医药中间体
医药中间体是指在药物合成过程中作为关键步骤的反应产物或原料物质，它们通常是化学结构较为简单的化合物，通过一系列化学反应可以转化为最终的药物成品。这些中间体在制药工业中扮演着重要角色，是实现复杂药物分子合成的关键组成部分。
特点- 多样性：医药中间体种类繁多，根据所需药品的不同而不同。
- 复杂性：有些医药中间体本身可能较为简单，但通过一系列复杂的化学反应才能获得最终的药物成品。
- 安全性与纯度要求高：在制药行业中，医药中间体的安全性和纯度直接影响到最终产品的质量和效果。
- 合成新药：许多复杂结构的新药都是通过一些简单的中间体经过一系列复杂的化学反应而合成得到的。
- 药物改良：通过对现有药物中的某些关键中间体进行优化，可以开发出更有效的治疗手段或者降低副作用。
- 原料供应保障：确保医药中间体的稳定供应对于维持药品市场供给至关重要。
医药中间体的研发和生产是一个复杂的过程，通常包括以下几个步骤：
- 合成设计：根据目标药物结构设计合适的合成路线。
- 实验室规模合成与优化：通过小规模实验来验证并优化反应条件。
- 中试放大：将实验室中的成功方案应用于工业化生产前的中间试验阶段。
- 工业化生产：在确保安全性和质量的前提下进行大规模生产。
随着化学合成技术的进步和新技术的应用（如绿色化学、计算机辅助设计等），医药中间体的研发与生产正朝着更加高效、环保的方向发展。同时，对药物分子结构的深入理解也为开发更有效的治疗方案提供了更多可能性。
| 中文名称 | 英文名称 | CAS号 | 化学式 | 结构式图片 |
|---|---|---|---|---|
| 4-{[4-({4-[(E)-2-氰基乙烯基]-2,6-二甲基苯基}氨基)-2-嘧啶基]氨基}苯甲腈盐酸盐(1:1) | Rilpivirine hydrochloride | 700361-47-3 | C22H18N6*ClH |
|
| 4-[[4-(苯基氨基)苯基]亚氨基]环己-2,5-二烯-1-酮 | [1,4]benzoquinone-mono-(4-anilino-phenylimine) | 6201-64-5 | C18H14N2O |
|
| 4-[[2-(4-氯苯基)-4,4-二甲基环己-1-烯基]甲基]哌嗪-1-羧酸叔丁酯 | tert-butyl 4-((2-(4-chlorophenyl)-4,4-dimethylcyclohex-1-enyl)methyl)piperazine-1-carboxylate | 1228780-71-9 | C24H35ClN2O2 |
|
| 4-[[(三丁基锡烷基)氧基]羰基]吡啶 | (C4H9)3SnOOCC5H4N-4 | 5107-59-5 | C18H31NO2Sn |
|
| 4-[[(3-氯-4-甲氧基苯基)甲基]氨基]-2-[(2S)-2-羟甲基-1-吡咯烷基]-5-嘧啶羧酸乙酯 | (S)-ethyl 4-(3-chloro-4-methoxybenzylamino)-2-(2-(hydroxymethyl)pyrrolidin-1-yl)pyrimidine-5-carboxylate | 330785-83-6 | C20H25ClN4O4 |
|
| 4-[8-氨基-3-(2S)-2-吡咯烷基咪唑并[1,5-a]吡嗪-1-基]-N-2-吡啶基苯甲酰胺 | (S)-4-(8-amino-3-(pyrrolidin-2-yl)imidazo[1,5-a]pyrazin-1-yl)-N-(pyridin-2-yl)benzamide | 1420478-90-5 | C22H21N7O |
|
| 4-[6-[[8-环戊基-6-(1-乙氧基乙烯基)-5-甲基-7-氧代-7,8-二氢吡啶并[2,3-d]嘧啶-2-基]氨基]吡啶-3-基]哌嗪-1-羧酸叔丁酯 | 4-{6-[8-cyclopentyl-6-(1-ethoxyvinyl)-5-methyl-7-oxo-7,8-dihydropyrido[2,3-d]pyrimidin-2-ylamino]pyridin-3-yl}piperazine-1-carboxylic acid tert-butyl ester | 571189-10-1 | C31H41N7O4 |
|
| 4-[5-(1H-1,2,4-三唑-1-甲基)-1H-1,2,4-三唑-5-基]吡啶 | 4-[5-(1H-1,2,4-triazol-1-ylmethyl)-1H-1,2,4-triazol-3-yl]pyridine | 477852-54-3 | C10H9N7 |
|
| 4-[4-羟基-3-[4-(吡啶-2-基氨基磺酰基)苯基]偶氮苯基]偶氮-N-吡啶-2-基苯磺酰胺 | 4,4'-((4-Hydroxy-1,3-phenylene)bis(diazenediyl))bis(N-(pyridin-2-yl)benzenesulfonamide) | 1391062-35-3 | C28H22N8O5S2 |
|
| 4-[4-溴-3-(四氢-吡喃-2-基氧基甲基)-苯氧基]-苄腈 | 4-[4-bromo-3-(tetrahydropyran-2-yloxymethyl)phenoxy]benzonitrile | 943311-78-2 | C19H18BrNO3 |
|
| 4-[4-[[2-(4-氯苯基)-5,5-二甲基-1-环己烯]甲基]-1-哌嗪]苯甲酸 | 4-(4-((4'-chloro-4,4-dimethyl-3,4,5,6-tetrahydro-[1,1'-biphenyl]-2-yl)methyl)piperazin-1-yl)benzoic acid | 1044598-91-5 | C26H31ClN2O2 |
|
| 4-[4-[4-(三氟甲氧基)苯氧基]哌啶-1-基]苯酚 | 4-(4-(4-(trifluoromethoxy)phenoxy)piperidin-1-yl)-phenol | 681482-81-5 | C18H18F3NO3 |
|
| 4-[4-[(环丙基氨基)羰基]氨基苯氧基]-7-甲氧基-6-喹啉甲酰胺 | 4-(4-((cyclopropylamino)carbonyl)aminophenoxy)-7-methoxy-6-quinolinecarboxamide | 417714-14-8 | C21H20N4O4 |
|
| 4-[4-(吡啶-3-基)咪唑-1-基]丁胺 | 4-[4-(3-pyridyl)imidazol-1-yl]butylamine | 173838-63-6 | C12H16N4 |
|
| 4-[4-(N-BOC)哌嗪-1-基]苯基硼酸频哪酯 | tert-butyl 4-[4-(4,4,5,5-tetramethyl[1,3,2]dioxaborolan-2-yl)phenyl]piperazine-1-carboxylate | 470478-90-1 | C21H33BN2O4 |
|
| 4-[4-(4,4,5,5-四甲基-1,3,2-二氧杂环戊硼烷-2-基)-1H-吡唑-1-基]哌啶-1-甲酸叔丁酯 | tert-butyl 4-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)-1H-pyrazol-1-yl)piperidine-1-carboxylate | 877399-74-1 | C19H32BN3O4 |
|
| 4-[3-羟基-3-苯基-3-(2-噻吩基)丙基]-4-甲基吗啉 | Tiemonium | 6252-92-2 | C18H24NO2S |
|
| 4-[3-(三氟甲基)苯基]-1-哌嗪乙醇 | N-2-hydroxyethyl-N'-(3-trifluoromethylphenyl)-piperazine | 40004-29-3 | C13H17F3N2O |
|
| 4-[2-哌啶-1-乙氧基]苯甲酸盐酸盐 | 4-(2-piperidin-1-ylethoxy)benzoic acid hydrochloride | 84449-80-9 | C14H19NO3*ClH |
|
| 4-[2-[(3-乙基-4-甲基-2-氧代-3-吡咯琳)甲酰胺基]乙基]苯磺酰胺 | 4-(2-(3-ethyl-4-methyl-2-oxo-3-pyrroline-1-carboxamido)ethyl)benzenesulfonamide | 119018-29-0 | C16H21N3O4S |
|
| 4-[2-[(1Z)-3-(叔丁氧基)-3-氧代-1-丙烯-1-基]苯基]-1,4-二氢-2,6-二甲基-3,5-吡啶二羧酸二乙酯 | diethyl (E)-4-<2-<3-(1,1-dimethylethoxy)-3-oxo-1-propenyl>phenyl>-1,4-dihydro-2,6-dimethylpyridine-3,5-dicarboxylate | 103890-79-5 | C26H33NO6 |
|
| 4-[2-(甲基-2-吡啶基氨基)乙氧基]苯甲醛 | 4-{2-[methyl(pyridin-2-yl)amino]ethoxy}benzaldehyde | 122321-03-3 | C15H16N2O2 |
|
| 4-[2-(二甲基氨基)乙基]吗啉 | 4-(2-(N,N-dimethylamino)ethyl)morpholine | 4385-05-1 | C8H18N2O |
|
| 4-[2-(乙氧羰基)-5-苯并呋喃基]-1-哌嗪羧酸叔丁酯 | ethyl 5-(4-tert-butoxycarbonyl-1-piperazinyl)benzofuran-2-carboxylate | 183288-43-9 | C20H26N2O5 |
|
| 4-[2-(5-氯-2-甲基苯基)偶氮]-3-羟基-N-(2-甲氧基苯基)-2-萘甲酰胺 | 2-Naphthalenecarboxamide, 4-[(5-chloro-2-methylphenyl)azo]-3-hydroxy-N-(2-methoxyphenyl)- | 21889-28-1 | C25H20ClN3O3 |
|
| 4-[2-(5-乙基-2-吡啶基)乙氧基]苯甲醛 | 4-[2-(5-ethylpyridyl)ethoxy]benzaldehyde | 114393-97-4 | C16H17NO2 |
|
| 4-[2-(5-乙基-2-吡啶基)乙氧基]硝基苯 | 4-(2-(5-ethyl-2-pyridyl)ethoxy)nitrobenzene | 85583-54-6 | C15H16N2O3 |
|
| 4-[2-(3,4-二氢-6,7-二甲氧基-2(1h)-异喹啉)乙基]-苯胺 | 4-(2-(6,7-dimethoxy-3,4-dihydroisoquinolin-2(1H)-yl)ethyl)aniline | 82925-02-8 | C19H24N2O2 |
|
| 4-[1-(4,5-二氢-4,4-二甲基-2-恶唑基)-1-甲基乙基]苯乙醇对甲苯磺酸酯 | 2-[4-[1-(4,4-dimethyl-5H-oxazol-2-yl)-1-methylethyl]phenyl]ethyl4-methylbenzenesulfonate | 202189-76-2 | C23H29NO4S |
|
| 4-[1-(2-乙氧基乙基)-1H-苯并咪唑-2-基]-1-哌啶羧酸叔丁酯 | tert-butyl 4-(1-(2-ethoxyethyl)-1H-benzo[d]imidazol-2-yl)piperidine-1-carboxylate | 1181267-36-6 | C21H31N3O3 |
|
| 4-[(三甲基硅基)乙炔基]吗啉 | 1-morpholino-2-trimethylsilyl acetylene | 64024-63-1 | C9H17NOSi |
|
| 4-[(7-氯-4-喹啉基)氨基]-1-戊醇 | 4-((7-chloroquinolin-4-yl)amino)pentan-1-ol | 10500-64-8 | C14H17ClN2O |
|
| 4-[(7-氯-2-甲氧基-1,5-二氢吡啶并[3,2-b]喹啉-10-基)亚氨]-2,6-二(吡咯烷-1-基甲基)环己-2,5-二烯-1-酮磷酸盐 (1:4) | pyronaridine tetraphosphate | 76748-86-2 | C29H32ClN5O2*4H3O4P |
|
| 4-[(6-溴吡啶-3-基)甲基]吗啉 | 4-((6-bromopyridin-3-yl)methyl)morpholine | 364793-93-1 | C10H13BrN2O |
|
| 4-[(5-溴嘧啶-2-基)硫代]苯胺 | 4-(5-bromopyrimidin-2-ylsulfanyl)phenylamine | 849035-61-6 | C10H8BrN3S |
|
| 4-[(5-溴-4,6-二氯-2-嘧啶)氨基]苯甲腈 | 4-[[(5-bromo-4,6-dichloro)-2-pyrimidinyl]amino]benzonitrile | 269055-75-6 | C11H5BrCl2N4 |
|
| 4-[(5-溴-2-嘧啶基)氧基]苯胺 | 4-(5-bromo-2-pyrimidyloxy)aniline | 76660-37-2 | C10H8BrN3O |
|
| 4-[(5-氯-2-羟基苯基)偶氮]间苯二酚 | 1,3-Benzenediol, 4-((5-chloro-2-hydroxyphenyl)azo)- | 4867-01-0 | C12H9ClN2O3 |
|
| 4-[(5-氨基-1-甲基-1H-吲哚-3-基)甲基]-3-甲氧基-苯甲酸甲酯 | methyl 4-((5-amino-1-methyl-1H-indol-3-yl)methyl)-3-methoxybenzoate | 107754-14-3 | C19H20N2O3 |
|
| 4-[(5,6-二苯基吡嗪-2-基)(异丙醇基)氨基]-1-丁醇 | 4-((5,6-diphenylpyrazin-2-yl)(isopropyl)amino)butan-1-ol | 475086-75-0 | C23H27N3O |
|
| 4-[(4-羟基-2-嘧啶基)氨基]苯腈 | 4-[(1,4-dihydro-4-oxo-2-pyrimidinyl)amino]benzonitrile | 189956-45-4 | C11H8N4O |
|
| 4-[(2S,3R)-1-(4-氟苯基)-3-[(3S)-3-(4-氟苯基)-3-羟基丙基]-4-氧代-2-氮杂环丁基]苯基beta-D-吡喃葡糖苷酸 | [14C]-Ezetimibe glucuronide | 190448-57-8 | C30H29F2NO9 |
|
| 4-[(2R)-2-(氯甲基)-3-甲基丁基]-1-甲氧基-2-(3-甲氧基丙氧基)苯 | (R)-2-[4-methoxy-3-(3-methoxypropoxyl)]phenylmethyl-3-methyl-1-chlorobutane | 324763-39-5 | C17H27ClO3 |
|
| 4-[(2,3-二氢噻吩并[3,4-b]-1,4-二噁英-2-基)甲氧基]-1-丁烷磺酸钠 | 4-(2,3-dihydrothieno[3,4-b][1,4]dioxin-2-yl-methoxy)-1-butanesulfonic acid sodium salt | 204444-01-9 | C11H15O6S2*Na |
|
| 4-[(1,3-二氢-1,3,3-三甲基-2H-吲哚-2-亚基)亚乙基]-2,4-二氢-5-甲基-2-苯基-3H-吡唑-3-酮 | 3H-Pyrazol-3-one, 4-[(1,3-dihydro-1,3,3-trimethyl-2H-indol-2-ylidene)ethylidene]-2,4-dihydro-5-methyl-2-phenyl- | 5190-63-6 | C23H23N3O |
|
| 4-[((1S)-1-氨乙基]哌啶-1-羧酸叔丁酯 | 4-((S)-1-amino-ethyl)-piperidine-1-carboxylic acid tert-butyl ester | 1036027-87-8 | C12H24N2O2 |
|
| 4-R-4H-二噻吩并[3,2-b:2',3'-d]吡咯 | 4H-dithieno[3,2-b:2',3'-d]pyrrole | 88537-32-0 | C8H5NS2 |
|
| 4-P-甲苯嘧啶-2-基胺 | 4-(p-tolyl)pyrimidin-2-amine | 263276-44-4 | C11H11N3 |
|
| 4-N[2(4-氯吡啶基)]-氨基苯腈 | 4-[(4-chloro-2-pyrimidinyl)amino]benzonitrile | 244768-32-9 | C11H7ClN4 |
|
| 4-N[2(4,6-二氯吡啶基)]-氨基苯腈 | 4-((4,6-dichloropyrimidin-2-yl)amino)benzonitrile | 329187-59-9 | C11H6Cl2N4 |
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