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CAS 71610-00-9
Benzoic acid (2alpha,5beta,7beta,10beta,13alpha)-4,10-diacetoxy-1,7-dihydroxy-13-[2(R)-hydroxy-3(S)-[2-methyl-2(E)-butenoylamino]-3-phenylpropionyloxy]-9-oxo-5,20-epoxytax-11-en-2-yl ester
登记编号：(VI)101438-20-b、(I)101438-63-a、(Ib)140605-3-a、(I)140605-20-a
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）
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 | - |
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。
(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-bis(acetyloxy)-1-hydroxy-10,14,17,17-tetramethyl-11-oxo-15-{[(2R,3S)-3-(2-oxopropanamido)-3-phenyl-2-[(triethylsilyl)oxy]propanoyl]oxy}-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)-1-hydroxy-10,14,17,17-tetramethyl-11-oxo-15-{[(2R,3S)-3-[(E)-(2-oxopropylidene)amino]-3-phenyl-2-[(triethylsilyl)oxy]propanoyl]oxy}-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)-1-hydroxy-10,14,17,17-tetramethyl-15-{[(2R,3S)-3-[(2E)-2-methylbut-2-enamido]-3-phenyl-2-[(triethylsilyl)oxy]propanoyl]oxy}-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)-1,9-dihydroxy-15-{[(2R,3S)-2-hydroxy-3-[(E)-[(2E)-2-methylbut-2-en-1-ylidene]amino]-3-phenylpropanoyl]oxy}-10,14,17,17-tetramethyl-11-oxo-6-oxatetracyclo[11.3.1.0(3,10).0(4,7)]heptadec-13-en-2-yl benzoate→(2alpha,5beta,7beta,10beta,13alpha)-4,10-Bis(acetyloxy)-13-[[(2R,3S)-3-amino-2-hydroxy-3-phenylpropanoyl]oxy]-1,7-dihydroxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate→Benzoic acid (2alpha,5beta,7beta,10beta,13alpha)-4,10-diacetoxy-1,7-dihydroxy-13-[2(R)-hydroxy-3(S)-[2-methyl-2(E)-butenoylamino]-3-phenylpropionyloxy]-9-oxo-5,20-epoxytax-11-en-2-yl ester
Benzoic acid (2alpha,5beta,7beta,10beta,13alpha)-4,10-diacetoxy-1,7-dihydroxy-13-[2(R)-hydroxy-3(S)-[2-methyl-2(E)-butenoylamino]-3-phenylpropionyloxy]-9-oxo-5,20-epoxytax-11-en-2-yl ester→(2alpha,5beta,7beta,10beta,13alpha)-4,10-Bis(acetyloxy)-13-[[(2R,3S)-3-amino-2-hydroxy-3-phenylpropanoyl]oxy]-1,7-dihydroxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate→(2alpha,5beta,7beta,10beta,13alpha)-4,10-Bis(acetyloxy)-13-([(2R,3S)-3-amino-3-phenyl-2-[(trimethylsilyl)oxy]propanoyl]oxy)-1-hydroxy-9-oxo-7-[(trimethylsilyl)oxy]-5,20-epoxytax-11-en-2-yl benzoate→Benzenecarboxylic acid→(2alpha,5beta,7beta,10beta,13alpha)-4,10-Bis(acetyloxy)-13-([(2R,3S)-3-benzamido-3-phenyl-2-[(trimethylsilyl)oxy]propanoyl]oxy)-1-hydroxy-9-oxo-7-[(trimethylsilyl)oxy]-5,20-epoxytax-11-en-2-yl benzoat e
[2aR-(2aalpha,4beta,4abeta,6beta,9alpha(2R,3S),11beta,12alpha,12aalpha,12balpha]-6-Acetoxy-9-[3-(4-deuterobenzamido)-2-hydroxy-3-phenylpropionyloxy]-12-(benzoyloxy)-12b-(trideuteroacetoxy)-4,11-dihydroxy-4a,8,13,13-tetramethyl-2a,3,4,4a,5,6,9,10,11,12,12a,12b-dodecahydro-1H-7,11-methanocyclodeca[3,4]benz[1,2-b]oxet- 5-one→Benzoic acid (2alpha,5beta,7beta,10beta,13alpha)-4,10-diacetoxy-1,7-dihydroxy-13-[2(R)-hydroxy-3(S)-[2-methyl-2(E)-butenoylamino]-3-phenylpropionyloxy]-9-oxo-5,20-epoxytax-11-en-2-yl ester→(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4,12-bis(acetyloxy)-15-{[(2R,3S)-3-(cyclopentylformamido)-2-hydroxy-3-phenylpropanoyl]oxy}-1,9-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→(2alpha,5beta,7beta,10beta,13alpha)-4-(Acetyloxy)-13-[[(2R,3S)-3-benzamido-2-hydroxy-3-phenylpropanoyl]oxy]-1,7,10-trihydroxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate→3'-N-Debenzoyl-3'-N-[2-methyl-2(E)-butenamido]paclitaxel→(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-(acetyloxy)-15-{[(2R,3S)-3-(cyclopentylformamido)-2-hydroxy-3-phenylpropanoyl]oxy}-1,9,12-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→(2alpha,5beta,7beta,10beta,13alpha)-4-(Acetyloxy)-1,10-dihydroxy-9-oxo-13-([(2R,3S)-3-phenyl-3-[(phenylcarbonyl)amino]-2-[(triethylsilyl)oxy]propanoyl]oxy)-7-[(triethylsilyl)oxy]-5,20-epoxytax-11-en-2-yl benzoate→(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-(acetyloxy)-1,12-dihydroxy-10,14,17,17-tetramethyl-15-{[(2R,3S)-3-(2-methylbut-2-enamido)-3-phenyl-2-[(triethylsilyl)oxy]propanoyl]oxy}-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-(acetyloxy)-15-{[(2R,3S)-3-(cyclopentylformamido)-3-phenyl-2-[(triethylsilyl)oxy]propanoyl]oxy}-1,12-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-(acetyloxy)-1,12-dihydroxy-10,14,17,17-tetramethyl-11-oxo-15-{[(2R,3S)-3-phenyl-3-[(E)-(phenylmethylidene)amino]-2-[(triethylsilyl)oxy]propanoyl]oxy}-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-(acetyloxy)-1,12-dihydroxy-10,14,17,17-tetramethyl-15-{[(2R,3S)-3-[(E)-(2-methylbut-2-en-1-ylidene)amino]-3-phenyl-2-[(triethylsilyl)oxy]propanoyl]oxy}-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-(acetyloxy)-15-{[(2R,3S)-3-[(E)-(cyclopentylmethylidene)amino]-3-phenyl-2-[(triethylsilyl)oxy]propanoyl]oxy}-1,12-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-(Acetyloxy)-15-[[(2R,3S)-3-amino-2-hydroxy-3-phenylpropanoyl]oxy]-1,9,12-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→1,3-Bis(1,1-dimethylethyl) propanedioate
Benzoic acid (2alpha,5beta,7beta,10beta,13alpha)-4,10-diacetoxy-1,7-dihydroxy-13-[2(R)-hydroxy-3(S)-[2-methyl-2(E)-butenoylamino]-3-phenylpropionyloxy]-9-oxo-5,20-epoxytax-11-en-2-yl ester→3'-N-Debenzoyl-3'-N-[2-methyl-2(E)-butenamido]paclitaxel→(1S,2S,3R,4S,7R,9S,10S,12R,15S)-4-(acetyloxy)-1,12-dihydroxy-10,14,17,17-tetramethyl-15-{[(2R,3S)-3-(2-methylbut-2-enamido)-3-phenyl-2-[(triethylsilyl)oxy]propanoyl]oxy}-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-(acetyloxy)-1,12-dihydroxy-10,14,17,17-tetramethyl-15-{[(2R,3S)-3-[(E)-(2-methylbut-2-en-1-ylidene)amino]-3-phenyl-2-[(triethylsilyl)oxy]propanoyl]oxy}-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)-13-([(2R,3S)-3-[(tert-butoxycarbonyl)amino]-2-hydroxy-3-phenylpropanoyl]oxy)-1-hydroxy-9-oxo-7,10-bis[[(2,2,2-trichloroethoxy)carbonyl]oxy]-5,20-epoxytax-11-en-2-yl benzoate→(2alpha,5beta,7beta,10beta,13alpha)-4-(Acetyloxy)-13-[[(2R,3S)-3-amino-2-hydroxy-3-phenylpropanoyl]oxy]-1-hydroxy-9-oxo-7,10-bis[[(2,2,2-trichloroethoxy)carbonyl]oxy]-5,20-epoxytax-11-en-2-yl benzoate→(2alpha,5beta,7beta,10beta,13alpha)-4-(Acetyloxy)-13-([(2R,3S)-3-amino-3-phenyl-2-[(triethylsilyl)oxy]propanoyl]oxy)-1-hydroxy-9-oxo-7,10-bis[[(2,2,2-trichloroethoxy)carbonyl]oxy]-5,20-epoxytax-11-en-2-yl benzoate→2-Methylbut-2-enoic acid→(2alpha,5beta,7beta,10beta,13alpha)-4-(Acetyloxy)-1-hydroxy-13-([(2R,3S)-3-[[(2E)-2-methylbut-2-enoyl]amino]-3-phenyl-2-[(triethylsilyl)oxy]propanoyl]oxy)-9-oxo-7,10-bis[[(2,2,2-trichloroethoxy)carbonyl]oxy]-5,20-epoxytax-11-en-2-yl benzoate
Benzoic acid (2alpha,5beta,7beta,10beta,13alpha)-4,10-diacetoxy-1,7-dihydroxy-13-[2(R)-hydroxy-3(S)-[2-methyl-2(E)-butenoylamino]-3-phenylpropionyloxy]-9-oxo-5,20-epoxytax-11-en-2-yl ester→(2alpha,5beta,7beta,10beta,13alpha)-4-(Acetyloxy)-1,7,10,13-tetrahydroxy-9-oxo-5,20-epoxytax-11-en-2-yl benzoate
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