cRGD-ZW800-1

Tier C · 观察 / 贸易

cRGD-ZW800-1

Curadel

原研

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：Not applicable

适应症（已批准）：头颈部鳞状细胞癌、胆管上皮癌、胰腺癌

各地区研发/上市状态

美国

欧盟

临床二期

2022-11-09

中国

日本

合成路线与中间体4 routes

原研路线 × 0优化路线（非专利）× 4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 4 · 总收率 /

(I)819152-1-a98-71-5(II)819152-1-a563-80-4(IIIa)819152-1-a184351-56-2(IIIb)819152-1-a132557-72-3(IV)819152-1-a3779-42-8(V)819152-1-a—(VI)819152-1-a108-94-1(VII)819152-1-a—(VIII)819152-1-a—(IX)819152-1-a—(X)819152-1-a501-97-3(XI)819152-1-a,(XI)819152-1-b2412139-24-1API · cRGD-ZW800-1

编号	CAS 号	中间体名称
(I)819152-1-a	98-71-5	4-Hydrazinobenzenesulfonic acid
(II)819152-1-a	563-80-4	2-Acetylpropane
(IIIa)819152-1-a	184351-56-2	Potassium 2,3,3-trimethyl-3H-indole-5-sulfonate
(IIIb)819152-1-a	132557-72-3	2,3,3-Trimethyl-3H-indole-5-sulfonic acid
(IV)819152-1-a	3779-42-8	3-Bromo-N,N,N-trimethylpropan-1-aminium bromide
(V)819152-1-a	-	2,3,3-Trimethyl-5-sulfo-1-[3-(trimethylazaniumyl)propyl]-3H-indol-1-ium dibromide
(VI)819152-1-a	108-94-1	4-Cyclohexanone
(VII)819152-1-a	-	[3-(Anilinomethylidene)-2-chlorocyclohex-1-en-1-yl]-N-phenylmethaniminium chloride
(VIII)819152-1-a	-	2-[2-[2-Chloro-3-[2-[3,3-dimethyl-5-sulfonato-1-[3-(trimethylazaniumyl)propyl]-1,3-dihydro-2H-indol-2-ylidene]ethylidene]cyclohex-1-en-1-yl]ethenyl]-3,3-dimethyl-1-[3-(trimethylazaniumyl)propyl]-3H-indol-1-ium-5-sulfonate sodium bromide (1/2/3)
(IX)819152-1-a	-	Disodium 3-(4-oxidophenyl)propanoate
(X)819152-1-a	501-97-3	3-(4-Hydroxyphenyl)propionic acid
(XI)819152-1-a,(XI)819152-1-b	2412139-24-1	3-[4-[[6-[2-[3,3-dimethyl-5-sulfonato-1-[3-(trimethylazaniumyl)propyl]-1,3-dihydro-2H-indol-2-ylidene]ethylidene]-2-[2-[3,3-dimethyl-5-sulfonato-1-[3-(trimethylazaniumyl)propyl]-3H-indol-1-ium-2-yl]ethenyl]cyclohex-1-en-1-yl]oxy]phenyl]propanoate trifluoroacetic acid

优化Route 2步骤 2 · 总收率 /

(IIIb)819152-1-a132557-72-3(XI)819152-1-a,(XI)819152-1-b2412139-24-1(XII)819152-1-b—(XIII)819152-1-b,(XIII)819152-1-d217099-14-4API · cRGD-ZW800-1

编号	CAS 号	中间体名称
(IIIb)819152-1-a	132557-72-3	2,3,3-Trimethyl-3H-indole-5-sulfonic acid
(XI)819152-1-a,(XI)819152-1-b	2412139-24-1	3-[4-[[6-[2-[3,3-dimethyl-5-sulfonato-1-[3-(trimethylazaniumyl)propyl]-1,3-dihydro-2H-indol-2-ylidene]ethylidene]-2-[2-[3,3-dimethyl-5-sulfonato-1-[3-(trimethylazaniumyl)propyl]-3H-indol-1-ium-2-yl]ethenyl]cyclohex-1-en-1-yl]oxy]phenyl]propanoate trifluoroacetic acid
(XII)819152-1-b	-	2-[2-[3-[2-[3,3-Dimethyl-5-sulfonato-1-[3-(trimethylazaniumyl)propyl]-1,3-dihydro-2H-indol-2-ylidene]ethylidene]-2-(4-[3-[(2,5-dioxopyrrolidin-1-yl)oxy]-3-oxopropyl]phenoxy)cyclohex-1-en-1-yl]ethenyl]-3,3-dimethyl-1-[3-(trimethylazaniumyl)propyl]-3H-indol-1-ium-5-sulfonate sodium bromide (1/2/2)
(XIII)819152-1-b,(XIII)819152-1-d	217099-14-4	Cyclo(L-arginylglycyl-L-alpha-aspartyl-D-tyrosyl-L-lysyl)

优化Route 3步骤 5 · 总收率 /

(XIV)819152-1-c—(XIX)819152-1-c—(XV)819152-1-c—(XVI)819152-1-c154445-77-9(XVII)819152-1-c—(XVIII)819152-1-c71989-26-9(XX)819152-1-c118488-18-9(XXI)819152-1-c—(XXII)819152-1-c71989-14-5(XXIII)819152-1-c,(XXIII)819152-1-d—API · cRGD-ZW800-1

编号	CAS 号	中间体名称
(XIV)819152-1-c	-	Resin bound [([[(9H-Fluoren-9-yl)methoxy]carbonyl]amino)acetyl]oxy
(XIX)819152-1-c	-	Resin bound N-[(2S)-2-[[N6-(tert-butoxycarbonyl)-L-lysyl]oxy]-5-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]pentanoyl]glycine
(XV)819152-1-c	-	Resin bound glycine
(XVI)819152-1-c	154445-77-9	(2S)-2-{[(9H-Fluoren-9-ylmethoxy)carbonyl]amino}-5-[2-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]pentanoic acid
(XVII)819152-1-c	-	Resin bound N5-[N-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidoyl]-L-ornithylglycine
(XVIII)819152-1-c	71989-26-9	(2S)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)-6-[(2-methylpropan-2-yl)oxycarbonylamino]hexanoic acid
(XX)819152-1-c	118488-18-9	Fmoc-O-tert-butyl-D-tyrosine
(XXI)819152-1-c	-	Resin bound (2S)-1-[(carboxymethyl)amino]-1-oxo-5-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]pentan-2-yl O-tert-butyl-D-tyrosyl-N6-(tert-butoxycarbonyl)-L-lysinate
(XXII)819152-1-c	71989-14-5	(2S)-2-(9H-Fluoren-9-ylmethoxycarbonylamino)-4-[(2-methylpropan-2-yl)oxy]-4-oxobutanoic acid
(XXIII)819152-1-c,(XXIII)819152-1-d	-	Resin bound (5S,8S,11R,14S)-14-amino-8-[4-[(tert-butoxycarbonyl)amino]butyl]-11-[(4-tert-butoxyphenyl)methyl]-18,18-dimethyl-4,7,10,13,16-pentaoxo-5-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-6,17-dioxa-3,9,12-triazanonadecan-1-oic acid

优化Route 4步骤 3 · 总收率 /

(XIII)819152-1-b,(XIII)819152-1-d217099-14-4(XXIII)819152-1-c,(XXIII)819152-1-d—(XXIV)819152-1-d—(XXV)819152-1-d—API · cRGD-ZW800-1

编号	CAS 号	中间体名称
(XIII)819152-1-b,(XIII)819152-1-d	217099-14-4	Cyclo(L-arginylglycyl-L-alpha-aspartyl-D-tyrosyl-L-lysyl)
(XXIII)819152-1-c,(XXIII)819152-1-d	-	Resin bound (5S,8S,11R,14S)-14-amino-8-[4-[(tert-butoxycarbonyl)amino]butyl]-11-[(4-tert-butoxyphenyl)methyl]-18,18-dimethyl-4,7,10,13,16-pentaoxo-5-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-6,17-dioxa-3,9,12-triazanonadecan-1-oic acid
(XXIV)819152-1-d	-	(5S,8S,11R,14S)-14-Amino-8-[4-[(tert-butoxycarbonyl)amino]butyl]-11-[(4-tert-butoxyphenyl)methyl]-18,18-dimethyl-4,7,10,13,16-pentaoxo-5-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-6,17-dioxa-3,9,12-triazanonadecan-1-oic acid
(XXV)819152-1-d	-	tert-Butyl [(2S,5R,8S,11S)-8-[4-[(tert-butoxycarbonyl)amino]butyl]-5-[(4-tert-butoxyphenyl)methyl]-3,6,9,12,15-pentaoxo-11-[3-[N'-(2,2,4,6,7-pentamethyl-2,3-dihydro-1-benzofuran-5-sulfonyl)carbamimidamido]propyl]-1,4,7,10,13-pentaazacyclopentadecan-2-yl]acetate

常见问题（FAQ）

cRGD-ZW800-1的适应症有哪些？

已批准的适应症包括：头颈部鳞状细胞癌、胆管上皮癌、胰腺癌。

cRGD-ZW800-1的专利什么时候到期？

cRGD-ZW800-1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。

cRGD-ZW800-1有几条合成路线？

本站收录 4 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。

cRGD-ZW800-1的关键中间体在哪里可以采购？

cRGD-ZW800-1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cRGD-ZW800-1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） · 2026-10-03