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CAS 32981-86-5
(2alpha,5beta,7beta,10beta,13alpha)-4-(Acetyloxy)-1,7,10,13-tetrahydroxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12b-acetoxy-4,6,9,11-tetrahydroxy-4a,8,13,13-tetramethyl-5-oxo-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxet-12-yl benzoate
登记编号:(XIII)101438-2-a、(I)101438-8-a、(XI)101438-21-a、(I)101438-33-a、(I)101438-43-a、(VI)101438-47-a、(I)101438-52-a、(I)101438-58-a、(I)101438-77-a、(I)140605-5-a、(I)140605-6-a、(I)140605-12-a 等 21 个
应用背景(按来源药适应症)
乳腺癌Paclitaxel/Encequidar mesylate腺癌Paclitaxel/Encequidar mesylate血管肉瘤Paclitaxel/Encequidar mesylate实体瘤Paclitaxel/Encequidar mesylate膀胱癌多西他赛纳米胶束 (Samyang Biopharmaceuticals)头颈癌多西他赛纳米胶束 (Samyang Biopharmaceuticals)头颈部鳞状细胞癌多西他赛纳米胶束 (Samyang Biopharmaceuticals)实体瘤多西他赛纳米胶束 (Samyang Biopharmaceuticals)胰腺癌紫杉醇非小细胞肺癌紫杉醇霍奇金病紫杉醇精原细胞瘤紫杉醇卵巢癌紫杉醇乳腺癌紫杉醇非小细胞肺癌多西他赛(贝海生物)前列腺癌多西他赛(贝海生物)去势抵抗性前列腺肿瘤多西他赛(贝海生物)乳腺癌多西他赛(贝海生物)头颈癌多西他赛(贝海生物)头颈部鳞状细胞癌多西他赛(贝海生物)前列腺癌卡巴他赛腺癌卡巴他赛食管胃结合部肿瘤卡巴他赛胃癌卡巴他赛生殖细胞和胚胎肿瘤卡巴他赛睾丸肿瘤卡巴他赛
来源药(使用该中间体的合成路线)
| 品种 | 梯队 | 到期年 |
|---|---|---|
| Paclitaxel/Encequidar mesylate | Tier C · 观察 / 贸易 | - |
| 多西他赛纳米胶束 (Samyang Biopharmaceuticals)Docetaxel polymeric micelle (Samyang Biopharmaceuticals) | Tier C · 观察 / 贸易 | - |
| 紫杉醇Paclitaxel | Tier B · 提前布局 | - |
| 多西他赛(贝海生物)Docetaxel (Beihai) | Tier C · 观察 / 贸易 | - |
| 卡巴他赛Cabazitaxel | Tier C · 观察 / 贸易 | - |
合成路线中的位置(上下游链)
按路线登记顺序排列,左→右为合成方向;高亮为当前 CAS,其余可点击跳转对应档案。
(NZ)-4-Methoxy-N-(phenylmethylidene)aniline→(2-Chloranyl-2-oxidanylideneethyl) ethanoate→cis-1-(4-Methoxyphenyl)-2-oxo-4-phenylazetidin-3-yl acetate→cis-2-Oxo-4-phenylazetidin-3-yl acetate→alpha-Chlorobenzaldehyde→(3R,4S)-3-hydroxy-4-phenylazetidin-2-one→[(Ethenyl)oxy]ethane→(3R,4S)-3-(1-Ethoxyethoxy)-4-phenylazetidin-2-one→1-Benzoyl-3(R)-(1-ethoxyethoxy)-4(S)-phenylazetidin-2-one→3(S)-(Benzamido)-2(R)-(1-ethoxyethoxy)-3-phenylpropionic acid→(4S,5R)-5-(1-ethoxyethoxy)-2,4-diphenyl-5,6-dihydro-4H-1,3-oxazin-6-one→(2alpha,5beta,7beta,10beta,13alpha)-4-(Acetyloxy)-1,7,10,13-tetrahydroxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate→(1S,2S,3R,4S,7R,9R,10S,12R,15S)-4,12-bis(acetyloxy)-1,15-dihydroxy-10,14,17,17-tetramethyl-11-oxo-9-[(triethylsilyl)oxy]-6-oxatetracyclo[11.3.1.0(3,10).0(4,7)]heptadec-13-en-2-yl benzoate
(2alpha,5beta,7beta,10beta,13alpha)-4-(Acetyloxy)-1,7,10,13-tetrahydroxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate→(2alpha,5beta,7beta,10beta,13alpha)-4-Acetoxy-1,10,13-trihydroxy-9-oxo-7-[(triethylsilyl)oxy]-5,20-epoxytax-11-en-2-yl benzoate→(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-Bis(acetyloxy)-1,15-dihydroxy-10,14,17,17-tetramethyl-11-oxo-9-[(triethylsilyl)oxy]-6-oxatetracyclo[11.3.1.0(3,10).0(4,7)]heptadec-13-en-2-yl benzoate→3(S)-(Benzamido)-2(R)-(1-ethoxyethoxy)-3-phenylpropionic acid→(2alpha,5beta,7beta,10beta,13alpha)-4,10-Diacetoxy-13-[[(2R,3S)-3-(benzoylamino)-2-(1-ethoxyethoxy)-3-phenylpropanoyl]oxy]-1-hydroxy-9-oxo-7-[(triethylsilyl)oxy]-5,20-epoxytax-11-en-2-yl benzoate
(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-Bis(acetyloxy)-1,15-dihydroxy-10,14,17,17-tetramethyl-11-oxo-9-[(triethylsilyl)oxy]-6-oxatetracyclo[11.3.1.0(3,10).0(4,7)]heptadec-13-en-2-yl benzoate→(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-bis(acetyloxy)-15-{[(2R,3S)-3-{[(benzyloxy)carbonyl]amino}-2-[(benzyloxy)methoxy]-3-phenylpropanoyl]oxy}-1-hydroxy-10,14,17,17-tetramethyl-11-oxo-9-[(triethylsilyl)oxy]-6-oxatetracyclo[11.3.1.0(3,10).0(4,7)]heptadec-13-en-2-yl benzoate→(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-bis(acetyloxy)-15-{[(2R,3S)-3-amino-2-[(benzyloxy)methoxy]-3-phenylpropanoyl]oxy}-1-hydroxy-10,14,17,17-tetramethyl-11-oxo-9-[(triethylsilyl)oxy]-6-oxatetracyclo[11.3.1.0(3,10).0(4,7)]heptadec-13-en-2-yl benzoate→(2alpha,5beta,7beta,10beta,13alpha)-4-(Acetyloxy)-1,7,10,13-tetrahydroxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate→(2alpha,5beta,7beta,10beta,13alpha)-4-Acetoxy-1,10,13-trihydroxy-9-oxo-7-[(triethylsilyl)oxy]-5,20-epoxytax-11-en-2-yl benzoate→(2R,3S)-3-{[(benzyloxy)carbonyl]amino}-2-[(benzyloxy)methoxy]-3-phenylpropanoic acid→ethyl (2R,3S)-3-{[(benzyloxy)carbonyl]amino}-2-[(benzyloxy)methoxy]-3-phenylpropanoate→ethyl (2R,3S)-3-{[(benzyloxy)carbonyl]amino}-2-hydroxy-3-phenylpropanoate→Ethyl (2R,3S)-3-amino-2-hydroxy-3-phenylpropanoate
(2alpha,5beta,7beta,10beta,13alpha)-4-(Acetyloxy)-1,7,10,13-tetrahydroxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate→dichlorodiethylsilane→(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-(acetyloxy)-9-{[diethyl(methoxy)silyl]oxy}-1,12,15-trihydroxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.0(3,10).0(4,7)]heptadec-13-en-2-yl benzoate→(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-bis(acetyloxy)-9-{[diethyl(methoxy)silyl]oxy}-1,15-dihydroxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.0(3,10).0(4,7)]heptadec-13-en-2-yl benzoate→(4S,5R)-2,4-Diphenyl-4,5-dihydro-1,3-oxazole-5-carboxylic acid→(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-bis(acetyloxy)-2-(benzoyloxy)-9-{[diethyl(methoxy)silyl]oxy}-1-hydroxy-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.0(3,10).0(4,7)]heptadec-13-en-15-yl (4S,5R)-2,4-diphenyl-4,5-dihydro-1,3-oxazole-5-carboxylate
(2alpha,5beta,7beta,10beta,13alpha)-4-(Acetyloxy)-1,7,10,13-tetrahydroxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate→Acetic acid acetic anhydride→(2alpha,5beta,7beta,10beta,13alpha)-4,10-Bis(acetyloxy)-1,7,13-trihydroxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate→(2alpha,5beta,7beta,10beta,13alpha)-4,10-Bis(acetyloxy)-1,13-dihydroxy-9-oxo-7-[[(2,2,2-trichloroethoxy)carbonyl]oxy]-5,20-epoxytax-11-en-2-yl benzoate→(3R,4S)-1-Benzoyl-4-phenyl-3-(triethylsiloxy)azetidin-2-one→(2alpha,5beta,7beta,10beta,13alpha)-4,10-Bis(acetyloxy)-1-hydroxy-9-oxo-13-([(2R,3S)-3-phenyl-3-[(phenylcarbonyl)amino]-2-[(triethylsilyl)oxy]propanoyl]oxy)-7-[[(2,2,2-trichloroethoxy)carbonyl]oxy]-5,20-epoxytax-11-en-2-yl benzoate
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