,3S,4S)-2,3,4,6-tetrakis(benzyloxy)-5-hydroxy-5-(hydroxymethyl)-1-(4-methylpiperazin-1-yl)hexan-1-one |
| ERTU-045 | 1431329-06-4在售 | (2R,3S,4S)-2,3,4-tris(benzyloxy)-4-(4-((benzyloxy)methyl)-2,2-dimethyl-1,3-dioxolan-4-yl)-1-(4-methylpiperazin-1-yl)butan-1-one oxalate |
| ERTU-046 | 1431329-05-3在售 | (2R,3S,4S)-2,3,4-tris(benzyloxy)-4-(4-((benzyloxy)methyl)-2,2-dimethyl-1,3-dioxolan-4-yl)-1-(4-methylpiperazin-1-yl)butan-1-one |
| ERTU-047 | 1298086-15-3在售 | 2-((benzyloxy)(4-ethoxyphenyl)methyl)-4-bromo-1-chlorobenzene |
| ERTU-048 | 1520113-20-5在售 | (2R,3S,4S)-2,3,4-tris(benzyloxy)-1-(3-((benzyloxy)(4-ethoxyphenyl)methyl)-4-chlorophenyl)-4-(4-((benzyloxy)methyl)-2,2-dimethyl-1,3-dioxolan-4-yl)butan-1-one |
| ERTU-049 | 1629222-50-9在售 | (2S,3S,4R)-2,3,4-tris(benzyloxy)-1-((benzyloxy)methyl)-5-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6,8-dioxabicyclo[3.2.1]octane |
| ERTU-050 | 1298086-18-6在售 | (1R,2S,3S,4R,5S)-1-(acetoxymethyl)-5-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6,8-dioxabicyclo[3.2.1]octane-2,3,4-triyl triacetate |
工艺Route 2步骤 8 · 总收率 9.59 kg

| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| ERTU-010 | 461432-23-5在售 | 4-bromo-1-chloro-2-(4-ethoxybenzyl)benzene |
| ERTU-013 | 32384-65-9在售 | (3R,4S,5R,6R)-3,4,5-tris((trimethylsilyl)oxy)-6-(((trimethylsilyl)oxy)methyl)tetrahydro-2H-pyran-2-one |
| ERTU-014 | 714269-57-5在售 | (2S,3R,4S,5S,6R)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3,4,5-triol |
| ERTU-015 | 1528636-29-4在售 | ((2R,3R,4S,5R,6S)-6-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-methoxy-3,4,5-tris((trimethylsilyl)oxy)tetrahydro-2H-pyran-2-yl)methanol |
| ERTU-016 | 1528636-33-0在售 | (2S,3R,4S,5R,6S)-6-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6-methoxy-3,4,5-tris((trimethylsilyl)oxy)tetrahydro-2H-pyran-2-carbaldehyde |
| ERTU-017 | 1528636-39-6在售 | (2S,3R,4S,5S)-2-(4-chloro-3-(4-ethoxybenzyl)phenyl)-6,6-bis(hydroxymethyl)-2-methoxytetrahydro-2H-pyran-3,4,5-triol |
| ERTU-018 | 98-79-3在售 | (S)-5-oxopyrrolidine-2-carboxylic acid |
常见问题(FAQ)
艾托格列净的适应症有哪些?
已批准的适应症包括:二型糖尿病。
艾托格列净的专利什么时候到期?
艾托格列净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。
艾托格列净有几条合成路线?
本站收录 4 条合成路线,最短路线 8 步、总收率 9.59 kg。每条路线的中间体均带登记编号与 CAS 号。
艾托格列净的关键中间体在哪里可以采购?
艾托格列净的多条路线中间体已挂接 CAS 档案,其中 48 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。
如何获取艾托格列净中间体的报价?
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) · 2026-09-24