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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
—— 4-(aminomethyl)-N,N,6-trimethylpyrimidin-2-amine 1177480-26-0 C8H14N4
4-(aminomethyl)-N,N,6-trimethylpyrimidin-2-amine
—— 3-Aminomethyl-5,6,7,8-tetrahydrochinolin 103041-34-5 C10H14N2
3-Aminomethyl-5,6,7,8-tetrahydrochinolin
—— 2-methoxy-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline 1609393-90-9 C13H20BNO3
2-methoxy-3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)aniline
—— 3',5'-O-acetyl-2'-deoxy-5-azacytidine 22432-93-5 C12H16N4O6
3',5'-O-acetyl-2'-deoxy-5-azacytidine
—— borane, 5-ethyl-2-methyl-pyridine 1006873-58-0 BH3*C8H11N
borane, 5-ethyl-2-methyl-pyridine
—— tert-butyl N-[4-[2-[methoxy(methyl)amino]-2-oxoethyl]phenyl]carbamate 1189399-11-8 C15H22N2O4
tert-butyl N-[4-[2-[methoxy(methyl)amino]-2-oxoethyl]phenyl]carbamate
—— 3-dimethylaminomethyl-benzofuran-2-carboxylic acid hydrochloride 1163245-85-9 C12H13NO3*ClH
3-dimethylaminomethyl-benzofuran-2-carboxylic acid hydrochloride
—— (E)-N'-(2-cyano-4-(3-(1-hydroxy-2-methylpropan-2-yl)thioureido)phenyl)-N,N-dimethylformimidamide 1429755-57-6 C15H21N5OS
(E)-N'-(2-cyano-4-(3-(1-hydroxy-2-methylpropan-2-yl)thioureido)phenyl)-N,N-dimethylformimidamide
—— 5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydropyrido[3,2-b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide 2125450-76-0 C19H18N6O3
5-benzyl-N-(5-methyl-4-oxo-2,3,4,5-tetrahydropyrido[3,2-b][1,4]oxazepin-3-yl)-4H-1,2,4-triazole-3-carboxamide
—— ethyl 2-hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxylate 52578-37-7 C11H10N2O4
ethyl 2-hydroxy-4-oxo-4H-pyrido[1,2-a]pyrimidine-3-carboxylate
—— 4-(5-bromopyridin-2-yl)tetrahydro-2H-pyran-4-carbonitrile 831203-30-6 C11H11BrN2O
4-(5-bromopyridin-2-yl)tetrahydro-2H-pyran-4-carbonitrile
—— trisodium 4-hydroxy-5-({5-sulfonato-4-[(p-tolyl)amino]naphthyl}azo)naphthalene-2,7-disulfonate 10359-95-2 C27H18N3O10S3*3Na
trisodium 4-hydroxy-5-({5-sulfonato-4-[(p-tolyl)amino]naphthyl}azo)naphthalene-2,7-disulfonate
—— N-(pyrazine-2-yl-carbonyl)-L-phenylalanine sodium salt 1093959-75-1 C14H12N3O3*Na
N-(pyrazine-2-yl-carbonyl)-L-phenylalanine sodium salt
—— 18820-82-1 BrH*C5H5N*As2O3
—— Bis(6-amino-2-pyridinaminium) sulfate 146997-97-9 C10H16N6O4S
Bis(6-amino-2-pyridinaminium) sulfate
—— 2-(4-(diphenylamino)phenyl)-3,3-diphenylacrylonitrile 1431371-51-5 C33H24N2
2-(4-(diphenylamino)phenyl)-3,3-diphenylacrylonitrile
—— methyl 6-cyano-1-hydroxy-7-methyl-5-oxo-3,5-dihydroindolizine-2-carboxylate 73427-92-6 C12H10N2O4
methyl 6-cyano-1-hydroxy-7-methyl-5-oxo-3,5-dihydroindolizine-2-carboxylate
—— (2-Bromo-allyl)-but-3-enyl-amine 87280-39-5 C7H12BrN
(2-Bromo-allyl)-but-3-enyl-amine
—— 5'-O-(4,4'-dimethoxytrityl)-5-(E)-(2-carboxyvinyl)-2'-deoxyuridine 923023-62-5 C33H32N2O9
5'-O-(4,4'-dimethoxytrityl)-5-(E)-(2-carboxyvinyl)-2'-deoxyuridine
—— 2-Naphthalenesulfonic acid, 5-amino-8-(phenylazo)-, monosodium salt 67969-74-8 C16H12N3NaO3S
2-Naphthalenesulfonic acid, 5-amino-8-(phenylazo)-, monosodium salt
—— 3-[(4S,7aS)-7a-methyl-1,5-dioxo-2,3,3a,4,6,7-hexahydroinden-4-yl]propanoic acid 1944-63-4 C13H18O4
3-[(4S,7aS)-7a-methyl-1,5-dioxo-2,3,3a,4,6,7-hexahydroinden-4-yl]propanoic acid
—— 5-Methoxy-2-methylpyrazolo[1,5-a]pyridine-3-carboxylic acid ethyl ester 1352393-99-7 C12H14N2O3
5-Methoxy-2-methylpyrazolo[1,5-a]pyridine-3-carboxylic acid ethyl ester
—— 2-chloro-4-iodo-5-(trifluoromethoxy)pyridine 1221171-84-1 C6H2ClF3INO
2-chloro-4-iodo-5-(trifluoromethoxy)pyridine
—— 2-THIENYLZINC BROMIDE 45438-80-0 C4H3BrSZn
2-THIENYLZINC BROMIDE
—— 4-Chloro-3-nitro-8-(trifluoromethyl)quinoline 39487-89-3 C10H4ClF3N2O2
4-Chloro-3-nitro-8-(trifluoromethyl)quinoline
—— trans-1-Aminomethyl-2-ethoxycarbonyl-cyclopropan 36458-93-2 C7H13NO2
trans-1-Aminomethyl-2-ethoxycarbonyl-cyclopropan
—— 1130959-42-0 C16H31N6O18P5
—— 2-ethoxy-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)quinoline 1363386-55-3 C17H22BNO3
2-ethoxy-6-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)quinoline
—— 5-Aza-cytidin-5'-triphosphat 2226-74-6 C8H15N4O14P3
5-Aza-cytidin-5'-triphosphat
—— 4-ethylcyclohexane-1-carbonyl chloride 67589-87-1 C9H15ClO
4-ethylcyclohexane-1-carbonyl chloride
—— 1,3-Bis-<3-(4-fluor-phenyl)-3-oxo-prop-1-enyl>-benzol 7059-61-2 C24H16F2O2
1,3-Bis-<3-(4-fluor-phenyl)-3-oxo-prop-1-enyl>-benzol
—— methyl 5-cyano-1H-indole-6-carboxylate 1227267-07-3 C11H8N2O2
methyl 5-cyano-1H-indole-6-carboxylate
—— tert-butyl 5-iodopyridine-2-carboxylate 165275-95-6 C10H12INO2
tert-butyl 5-iodopyridine-2-carboxylate
—— [(2-phenylpyridine)<sub>2</sub>Ir(μ-Cl)]<sub>2</sub> 1413974-24-9 C44H34Cl2Ir2N4
[(2-phenylpyridine)<sub>2</sub>Ir(μ-Cl)]<sub>2</sub>
—— sulfuric acid mono[2-(5-((R)-1-aminoethyl)[1,3,4]oxadiazol-2-yl)-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl] ester 1426572-57-7 C10H15N5O6S
sulfuric acid mono[2-(5-((R)-1-aminoethyl)[1,3,4]oxadiazol-2-yl)-7-oxo-1,6-diazabicyclo[3.2.1]octan-6-yl] ester
—— cis-4-(tert-butoxycarbonylamino)cyclohexanecarboxylic acid methyl ester 364385-64-8 C13H23NO4
cis-4-(tert-butoxycarbonylamino)cyclohexanecarboxylic acid methyl ester
—— (<i>S</i>)-2-ammonio-2-carboxy-1,1-dimethyl-ethylsulfanyl 52-66-4 C5H10NO2S*H
(<i>S</i>)-2-ammonio-2-carboxy-1,1-dimethyl-ethylsulfanyl
—— DL-α-TOCOPHEROL HYDROGEN SUCCINATE 4345-03-3 C33H54O5
DL-α-TOCOPHEROL HYDROGEN SUCCINATE
—— Unii-0TZ883O8PW 34393-59-4 C10H15N3Na3O13P2-3
Unii-0TZ883O8PW
—— 3,3'-Diamino-N,N'-[perfluoropropane-2,2-diylbis(6-hydroxy-3,1-phenylene)]dibenzamide 220426-92-6 C29H16F12N4O4
3,3'-Diamino-N,N'-[perfluoropropane-2,2-diylbis(6-hydroxy-3,1-phenylene)]dibenzamide
—— 2-methoxy-quinolin-7-ol 1236222-46-0 C10H9NO2
2-methoxy-quinolin-7-ol
—— 3-[(8aS)-7-[[(4S)-5-ethoxycarbonyl-4-(3-fluoro-2-methylphenyl)-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1H-imidazo[1,5-a]pyrazin-2-yl]-2,2-dimethylpropanoic acid 1808248-05-6 C29H35FN6O5S
3-[(8aS)-7-[[(4S)-5-ethoxycarbonyl-4-(3-fluoro-2-methylphenyl)-2-thiazol-2-yl-1,4-dihydropyrimidin-6-yl]methyl]-3-oxo-5,6,8,8a-tetrahydro-1H-imidazo[1,5-a]pyrazin-2-yl]-2,2-dimethylpropanoic acid
—— tert-butyl (1r,4r)-4-(dimethylamino)cyclohexylcarbamate 1286275-84-0 C13H26N2O2
tert-butyl (1r,4r)-4-(dimethylamino)cyclohexylcarbamate
—— Potassium hydroxyquinoline sulfate 14534-95-3 C9H6KNO4S
Potassium hydroxyquinoline sulfate
—— 3,3,3',3'-tetramethyl-1,1'-spirobi(indan)-6,6'-diol 137062-65-8 C21H24O2
3,3,3',3'-tetramethyl-1,1'-spirobi(indan)-6,6'-diol
—— 1α,25-dihydroxy-22-oxavitamin D<sub>3</sub> 103909-75-7 C26H42O4
1α,25-dihydroxy-22-oxavitamin D<sub>3</sub>
—— 2,8-dibromoindolo[3,2-b]carbazole 536757-96-7 C18H10Br2N2
2,8-dibromoindolo[3,2-b]carbazole
—— (6E)-6-[(2E,4E,6E)-3,7-dimethylnona-2,4,6,8-tetraenylidene]-1,5,5-trimethylcyclohexene 1224-78-8 C20H28
(6E)-6-[(2E,4E,6E)-3,7-dimethylnona-2,4,6,8-tetraenylidene]-1,5,5-trimethylcyclohexene
—— Propanoic acid, 3-[(1S)-1-[(1S,3aS,4E,7aS)-4-[(2Z)-[(3S,5R)-3,5-bis[[(1,1-dimethylethyl)dimethylsilyl]oxy]-2-methylenecyclohexylidene]ethylidene]octahydro-7a-methyl-1H-inden-1-yl]ethoxy]-, ethyl este 413571-27-4 C38H68O5Si2
Propanoic acid, 3-[(1S)-1-[(1S,3aS,4E,7aS)-4-[(2Z)-[(3S,5R)-3,5-bis[[(1,1-dimethylethyl)dimethylsilyl]oxy]-2-methylenecyclohexylidene]ethylidene]octahydro-7a-methyl-1H-inden-1-yl]ethoxy]-, ethyl este
—— 6<sup>A</sup>-(6-aminohexylamino)-6<sup>A</sup>-deoxy-β-cyclodextrin 131991-61-2 C48H84N2O34
6<sup>A</sup>-(6-aminohexylamino)-6<sup>A</sup>-deoxy-β-cyclodextrin