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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
—— 5,7-dichloro-2-(pyridin-2-yl)pyrazolo[1,5-a]pyrimidine 1232223-43-6 C11H6Cl2N4
5,7-dichloro-2-(pyridin-2-yl)pyrazolo[1,5-a]pyrimidine
—— cis-2,3-Dimethyl-cyclohexanol 1502-24-5 C8H16O
cis-2,3-Dimethyl-cyclohexanol
—— 5-bromo-3-isopropyl-1H-pyrrolo[2,3-b]pyridine 1256819-54-1 C10H11BrN2
5-bromo-3-isopropyl-1H-pyrrolo[2,3-b]pyridine
—— 1-(2,4-Dimethylphenyl)-3-phenyl-1H-pyrazole-5(4H)-one 1003751-09-4 C17H16N2O
1-(2,4-Dimethylphenyl)-3-phenyl-1H-pyrazole-5(4H)-one
—— 2-methyl-4-hydroxy-5,6-dichloropyrimidine 32265-50-2 C5H4Cl2N2O
2-methyl-4-hydroxy-5,6-dichloropyrimidine
—— L-methoxyproline 75176-09-9 C6H11NO3
L-methoxyproline
—— 8-nitro-quinoline-4-carboxylic acid 121689-22-3 C10H6N2O4
8-nitro-quinoline-4-carboxylic acid
—— 2-bromo-4-chloro-3-fluorobenzoic acid 170108-06-2 C7H3BrClFO2
2-bromo-4-chloro-3-fluorobenzoic acid
—— 2,8-dichloro-7-nitro-1,5-naphthyridine 1366050-48-7 C8H3Cl2N3O2
2,8-dichloro-7-nitro-1,5-naphthyridine
—— 1-methyl-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine 1228994-66-8 C7H11N3
1-methyl-4,5,6,7-tetrahydro-1H-pyrazolo[3,4-c]pyridine
—— 2-chloro-5-nitropyrimidine-4,6-diamine 408352-74-9 C4H4ClN5O2
2-chloro-5-nitropyrimidine-4,6-diamine
—— tert-butyl 4-(1H-indazol-3-yl)piperidine-1-carboxylate 889945-69-1 C17H23N3O2
tert-butyl 4-(1H-indazol-3-yl)piperidine-1-carboxylate
—— 3-bromo-2-methoxy-9H-carbazole 890079-77-3 C13H10BrNO
3-bromo-2-methoxy-9H-carbazole
—— ethyl imidazo[1,2-a]pyridine-2-carboxylate hydrobromide 38922-77-9 BrH*C10H10N2O2
ethyl imidazo[1,2-a]pyridine-2-carboxylate hydrobromide
—— (6<i>R</i>)-7<i>t</i>-(2-bromo-acetylamino)-3-methyl-8-oxo-(6<i>r</i><i>H</i>)-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid 58197-02-7 C10H11BrN2O4S
(6<i>R</i>)-7<i>t</i>-(2-bromo-acetylamino)-3-methyl-8-oxo-(6<i>r</i><i>H</i>)-5-thia-1-aza-bicyclo[4.2.0]oct-2-ene-2-carboxylic acid
—— longifolan-15-ol 469-27-2 C15H26O
longifolan-15-ol
—— estra-1,3,5(10)-triene-3,17β-diol 17β-hemisuccinate 7698-93-3 C22H28O5
estra-1,3,5(10)-triene-3,17β-diol 17β-hemisuccinate
—— pyrazolo[1,5-a]pyridine-6-carboxylic acid 474432-61-6 C8H6N2O2
pyrazolo[1,5-a]pyridine-6-carboxylic acid
—— 3-(aminomethyl)pyridine 1-oxide hydrochloride 106940-10-7 C6H8N2O*ClH
3-(aminomethyl)pyridine 1-oxide hydrochloride
—— syn-tert-butyl ((5S,6R)-6-methyl-2-oxo-5-phenylpiperidin-3-yl)carbamate 1375541-78-8 C17H24N2O3
syn-tert-butyl ((5S,6R)-6-methyl-2-oxo-5-phenylpiperidin-3-yl)carbamate
—— N-Methyldichloropane hydrochloride 150653-91-1 C16H20Cl3NO2
N-Methyldichloropane hydrochloride
—— D-Glucitol, bis-O-[(4-methylphenyl)methylene]- 54686-97-4 C22H26O6
D-Glucitol, bis-O-[(4-methylphenyl)methylene]-
—— sodium salt of sulfanilic acid 2-pyridylamide 127-57-1 C11H10N3O2S*Na
sodium salt of sulfanilic acid 2-pyridylamide
—— tert-butyl (4aR,7aR)-octahydro-1H-pyrrolo[3,4-b]pyridine-1-carboxylate 159877-36-8 C12H22N2O2
tert-butyl (4aR,7aR)-octahydro-1H-pyrrolo[3,4-b]pyridine-1-carboxylate
—— 5-bromo-4-chloro-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidine 717900-59-9 C11H11BrClN3
5-bromo-4-chloro-7-cyclopentyl-7H-pyrrolo[2,3-d]pyrimidine
—— 3-oxo-1-phenyl-2,7,10,13-tetraoxa-4-azahexadecan-16-oic acid 1310327-18-4 C17H25NO7
3-oxo-1-phenyl-2,7,10,13-tetraoxa-4-azahexadecan-16-oic acid
—— 5-((+)-biotinamido)pentylamine trifluoroacetic acid 288259-39-2 C2HF3O2*C15H28N4O2S
5-((+)-biotinamido)pentylamine trifluoroacetic acid
—— (15S)-Prostaglandin A2 13345-50-1 C20H30O4
(15S)-Prostaglandin A2
—— (1R,4S,5'S,6R,6'S,8R,10E,12S,13S,14E,16E,20R,21E,24S)-6'-cyclohexyl-24-hydroxy-21-hydroxyimino-12-[(4S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one 220119-17-5 C43H63NO11
(1R,4S,5'S,6R,6'S,8R,10E,12S,13S,14E,16E,20R,21E,24S)-6'-cyclohexyl-24-hydroxy-21-hydroxyimino-12-[(4S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
—— methyl (4-amino-3,5-dichloro-6-fluoro-2-pyridinyloxy)acetate 69184-17-4 C8H7Cl2FN2O3
methyl (4-amino-3,5-dichloro-6-fluoro-2-pyridinyloxy)acetate
—— 4,4''-di(4-pyridyl)-4',5'-bis[4-(4-pyridyl)-phenyl]-1,1':2',1''-terphenyl 591215-20-2 C50H34N4
4,4''-di(4-pyridyl)-4',5'-bis[4-(4-pyridyl)-phenyl]-1,1':2',1''-terphenyl
—— tert-butyl (S)-2-ethynylmorpholine-4-carboxylate 1621165-19-2 C11H17NO3
tert-butyl (S)-2-ethynylmorpholine-4-carboxylate
—— Imino-bis-carbimidsaeuremethylester 25649-35-8 C4H9N3O2
Imino-bis-carbimidsaeuremethylester
—— 2-Methylaminomethyl-cyclohexanol 87974-29-6 C8H17NO
2-Methylaminomethyl-cyclohexanol
—— (1R,4S,5'S,6R,6'S,8R,10E,12S,13S,14E,16E,20R,21E,24S)-6'-cyclohexyl-24-hydroxy-21-hydroxyimino-12-[(2R,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one 165108-07-6 C43H63NO11
(1R,4S,5'S,6R,6'S,8R,10E,12S,13S,14E,16E,20R,21E,24S)-6'-cyclohexyl-24-hydroxy-21-hydroxyimino-12-[(2R,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
—— Ionomycincalciumsalt 56092-82-1 C41H70CaO9
Ionomycincalciumsalt
—— 4-formyl-3-(hydroxymethyl)benzoic acid ethylester 82304-99-2 C11H12O4
4-formyl-3-(hydroxymethyl)benzoic acid ethylester
—— 1-(3-chlorophenyl)-5-methyl-1H-pyrazole-3-carboxylic acid 1175972-08-3 C11H9ClN2O2
1-(3-chlorophenyl)-5-methyl-1H-pyrazole-3-carboxylic acid
—— sudexanox 58761-87-8 C4H11NO3*C21H23NO5S
sudexanox
—— 1,2,3,4-Tetrahydroisoquinolin-2-ium-6,7-diol 52768-23-7 C9H12NO2+
1,2,3,4-Tetrahydroisoquinolin-2-ium-6,7-diol
—— 5-(methoxycarbonyl)-1H-pyrrole-3-carboxylic acid 67858-48-4 C7H7NO4
5-(methoxycarbonyl)-1H-pyrrole-3-carboxylic acid
—— benzyl N-[6-oxo-6-[[(2R,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]amino]hexyl]carbamate 38822-58-1 C20H30N2O8
benzyl N-[6-oxo-6-[[(2R,3R,4S,5R,6R)-3,4,5-trihydroxy-6-(hydroxymethyl)oxan-2-yl]amino]hexyl]carbamate
—— Catharanthin 467-77-6 C21H26N2O2
Catharanthin
—— (1R,5'S,6R,6'S,8R,10E,12S,13S,14E,16E,20R,21Z,24S)-6'-cyclohexyl-24-hydroxy-21-hydroxyimino-12-[(2R,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one 165108-07-6 C43H63NO11
(1R,5'S,6R,6'S,8R,10E,12S,13S,14E,16E,20R,21Z,24S)-6'-cyclohexyl-24-hydroxy-21-hydroxyimino-12-[(2R,4S,5S,6S)-5-hydroxy-4-methoxy-6-methyloxan-2-yl]oxy-5',11,13,22-tetramethylspiro[3,7,19-trioxatetracyclo[15.6.1.14,8.020,24]pentacosa-10,14,16,22-tetraene-6,2'-oxane]-2-one
—— Selgantolimod 2004677-13-6 C14H20FN5O
Selgantolimod
—— Disodium 4-hydroxy-6-(phenylamino)-3-((4-sulphonatophenyl)azo)naphthalene-2-sulphonate 6222-56-6 C22H15N3Na2O7S2
Disodium 4-hydroxy-6-(phenylamino)-3-((4-sulphonatophenyl)azo)naphthalene-2-sulphonate
—— Disodium 2'-(4-((1-hydroxy-7-(phenylamino)-3-sulphonato-2-naphthyl)azo)phenyl)-6-methyl(2,6'-bibenzothiazole)-7-sulphonate 6222-60-2 C37H23N5Na2O7S4
Disodium 2'-(4-((1-hydroxy-7-(phenylamino)-3-sulphonato-2-naphthyl)azo)phenyl)-6-methyl(2,6'-bibenzothiazole)-7-sulphonate
—— 24,25 Dihydroxyvitamin D3 55721-11-4 C27H44O3
24,25 Dihydroxyvitamin D3
—— 2-[2-[2-[Bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]ethyl-(carboxymethyl)amino]-3-phenylmethoxypropanoic acid;gadolinium 113662-23-0 C22H31GdN3O11
2-[2-[2-[Bis(carboxymethyl)amino]ethyl-(carboxymethyl)amino]ethyl-(carboxymethyl)amino]-3-phenylmethoxypropanoic acid;gadolinium
—— (2R)-2-{[(5Sa)-5-{3-chloro-2-methyl-4-[2-(4-methylpiperazin-1-yl)ethoxy]phenyl}-6-(5-fluorofuran-2-yl)thieno[2,3-d]pyrimidin-4-yl]oxy}-3-(2-{[1-(2,2,2-trifluoroethyl)-1H-pyrazol-5-yl]methoxy}phenyl)propanoic acid 1799633-27-4 C39H37ClF4N6O6S
(2R)-2-{[(5Sa)-5-{3-chloro-2-methyl-4-[2-(4-methylpiperazin-1-yl)ethoxy]phenyl}-6-(5-fluorofuran-2-yl)thieno[2,3-d]pyrimidin-4-yl]oxy}-3-(2-{[1-(2,2,2-trifluoroethyl)-1H-pyrazol-5-yl]methoxy}phenyl)propanoic acid