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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
  1. 多样性:医药中间体种类繁多,根据所需药品的不同而不同。
  2. 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。
  3. 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。
应用
  1. 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。
  2. 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。
  3. 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。
生产与研发

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。
发展趋势

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
—— 10,13-dimethyl-2,16-di(piperidin-1-yl)-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthrene-3,17-diol 13522-16-2 C29H50N2O2
10,13-dimethyl-2,16-di(piperidin-1-yl)-2,3,4,5,6,7,8,9,11,12,14,15,16,17-tetradecahydro-1H-cyclopenta[a]phenanthrene-3,17-diol
—— 3-Pyridinecarbonitrile, 1-butyl-1,2-dihydro-6-hydroxy-4-methyl-2-oxo- 39108-47-9 C11H14N2O2
3-Pyridinecarbonitrile, 1-butyl-1,2-dihydro-6-hydroxy-4-methyl-2-oxo-
—— 5,6-diamino-1H-pyrimidine-2,4-dione;sulfate 42965-55-9 C4H6N4O6S-2
5,6-diamino-1H-pyrimidine-2,4-dione;sulfate
—— Norepinephrine bitartrate salt 3414-63-9 C12H15NO9-2
Norepinephrine bitartrate salt
—— Chloroorienticin A 118395-73-6 C73H88Cl2N10O26
Chloroorienticin A
—— Aivlosin 63409-12-1 C53H87NO19
Aivlosin
—— Pyronaridine Tetraphosphate 76748-86-2 C29H44ClN5O18P4
Pyronaridine Tetraphosphate
—— Disodium N-(8-oxido-3,6-disulfonaphthalen-1-yl)benzenecarboximidate 5045-22-7 C17H11NNa2O8S2
Disodium N-(8-oxido-3,6-disulfonaphthalen-1-yl)benzenecarboximidate
—— 1-ethyl-5-cyano-6-hydroxy-4-methyl-2(1H)-pyridinone 28141-13-1 C9H10N2O2
1-ethyl-5-cyano-6-hydroxy-4-methyl-2(1H)-pyridinone
—— 1-ethyl-5-carbamoyl-6-hydroxy-4-methyl-2-pyridone 29097-12-9 C9H12N2O3
1-ethyl-5-carbamoyl-6-hydroxy-4-methyl-2-pyridone
—— 5,6-Diaminouracil semisulfate 63981-35-1 C8H14N8O8S
5,6-Diaminouracil semisulfate
—— (E)-4-((Benzyloxy)methyl)-2-(bromomethyl)-1,3-dioxolane 6204-41-7 C12H15BrO3
(E)-4-((Benzyloxy)methyl)-2-(bromomethyl)-1,3-dioxolane
—— (Z)-4-((Benzyloxy)methyl)-2-(bromomethyl)-1,3-dioxolane 6204-40-6 C12H15BrO3
(Z)-4-((Benzyloxy)methyl)-2-(bromomethyl)-1,3-dioxolane
—— cis-2-(Bromomethyl)-1,3-dioxolane-4-methanol 6204-42-8 C5H9BrO3
cis-2-(Bromomethyl)-1,3-dioxolane-4-methanol
—— 5,7-Dichloro-1,2-dihydro-2-(5,6,7-trichloro-3-oxobenzo(b)thien-2(3H)-ylidene)-3H-indol-3-one 6904-93-4 C16H4Cl5NO2S
5,7-Dichloro-1,2-dihydro-2-(5,6,7-trichloro-3-oxobenzo(b)thien-2(3H)-ylidene)-3H-indol-3-one
—— Pyrimidin-4(5h)-one 51953-17-4 C4H4N2O
Pyrimidin-4(5h)-one
—— Ethyl 4-oxo-8-(trifluoromethyl)-1,4-dihydroquinoline-2-carboxylate 23851-84-5 C13H10F3NO3
Ethyl 4-oxo-8-(trifluoromethyl)-1,4-dihydroquinoline-2-carboxylate
—— 3,20-Bis(ethylenedioxy)pregna-5,7-diene 19592-55-3 C25H36O4
3,20-Bis(ethylenedioxy)pregna-5,7-diene
—— 2-Thienyllithium 2786-07-4 C4H3LiS
2-Thienyllithium
—— Indigo White 894-86-0 C16H10N2Na2O2
Indigo White
—— Oxyquinoline sulfate 134-31-6 C18H16N2O6S
Oxyquinoline sulfate
—— 7-(3-methylpyrazol-1-yl)-3-phenylcoumarin 6025-18-9 C19H14N2O2
7-(3-methylpyrazol-1-yl)-3-phenylcoumarin
—— 4-Chloro-2-(4-chloro-1,3-dihydro-3-oxo-2H-indol-2-ylidene)-1,2-dihydro-3H-indol-3-one 6275-44-1 C16H8Cl2N2O2
4-Chloro-2-(4-chloro-1,3-dihydro-3-oxo-2H-indol-2-ylidene)-1,2-dihydro-3H-indol-3-one
—— [1,1'-Bianthracene]-3,3'-disulfonic acid, 4,4'-diamino-9,9',10,10'-tetrahydro-9,9',10,10'-tetraoxo-, disodium salt 6022-22-6 C28H14N2Na2O10S2
[1,1'-Bianthracene]-3,3'-disulfonic acid, 4,4'-diamino-9,9',10,10'-tetrahydro-9,9',10,10'-tetraoxo-, disodium salt
—— 5-Diazo-uracil 2435-76-9 C4H2N4O2
5-Diazo-uracil
—— 1-Chlorosulfinyloxy-3-fluoropropane 461-28-9 C3H6ClFO2S
1-Chlorosulfinyloxy-3-fluoropropane
—— 7-Amino-3-[(5-methyl-1,3,4-thiadiazol-2-YL)thiomethyl]cephalosphoranic acid 30246-33-4 C11H12N4O3S3
7-Amino-3-[(5-methyl-1,3,4-thiadiazol-2-YL)thiomethyl]cephalosphoranic acid
—— (2S,4R,8S,12S)-8-acetyl-6,9,13-trimethyl-6-phenyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icos-17-en-16-one 24356-94-3 C29H36O4
(2S,4R,8S,12S)-8-acetyl-6,9,13-trimethyl-6-phenyl-5,7-dioxapentacyclo[10.8.0.02,9.04,8.013,18]icos-17-en-16-one
—— Aniline, N-acetyl-3-methylthio- 2524-78-9 C9H11NOS
Aniline, N-acetyl-3-methylthio-
—— 5H-1,3-DIOXOLO(4,5-f)INDOLE 267-48-1 C9H7NO2
5H-1,3-DIOXOLO(4,5-f)INDOLE
—— 5-Methyl-7-oxo-4,7-dihydro-pyrazolo[1,5-a]pyrimidine-3-carboxylic acid ethyl ester 77493-86-8 C10H11N3O3
5-Methyl-7-oxo-4,7-dihydro-pyrazolo[1,5-a]pyrimidine-3-carboxylic acid ethyl ester
—— 3-(difluoromethyl)-1H-pyrazole 1007468-17-8 C4H4F2N2
3-(difluoromethyl)-1H-pyrazole
—— (5-bromo-pyrimidin-2-yl)-tert-butyl-amine 14001-72-0 C8H12BrN3
(5-bromo-pyrimidin-2-yl)-tert-butyl-amine
—— 2-chloro-6-methyl-quinoline-4-carboxylic acid 50503-75-8 C11H8ClNO2
2-chloro-6-methyl-quinoline-4-carboxylic acid
—— Sodium N-(2,6-dimethyl-4-pyrimidinyl)sulphanilamidate 2462-17-1 C12H14N4NaO2S+
Sodium N-(2,6-dimethyl-4-pyrimidinyl)sulphanilamidate
—— 1-(3-aminophenyl)-2,2,2-trifluoroethanol 17556-38-6 C8H8F3NO
1-(3-aminophenyl)-2,2,2-trifluoroethanol
—— 2-Deoxystreptamine 2037-48-1 C6H14N2O3
2-Deoxystreptamine
—— 2-Benzyl-2,3-dihydro-4(1H)-isochinolon 53667-19-9 C16H15NO
2-Benzyl-2,3-dihydro-4(1H)-isochinolon
—— 4-(4-methyl-2-pyrimidinyl)benzaldehyde 433920-95-7 C12H10N2O
4-(4-methyl-2-pyrimidinyl)benzaldehyde
—— Bromadol HCL BDPC 77239-98-6 C22H28BrNO
Bromadol HCL BDPC
—— 3-methyl-[1,2,4]oxadiazole-5-carboxylic acid potassium salt 1240605-84-8 C4H3N2O3*K
3-methyl-[1,2,4]oxadiazole-5-carboxylic acid potassium salt
—— Diphenyl azodicarboxylate 2449-14-1 C14H10N2O4
Diphenyl azodicarboxylate
—— (±)-E-3,5-dihydroxy-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-6-heptenoic acid ethyl ester 172336-32-2 C27H28FNO4
(±)-E-3,5-dihydroxy-7-[2-cyclopropyl-4-(4-fluorophenyl)-3-quinolyl]-6-heptenoic acid ethyl ester
—— sodium sulfamethoxypyridazinato 2577-32-4 C11H11N4O3S*Na
sodium sulfamethoxypyridazinato
—— 4-chloro-2-(chloromethyl)pyrimidine 3842-28-2 C5H4Cl2N2
4-chloro-2-(chloromethyl)pyrimidine
—— 4-hydroxy-5-chloro-6-(1-fluoroethyl)pyrimidine 227184-12-5 C6H6ClFN2O
4-hydroxy-5-chloro-6-(1-fluoroethyl)pyrimidine
—— 6-(1-fluoroethyl)-5-iodo-4-pyrimidone 438449-92-4 C6H6FIN2O
6-(1-fluoroethyl)-5-iodo-4-pyrimidone
—— 2-[2-(4-chlorophenyl)ethenyl]quinoline 38101-91-6 C17H12ClN
2-[2-(4-chlorophenyl)ethenyl]quinoline
—— (+/-)-coronaridine 467-77-6 C21H26N2O2
(+/-)-coronaridine
—— 6-chloronicotinoyl chloride 58757-38-3 C10H10Cl2N2O
6-chloronicotinoyl chloride