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Lutetium (177Lu) zaregreptide dizuxetan
Tier C · 观察 / 贸易Lutetium (177Lu) zaregreptide dizuxetan
诺华制药
原研
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首批上市
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到期年（公开口径）
无销量数据
峰值销售
体内诊断试剂
类型
靶点：GRPR
适应症（已批准）：转移性乳腺癌、乳腺癌、肿瘤、前列腺癌、神经内分泌癌、实体瘤
各地区研发/上市状态
美国
临床二期
2019-07-24
欧盟
临床二期
2019-07-24
中国
临床二期
2024-08-14
日本
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合成路线与中间体5 routes
原研路线 × 0优化路线（非专利）× 5工艺路线 × 0
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 6 · 总收率 /
(I) 847759-1-a—(II) 847759-1-a—(III) 847759-1-a—(IV) 847759-1-a29022-11-5(V) 847759-1-a—(VI) 847759-1-a68858-20-8(VII) 847759-1-a—(VIII) 847759-1-a35661-39-3(IX) 847759-1-a—(X) 847759-1-a143824-78-6(XI) 847759-1-a, (XI) 847759-1-b—API · Lutetium (177Lu) zaregreptide dizuxetan
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (I) 847759-1-a | - | (2S)-2-({[(9H-Fluoren-9-yl)methoxy]carbonyl}amino)-3-[1-(triphenylmethyl)-1H-imidazol-4-yl]propanoic acid |
| (II) 847759-1-a | - | Resin bound N-[[(9H-fluoren-9-yl)methoxy]carbonyl]-1-(triphenylmethyl)-L-histidine |
| (III) 847759-1-a | - | Resin bound 1-(triphenylmethyl)-L-histidine |
| (IV) 847759-1-a | 29022-11-5 | 2-(9H-Fluoren-9-ylmethoxycarbonylamino)acetic acid |
| (V) 847759-1-a | - | Resin bound glycyl-1-(triphenylmethyl)-L-histidine |
| (VI) 847759-1-a | 68858-20-8 | (2S)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)-3-methylbutanoic acid |
| (VII) 847759-1-a | - | Resin bound L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (VIII) 847759-1-a | 35661-39-3 | (2S)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)propanoic acid |
| (IX) 847759-1-a | - | Resin bound L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (X) 847759-1-a | 143824-78-6 | (S)-2-((((9H-Fluoren-9-yl)methoxy)carbonyl)amino)-3-(1-(tert-butoxycarbonyl)-1H-indol-3-yl)propanoic acid |
| (XI) 847759-1-a, (XI) 847759-1-b | - | Resin bound 1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
优化Route 2步骤 2 · 总收率 /
(XI) 847759-1-a, (XI) 847759-1-b—(XII) 847759-1-b132327-80-1(XIII) 847759-1-b—(XIV) 847759-1-b86123-10-6(XV) 847759-1-b, (XV) 847759-1-c—API · Lutetium (177Lu) zaregreptide dizuxetan
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XI) 847759-1-a, (XI) 847759-1-b | - | Resin bound 1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (XII) 847759-1-b | 132327-80-1 | (2S)-2-({[(9H-Fluoren-9-yl)methoxy]carbonyl}amino)-4-[(triphenylmethyl)carbamoyl]butanoic acid |
| (XIII) 847759-1-b | - | Resin bound N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (XIV) 847759-1-b | 86123-10-6 | (2R)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)-3-phenylpropanoic acid |
| (XV) 847759-1-b, (XV) 847759-1-c | - | Resin bound D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
优化Route 3步骤 2 · 总收率 /
(XIX) 847759-1-c, (XIX) 847759-1-d—(XV) 847759-1-b, (XV) 847759-1-c—(XVI) 847759-1-c—(XVII) 847759-1-c—(XVIII) 847759-1-c137076-54-1API · Lutetium (177Lu) zaregreptide dizuxetan
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XIX) 847759-1-c, (XIX) 847759-1-d | - | Resin bound N-([2-oxo-2-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)anilino]ethoxy]acetyl)-D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (XV) 847759-1-b, (XV) 847759-1-c | - | Resin bound D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (XVI) 847759-1-c | - | (2-[4-[([[(9H-Fluoren-9-yl)methoxy]carbonyl]amino)methyl]anilino]-2-oxoethoxy)acetic acid |
| (XVII) 847759-1-c | - | Resin bound N-([2-[4-(aminomethyl)anilino]-2-oxoethoxy]acetyl)-D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (XVIII) 847759-1-c | 137076-54-1 | DOTA-Tris(t-Bu)ester |
优化Route 4步骤 2 · 总收率 /
(XIX) 847759-1-c, (XIX) 847759-1-d—(XX) 847759-1-d—(XXI) 847759-1-d65530-92-9(XXII) 847759-1-d, (XXII) 847759-1-e—API · Lutetium (177Lu) zaregreptide dizuxetan
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XIX) 847759-1-c, (XIX) 847759-1-d | - | Resin bound N-([2-oxo-2-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)anilino]ethoxy]acetyl)-D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (XX) 847759-1-d | - | N-([2-Oxo-2-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)anilino]ethoxy]acetyl)-D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-1-(triphenylmethyl)-L-histidine |
| (XXI) 847759-1-d | 65530-92-9 | 1-Isobutyl-3-methylbutylamine |
| (XXII) 847759-1-d, (XXII) 847759-1-e | - | N-([2-Oxo-2-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)anilino]ethoxy]acetyl)-D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-N-(2,6-dimethylheptan-4-yl)-1-(triphenylmethyl)-L-histidinamide |
优化Route 5步骤 2 · 总收率 /
(XXIII) 847759-1-e—(XXII) 847759-1-d, (XXII) 847759-1-e—API · Lutetium (177Lu) zaregreptide dizuxetan
| 编号 | CAS 号 | 中间体名称 |
|---|---|---|
| (XXIII) 847759-1-e | - | 2-[4-[2-[[4-[[2-[2-[[(2R)-1-[[(2S)-5-Amino-1-[[(2S)-1-[[(2S)-1-[[(2S)-1-[[2-[[(2S)-1-(2,6-Dimethylheptan-4-ylamino)-3-(1H-imidazol-5-yl)-1-oxopropan-2-yl]amino]-2-oxoethyl]amino]-3-methyl-1-oxobutan-2-yl]amino]-1-oxopropan-2-yl]amino]-3-(1H-indol-3-yl)-1-oxopropan-2-yl]amino]-1,5-dioxopentan-2-yl]amino]-1-oxo-3-phenylpropan-2-yl]amino]-2-oxoethoxy]acetyl]amino]phenyl]methylamino]-2-oxoethyl]-7,10-bis(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetic acid |
| (XXII) 847759-1-d, (XXII) 847759-1-e | - | N-([2-Oxo-2-[4-([2-[4,7,10-tris(2-tert-butoxy-2-oxoethyl)-1,4,7,10-tetraazacyclododecan-1-yl]acetamido]methyl)anilino]ethoxy]acetyl)-D-phenylalanyl-N-(triphenylmethyl)-L-glutaminyl-1-(tert-butoxycarbonyl)-L-tryptophyl-L-alanyl-L-valylglycyl-N-(2,6-dimethylheptan-4-yl)-1-(triphenylmethyl)-L-histidinamide |
常见问题（FAQ）
Lutetium (177Lu) zaregreptide dizuxetan的适应症有哪些？
已批准的适应症包括：转移性乳腺癌、乳腺癌、肿瘤、前列腺癌、神经内分泌癌、实体瘤。
Lutetium (177Lu) zaregreptide dizuxetan的专利什么时候到期？
Lutetium (177Lu) zaregreptide dizuxetan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。
Lutetium (177Lu) zaregreptide dizuxetan有几条合成路线？
本站收录 5 条合成路线，最短路线 2 步、总收率 /。每条路线的中间体均带登记编号与 CAS 号。
Lutetium (177Lu) zaregreptide dizuxetan的关键中间体在哪里可以采购？
Lutetium (177Lu) zaregreptide dizuxetan路线中的中间体均已建立 CAS 档案，可直接按 CAS 发起询价，需求会进入供应网络撮合池。
如何获取Lutetium (177Lu) zaregreptide dizuxetan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） · 2026-10-07