2,2,2-trichloroethyl carbonochloridate（CAS 17341-93-4）中间体

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膀胱炎西他沙星鼻窦炎西他沙星扁桃体炎西他沙星肺炎西他沙星宫颈炎西他沙星冠周炎西他沙星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

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	-
西他沙星Sitafloxacin Hydrate	Tier C · 观察 / 贸易	-
紫杉醇Paclitaxel	Tier B · 提前布局	-

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。

Paclitaxel/Encequidar mesylate优化路线步数：6总收率：/

(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12-(benzoyloxy)-4,9,11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-3,4,4a,5,6,9,10,11,12,12a-decahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxete-6,12b(2aH)-diyl diacetate→2,2,2-trichloroethyl carbonochloridate→(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12-(benzoyloxy)-9,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-4-(((2,2,2-trichloroethoxy)carbonyl)oxy)-3,4,4a,5,6,9,10,11,12,12a-decahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxete-6,12b(2aH)-diyl diacetate→(Z)-3-phenylacrylic acid→(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12-(benzoyloxy)-11-hydroxy-4a,8,13,13-tetramethyl-5-oxo-9-(((Z)-3-phenylacryloyl)oxy)-4-(((2,2,2-trichloroethoxy)carbonyl)oxy)-3,4,4a,5,6,9,10,11,12,12a-decahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxete-6,12b(2aH)-diyl diacetate→(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12-(benzoyloxy)-9-(((2R,3S)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-3-phenylpropanoyl)oxy)-11-hydroxy-4a,8,13,13-tetramethyl-5-oxo-4-(((2,2,2-trichloroethoxy)carbonyl)oxy)-3,4,4a,5,6,9,10,11,12,12a-decahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxete-6,12b(2aH)-diyl diacetate→(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-9-(((2R,3S)-3-amino-2-hydroxy-3-phenylpropanoyl)oxy)-12-(benzoyloxy)-11-hydroxy-4a,8,13,13-tetramethyl-5-oxo-4-(((2,2,2-trichloroethoxy)carbonyl)oxy)-3,4,4a,5,6,9,10,11,12,12a-decahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxete-6,12b(2aH)-diyl diacetate→benzoyl chloride→(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-9-(((2R,3S)-3-benzamido-2-hydroxy-3-phenylpropanoyl)oxy)-12-(benzoyloxy)-11-hydroxy-4a,8,13,13-tetramethyl-5-oxo-4-(((2,2,2-trichloroethoxy)carbonyl)oxy)-3,4,4a,5,6,9,10,11,12,12a-decahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxete-6,12b(2aH)-diyl diacetate→(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-9-(((2R,3S)-3-benzamido-2-hydroxy-3-phenylpropanoyl)oxy)-12-(benzoyloxy)-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-3,4,4a,5,6,9,10,11,12,12a-decahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxete-6,12b(2aH)-diyl diacetate

西他沙星优化路线步数：6总收率：/

tert-butyl ((1R,2S)-2-fluorocyclopropyl)carbamate→(1S,2R)-2-amino-1,2-diphenylethan-1-ol→2,2,2-trichloroethyl carbonochloridate→(4R,5S)-4,5-diphenyloxazolidin-2-one→1,1-dimethoxyethane→(4R,5S)-3-(1-methoxyethyl)-4,5-diphenyloxazolidin-2-one→(4R,5S)-4,5-diphenyl-3-vinyloxazolidin-2-one→(4R,5S)-3-((1R,2S)-2-fluorocyclopropyl)-4,5-diphenyloxazolidin-2-one→(1R,2S)-2-fluorocyclopropan-1-amine hydrochloride

紫杉醇优化路线步数：6总收率：/

(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12-(benzoyloxy)-4,9,11-trihydroxy-4a,8,13,13-tetramethyl-5-oxo-3,4,4a,5,6,9,10,11,12,12a-decahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxete-6,12b(2aH)-diyl diacetate→2,2,2-trichloroethyl carbonochloridate→(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12-(benzoyloxy)-9,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-4-(((2,2,2-trichloroethoxy)carbonyl)oxy)-3,4,4a,5,6,9,10,11,12,12a-decahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxete-6,12b(2aH)-diyl diacetate→(Z)-3-phenylacrylic acid→(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12-(benzoyloxy)-11-hydroxy-4a,8,13,13-tetramethyl-5-oxo-9-(((Z)-3-phenylacryloyl)oxy)-4-(((2,2,2-trichloroethoxy)carbonyl)oxy)-3,4,4a,5,6,9,10,11,12,12a-decahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxete-6,12b(2aH)-diyl diacetate→(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-12-(benzoyloxy)-9-(((2R,3S)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-3-phenylpropanoyl)oxy)-11-hydroxy-4a,8,13,13-tetramethyl-5-oxo-4-(((2,2,2-trichloroethoxy)carbonyl)oxy)-3,4,4a,5,6,9,10,11,12,12a-decahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxete-6,12b(2aH)-diyl diacetate→(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-9-(((2R,3S)-3-amino-2-hydroxy-3-phenylpropanoyl)oxy)-12-(benzoyloxy)-11-hydroxy-4a,8,13,13-tetramethyl-5-oxo-4-(((2,2,2-trichloroethoxy)carbonyl)oxy)-3,4,4a,5,6,9,10,11,12,12a-decahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxete-6,12b(2aH)-diyl diacetate→benzoyl chloride→(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-9-(((2R,3S)-3-benzamido-2-hydroxy-3-phenylpropanoyl)oxy)-12-(benzoyloxy)-11-hydroxy-4a,8,13,13-tetramethyl-5-oxo-4-(((2,2,2-trichloroethoxy)carbonyl)oxy)-3,4,4a,5,6,9,10,11,12,12a-decahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxete-6,12b(2aH)-diyl diacetate→(2aR,4S,4aS,6R,9S,11S,12S,12aR,12bS)-9-(((2R,3S)-3-benzamido-2-hydroxy-3-phenylpropanoyl)oxy)-12-(benzoyloxy)-4,11-dihydroxy-4a,8,13,13-tetramethyl-5-oxo-3,4,4a,5,6,9,10,11,12,12a-decahydro-1H-7,11-methanocyclodeca[3,4]benzo[1,2-b]oxete-6,12b(2aH)-diyl diacetate

本站可供应的对应中间体

同 CAS 多家在售供应横向对比；价格区间为供应方挂牌口径，实价以询价确认为准。

供应商	产品	价格区间	最小起订	货期	资质	操作
Unibest Nantong cGMP Site	Carbamic acid, (7S)-5-azaspiro[2.4]hept-7-yl-, 1,1-dimethylethyl ester (9CI) Pharmaceutical Intermediates	询价	询价	询价	—