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克拉霉素

Tier C · 观察 / 贸易

Clarithromycin

Taisho Pharmaceutical Holdings Co Ltd
原研
1991
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:50S ribosomal subunit

商品名:Naxy、Klaricid、Macladin、Klacid、Biaxin、Clarino-500、Clarimax、Cyllind、Clarith、Veclam、Biaxin XL、Minebase

适应症(已批准):鼻窦炎、扁桃体炎、急性支气管炎、慢性支气管炎、下呼吸道感染、咽炎、传染性疾病、肺炎

各地区研发/上市状态

美国
临床二期
1999-11-02
欧盟
临床三期
2000-04-01
中国
批准上市
1996-01-01
日本
批准上市
1991-03-29

生产该 API 的工厂1

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合成路线与中间体8 routes

原研路线 × 0优化路线(非专利)× 7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。

优化Route 1步骤 3 · 总收率 6g(Clarithromycin (Free))
Clarithromycin-001—Clarithromycin-002—Clarithromycin-003—API · 克拉霉素
编号CAS 号中间体名称
Clarithromycin-001-benzyl (2S,3R,4S,6R)-4-{[(benzyloxy)carbonyl](methyl)amino}-2-{[(3R,4S,5S,6R,7S,9R,11R,12R,13S,14R)-14-ethyl-7,12,13-trihydroxy-4-{[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy}-3,5,7,9,11,13-hexamethyl-2,10-dioxo-1-oxacyclotetradecan-6-yl]oxy}-6-methyloxan-3-yl carbonate
Clarithromycin-002-benzyl (2S,3R,4S,6R)-4-{[(benzyloxy)carbonyl](methyl)amino}-2-{[(3R,4S,5S,6R,7S,9R,11R,12R,13S,14R)-14-ethyl-12,13-dihydroxy-4-{[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy}-7-methoxy-3,5,7,9,11,13-hexamethyl-2,10-dioxo-1-oxacyclotetradecan-6-yl]oxy}-6-methyloxan-3-yl carbonate
Clarithromycin-003-(3R,4S,5S,6R,7S,9R,11R,12R,13S,14R)-14-ethyl-12,13-dihydroxy-4-{[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy}-6-{[(2S,3R,4S,6R)-3-hydroxy-6-methyl-4-(methylamino)oxan-2-yl]oxy}-7-methoxy-3,5,7,9,11,13-hexamethyl-1-oxacyclotetradecane-2,10-dione
优化Route 3步骤 4 · 总收率 18g(Clarithromycin (Free))
Clarithromycin-006133445-26-8Clarithromycin-007887125-82-8Clarithromycin-008—Clarithromycin-009—Clarithromycin-010—Clarithromycin-011133415-69-7API · 克拉霉素
编号CAS 号中间体名称
Clarithromycin-006133445-26-8(3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-6-[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyltetrahydropyran-2-yloxy]-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydrpyran-2-yloxy]-3,5,7,9,11,13-hexamethyloxacyclotetradecane-2,10-dione 10-[O-(1-isopropoxycyclohexyl)oxime]
Clarithromycin-007887125-82-8Acetic acid (2S,3R,4S,6R)-4-(dimethylamino)-2-[((3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydropyran-2-yloxy]-10-[[(1-isopropoxycyclohexyl)oxy]imino]-3,5,7,9,11,13-hexamethyl-2-oxooxacyclotetradecan-6-yl)oxy]-6-methyltetrahydropyran-3-yl ester
Clarithromycin-008-Benzoic acid (2S,3R,4S,6R)-4-(dimethylamino)-2-[((3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydropyran-2-yloxy]-10-[[(1-isopropoxycyclohexyl)oxy]imino]-3,5,7,9,11,13-hexamethyl-2-oxooxacyclotetradecan-6-yl)oxy]-6-methyltetrahydropyran-3-yl ester
Clarithromycin-009-Benzoic acid (2S,3R,4S,6R)-4-(dimethylamino)-2-[(3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-14-ethyl-12,13-dihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydropyran-2-yloxy]-10-[[(1-isopropoxycyclohexyl)oxy]imino]-7-methoxy-3,5,7,9,11,13-hexamethyl-2-oxooxacyclotetradecan-6-yloxy]-6-methyltetrahydropyran-3-yl ester
Clarithromycin-010-Acetic acid (2S,3R,4S,6R)-4-(dimethylamino)-2-[((3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-14-ethyl-12,13-dihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydropyran-2-yloxy]-10-[[(1-isopropoxycyclohexyl)oxy]imino]-7-methoxy-3,5,7,9,11,13-hexamethyl-2-oxooxacyclotetradecan-6-yl)oxy]-6-methyltetrahydropyran-3-yl ester
Clarithromycin-011133415-69-7(3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-6-[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyltetrahydropyran-2-yloxy]-14-ethyl-12,13-dihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydropyran-2-yloxy]-7-methoxy-3,5,7,9,11,13-hexamethyloxacyclotetradecane-2,10-dione 10-[O-(1-isopropoxycyclohexyl)oxime]
优化Route 4步骤 5 · 总收率 4.2g(Clarithromycin (Free))
Clarithromycin-01213127-18-9Clarithromycin-013611-19-8Clarithromycin-014206997-62-8Clarithromycin-0151395892-49-5Clarithromycin-016—Clarithromycin-017—Clarithromycin-018—Clarithromycin-019149882-99-5API · 克拉霉素
编号CAS 号中间体名称
Clarithromycin-01213127-18-9(3R,4S,5S,6R,7R,9R,10Z,11S,12R,13S,14R)-6-[[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy]-14-ethyl-7,12,13-trihydroxy-10-(hydroxyimino)-4-[[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl]oxy]-3,5,7,9,11,13-hexamethyloxacyclotetradecan-2-one
Clarithromycin-013611-19-82-Chlorobenzyl chloride
Clarithromycin-014206997-62-8(3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-6-[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyltetrahydropyran-2-yloxy]-14-ethyl-7,12,13-trihydroxy-4- [(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydropyran-2-yloxy]-3,5,7,9,11,13-hexamethyloxacyclotetradecane-2,10-dione 10-[O-(2-chlorobenzyl)oxime]
Clarithromycin-0151395892-49-5Acetic acid (2S,3R,4S,6R)-2-[((3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-10-[[(2-chlorobenzyl)oxy]imino]-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydropyran-2-yloxy]-3,5,7,9,11,13-hexamethyl-2-oxooxacyclotetradecan-6-yl)oxy]-4-(dimethylamino)-6-methyltetrahydropyran-3-yl ester
Clarithromycin-016-Benzoic acid (2S,3R,4S,6R)-2-[(3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-10-[[(2-chlorobenzyloxy]imino]-14-ethyl-7,12,13-trihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydropyran-2-yloxy]-3,5,7,9,11,13-hexamethyl-2-oxooxacyclotetradecan-6-yloxy]-4-(dimethylamino)-6-methyltetrahydropyran-3-yl ester
Clarithromycin-017-Acetic acid (2S,3R,4S,6R)-2-[(3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-10-[[(2-chlorobenzyloxy]imino]-14-ethyl-12,13-dihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydropyran-2-yloxy]-7-methoxy-3,5,7,9,11,13-hexamethyl-2-oxooxacyclotetradecan-6-yloxy]-4-(dimethylamino)-6-methyltetrahydropyran-3-yl ester
Clarithromycin-018-Benzoic acid (2S,3R,4S,6R)-2-[(3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-10-[[2-chlorobenzyloxy]imino]-14-ethyl-12,13-dihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydropyran-2-yloxy]-7-methoxy-3,5,7,9,11,13-hexamethyl-2-oxooxacyclotetradecan-6-yloxy]-4-(dimethylamino)-6-methyltetrahydropyran-3-yl ester
Clarithromycin-019149882-99-5(3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-6-[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyltetrahydropyran-2-yloxy]-14-ethyl-12,13-dihydroxy-4-[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydropyran-2-yloxy]-7-methoxy-3,5,7,9,11,13-hexamethyloxacyclotetradecane-2,10-dione 10-[O-(2-chlorobenzyl)oxime]
优化Route 5步骤 1 · 总收率 /
Clarithromycin-01213127-18-9API · 克拉霉素
编号CAS 号中间体名称
Clarithromycin-01213127-18-9(3R,4S,5S,6R,7R,9R,10Z,11S,12R,13S,14R)-6-[[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy]-14-ethyl-7,12,13-trihydroxy-10-(hydroxyimino)-4-[[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl]oxy]-3,5,7,9,11,13-hexamethyloxacyclotetradecan-2-one
优化Route 6步骤 5 · 总收率 17.5g(Clarithromycin (Free))
Clarithromycin-0207704-67-8Clarithromycin-01213127-18-9Clarithromycin-02113127-18-9Clarithromycin-022926-66-9Clarithromycin-023—Clarithromycin-0241253181-38-2Clarithromycin-02574-88-4Clarithromycin-02674-83-9Clarithromycin-0271253181-39-3API · 克拉霉素
编号CAS 号中间体名称
Clarithromycin-0207704-67-8(3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-6-[[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy]-14-ethyl-7,12,13-trihydroxy-4-[[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl]oxy]-3,5,7,9,11,13-hexamethyloxacyclotetradecane-2,10-dione thiocyanate
Clarithromycin-01213127-18-9Thiocyanic acid--(3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-6-[[(2S,3R,4S,6R)-4-(dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy]-14-ethyl-7,12,13-trihydroxy-10-(hydroxyimino)-4-[[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy]-3,5,7,9,11,13-hexamethyl-1-oxacyclotetradecan-2-one (1/1)
Clarithromycin-02113127-18-9(3R,4S,5S,6R,7R,9R,10Z,11S,12R,13S,14R)-6-[[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy]-14-ethyl-7,12,13-trihydroxy-10-(hydroxyimino)-4-[[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl]oxy]-3,5,7,9,11,13-hexamethyloxacyclotetradecan-2-one
Clarithromycin-022926-66-92-Ethoxyprop-1-ene
Clarithromycin-023-(3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-6-[[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy]-10-[[(2-ethoxypropan-2-yl)oxy]imino]-14-ethyl-7,12,13-trihydroxy-4-[[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy]-3,5,7,9,11,13-hexamethyl-1-oxacyclotetradecan-2-one
Clarithromycin-0241253181-38-2(3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-6-([(2S,3R,4S,6R)-4-(Dimethylamino)-6-methyl-3-[(trimethylsilyl)oxy]tetrahydro-2H-pyran-2-yl]oxy)-10-[[(2-ethoxypropan-2-yl)oxy]imino]-14-ethyl-7,12,13-trihydroxy-4-([(2R,4R,5S,6S)-4-methoxy-4,6-dimethyl-5-[(trimethylsilyl)oxy]tetrahydro-2H-pyran-2-yl]oxy)-3,5,7,9,11,13-hexamethyloxacyclotetradecan-2-one
Clarithromycin-02574-88-4在售Methyl iodide
Clarithromycin-02674-83-9Bromomethane
Clarithromycin-0271253181-39-3(3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-6-([(2S,3R,4S,6R)-4-(Dimethylamino)-6-methyl-3-[(trimethylsilyl)oxy]tetrahydro-2H-pyran-2-yl]oxy)-10-[[(2-ethoxypropan-2-yl)oxy]imino]-14-ethyl-12,13-dihydroxy-7-methoxy-4-([(2R,4R,5S,6S)-4-methoxy-4,6-dimethyl-5-[(trimethylsilyl)oxy]tetrahydro-2H-pyran-2-yl]oxy)-3,5,7,9,11,13-hexamethyloxacyclotetradecan-2-one
优化Route 7步骤 2 · 总收率 52g(Clarithromycin-028)
Clarithromycin-01213127-18-9Clarithromycin-022926-66-9Clarithromycin-023—Clarithromycin-028—API · 克拉霉素
编号CAS 号中间体名称
Clarithromycin-01213127-18-9(3R,4S,5S,6R,7R,9R,10Z,11S,12R,13S,14R)-6-[[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy]-14-ethyl-7,12,13-trihydroxy-10-(hydroxyimino)-4-[[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl]oxy]-3,5,7,9,11,13-hexamethyloxacyclotetradecan-2-one
Clarithromycin-022926-66-92-Ethoxyprop-1-ene
Clarithromycin-023-(3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-6-[[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy]-10-[[(2-ethoxypropan-2-yl)oxy]imino]-14-ethyl-7,12,13-trihydroxy-4-[[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyloxan-2-yl]oxy]-3,5,7,9,11,13-hexamethyl-1-oxacyclotetradecan-2-one
Clarithromycin-028-(3R,4S,5S,6R,7R,9R,10E,11S,12R,13S,14R)-6-[[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyloxan-2-yl]oxy]-10-[[(2-ethoxypropan-2-yl)oxy]imino]-14-ethyl-7,12,13-trihydroxy-4-([(2R,4R,5S,6S)-4-methoxy-4,6-dimethyl-5-[(trimethylsilyl)oxy]oxan-2-yl]oxy)-3,5,7,9,11,13-hexamethyl-1-oxacyclotetradecan-2-one
优化Route 8步骤 1 · 总收率 88g(Clarithromycin-012)
Clarithromycin-0207704-67-8Clarithromycin-01213127-18-9API · 克拉霉素
编号CAS 号中间体名称
Clarithromycin-0207704-67-8(3R,4S,5S,6R,7R,9R,11R,12R,13S,14R)-6-[[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy]-14-ethyl-7,12,13-trihydroxy-4-[[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl]oxy]-3,5,7,9,11,13-hexamethyloxacyclotetradecane-2,10-dione thiocyanate
Clarithromycin-01213127-18-9(3R,4S,5S,6R,7R,9R,10Z,11S,12R,13S,14R)-6-[[(2S,3R,4S,6R)-4-(Dimethylamino)-3-hydroxy-6-methyltetrahydro-2H-pyran-2-yl]oxy]-14-ethyl-7,12,13-trihydroxy-10-(hydroxyimino)-4-[[(2R,4R,5S,6S)-5-hydroxy-4-methoxy-4,6-dimethyltetrahydro-2H-pyran-2-yl]oxy]-3,5,7,9,11,13-hexamethyloxacyclotetradecan-2-one
工艺Route 2步骤 2 · 总收率 429.768g(Clarithromycin (Free))
Clarithromycin-004—Clarithromycin-005—API · 克拉霉素
编号CAS 号中间体名称
Clarithromycin-004-(2R,3R,4R,5R,6R,8R,9E,10S,11R,12R,13S)-5-{[(2S,3R,4S,6R)-4-(dimethylamino)-6-methyl-3-[(trimethylsilyl)oxy]oxan-2-yl]oxy}-13-ethyl-6,11,12-trihydroxy-3-{[(4R,5S,6S)-4-methoxy-4,6-dimethyl-5-[(trimethylsilyl)oxy]oxan-2-yl]oxy}-9-{[(2-methoxypropan-2-yl)oxy]imino}-2,4,6,8,10,12-hexamethylcyclotetradecan-1-one
Clarithromycin-005-(2R,3R,4R,5R,6R,8R,9E,10S,11R,12R,13S)-5-{[(2S,3R,4S,6R)-4-(dimethylamino)-6-methyl-3-[(trimethylsilyl)oxy]oxan-2-yl]oxy}-13-ethyl-11,12-dihydroxy-6-methoxy-3-{[(4R,5S,6S)-4-methoxy-4,6-dimethyl-5-[(trimethylsilyl)oxy]oxan-2-yl]oxy}-9-{[(2-methoxypropan-2-yl)oxy]imino}-2,4,6,8,10,12-hexamethylcyclotetradecan-1-one

常见问题(FAQ)

克拉霉素的适应症有哪些?

已批准的适应症包括:鼻窦炎、扁桃体炎、急性支气管炎、慢性支气管炎、下呼吸道感染、咽炎、传染性疾病、肺炎。

克拉霉素的专利什么时候到期?

克拉霉素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。

克拉霉素有几条合成路线?

本站收录 8 条合成路线,最短路线 1 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。

克拉霉素的关键中间体在哪里可以采购?

克拉霉素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。

如何获取克拉霉素中间体的报价?

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