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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
—— 8-bromo-5-methoxyquinoline 1312610-18-6 C10H8BrNO
8-bromo-5-methoxyquinoline
—— 5,6,7,12,13,14-hexahydro-5,14:7,12-bis(o-benzeno)pentacene-6,13-dione 6932-41-8 C34H20O2
5,6,7,12,13,14-hexahydro-5,14:7,12-bis(o-benzeno)pentacene-6,13-dione
—— AG10 1446711-81-4 C15H17FN2O3
AG10
—— pyridine hydrogen chloride 628-13-7 C5H6ClN
pyridine hydrogen chloride
—— ethyl (1S,3S,6R)-7-oxabicyclo[4.1.0]heptane-3-carboxylate 365997-31-5 C9H14O3
ethyl (1S,3S,6R)-7-oxabicyclo[4.1.0]heptane-3-carboxylate
—— 5'-O-tritylthymidine 7791-71-1 C29H28N2O5
5'-O-tritylthymidine
—— 4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine dihydrochloride 62002-31-7 C6H9N3*2ClH
4,5,6,7-tetrahydro-1H-imidazo[4,5-c]pyridine dihydrochloride
—— 2-(4-methylphenoxy)pyridine 4783-71-5 C12H11NO
2-(4-methylphenoxy)pyridine
—— 2-deoxystreptamine 2037-48-1 C6H14N2O3
2-deoxystreptamine
—— mesna 19767-45-4 C2H5O3S2*Na
mesna
—— 2-acetyldibenzoylmethane 19221-93-3 C17H14O3
2-acetyldibenzoylmethane
—— 2-Thiobarbituric acid 91759-32-9 C4H4N2O2S
2-Thiobarbituric acid
—— tert-butyl 4-(pyrimidin-2-yl)piperazine-1-carboxylate 780705-64-8 C13H20N4O2
tert-butyl 4-(pyrimidin-2-yl)piperazine-1-carboxylate
—— 4,8-anhydro-1,3-dideoxy-D-gulo-octulose 439685-73-1 C8H14O5
4,8-anhydro-1,3-dideoxy-D-gulo-octulose
—— 6-(1H-benzimidazol-2-yl)pyridine-2-carboxylic acid 144493-38-9 C13H9N3O2
6-(1H-benzimidazol-2-yl)pyridine-2-carboxylic acid
—— 1-bromo-4-(4-ethylcyclohexyl)benzene 91538-82-8 C14H19Br
1-bromo-4-(4-ethylcyclohexyl)benzene
—— methyl 2-(4-(tert-butoxycarbonyl)piperazin-1-yl)pyrimidine-5-carboxylate 1057682-17-3 C15H22N4O4
methyl 2-(4-(tert-butoxycarbonyl)piperazin-1-yl)pyrimidine-5-carboxylate
—— 2-(diacetoxyiodo)mesitylene 33035-41-5 C13H17IO4
2-(diacetoxyiodo)mesitylene
—— 3,7-dichloro-8-chloromethylquinoline 84086-96-4 C10H6Cl3N
3,7-dichloro-8-chloromethylquinoline
—— N-salicyloyl phytosphingosine 212908-67-3 C25H43NO5
N-salicyloyl phytosphingosine
—— ethyl 5-aminothiophene-2-carboxylate 67318-11-0 C7H9NO2S
ethyl 5-aminothiophene-2-carboxylate
—— N-(9-((2R,4S,5R)-4-((tert-butyldimethylsilyl)oxy)-5-(hydroxymethyl)tetrahydrofuran-2-yl)-6-oxo-6,9-dihydro-1H-purin-2-yl)isobutyramide 99540-94-0 C20H33N5O5Si
N-(9-((2R,4S,5R)-4-((tert-butyldimethylsilyl)oxy)-5-(hydroxymethyl)tetrahydrofuran-2-yl)-6-oxo-6,9-dihydro-1H-purin-2-yl)isobutyramide
—— prednisolone 17,21-diacetate 17652-24-3 C25H32O7
prednisolone 17,21-diacetate
—— 5'-O-(4,4'-Dimethoxytrityl)-N<sup>2</sup>-dimethylformamidine-2'-deoxyguanosine 40094-22-2 C34H36N6O6
5'-O-(4,4'-Dimethoxytrityl)-N<sup>2</sup>-dimethylformamidine-2'-deoxyguanosine
—— cis-hexahydroisoindoline 1470-99-1 C8H15N
cis-hexahydroisoindoline
—— aureobasidin A 127785-64-2 C60H92N8O11
aureobasidin A
—— 2-(3-amino-6-chloroquinolin-2-yl)propan-2-ol 916056-79-6 C12H13ClN2O
2-(3-amino-6-chloroquinolin-2-yl)propan-2-ol
—— 3-Methoxy-4-bromo-5-bromomethyl-isoxazole 205645-05-2 C5H5Br2NO2
3-Methoxy-4-bromo-5-bromomethyl-isoxazole
—— 2-bromo-7-methyl-5-oxo-5H-1,3,4-thiadiazolo<3,2-a>pyrimidine 139535-51-6 C6H4BrN3OS
2-bromo-7-methyl-5-oxo-5H-1,3,4-thiadiazolo<3,2-a>pyrimidine
—— (3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine dihydrochloride 1062580-52-2 C14H22N2*2ClH
(3R,4R)-1-benzyl-N,4-dimethylpiperidin-3-amine dihydrochloride
—— 10-(4'-tert-butylphenyl)-10H-phenothiazine 883983-86-6 C22H21NS
10-(4'-tert-butylphenyl)-10H-phenothiazine
—— 1,3-bis(2,4,6-trimethylphenyl)-4,5-dihydroimidazolium chloride 173035-10-4 C21H27N2*Cl
1,3-bis(2,4,6-trimethylphenyl)-4,5-dihydroimidazolium chloride
—— gadopiclenol 933983-75-6 C35H54N7O15*Gd
gadopiclenol
—— Pipamperone dihydrochloride 2448-68-2 C21H30FN3O2*2ClH
Pipamperone dihydrochloride
—— 2-(2,6-dichlorophenyl)-1-[(1S,3R)-3-(hydroxymethyl)-5-(3-hydroxy-3-methylbutyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl]ethanone 1638667-79-4 C24H29Cl2NO3
2-(2,6-dichlorophenyl)-1-[(1S,3R)-3-(hydroxymethyl)-5-(3-hydroxy-3-methylbutyl)-1-methyl-3,4-dihydroisoquinolin-2(1H)-yl]ethanone
—— vitamin K epoxide 25486-55-9 C31H46O3
vitamin K epoxide
—— vitamin K<sub>1</sub> epoxide 25486-55-9 C31H46O3
vitamin K<sub>1</sub> epoxide
—— (3R)-dihydroarteannuin B 87206-33-5 C15H22O3
(3R)-dihydroarteannuin B
—— 6-bromoimidazo[1,2-a]pyridin-8-ol hydrochloride 1379358-48-1 C7H5BrN2O*ClH
6-bromoimidazo[1,2-a]pyridin-8-ol hydrochloride
—— 6-chloro-8-methylimidazo[1,2-b]pyridazine 17412-22-5 C7H6ClN3
6-chloro-8-methylimidazo[1,2-b]pyridazine
—— pyridinium hydrobromide perbromide 39416-48-3 Br3*C5H6N
pyridinium hydrobromide perbromide
—— trans-tetrahydrofuran-3,4-diol 22554-74-1 C4H8O3
trans-tetrahydrofuran-3,4-diol
—— 2,4,5-triamino-6-hydroxypyrimidine sulfate 39267-74-8 C4H7N5O*H2O4S
2,4,5-triamino-6-hydroxypyrimidine sulfate
—— 1-deoxy-1-fluoro-α-D-glucose 2106-10-7 C6H11FO5
1-deoxy-1-fluoro-α-D-glucose
—— 1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6,7-difluoro-4-oxo-1,4-dihydroquinolin-3-carboxylic acid 189279-53-6 C15H6ClF4N3O3
1-(6-amino-3,5-difluoropyridin-2-yl)-8-chloro-6,7-difluoro-4-oxo-1,4-dihydroquinolin-3-carboxylic acid
—— (R,R)-trans-1,2-cyclohexanediaminetetraacetic acid 482-54-2 C14H22N2O8
(R,R)-trans-1,2-cyclohexanediaminetetraacetic acid
—— [4-(aminomethyl)cyclohexyl]methanamine 10029-07-9 C8H18N2
[4-(aminomethyl)cyclohexyl]methanamine
—— (R)-1-acetyl-5-[2-(phenylsulfonyl)ethyenyl]-3-(N-methylpyrrolidin-2-ylmethyl)-1H-indole 180637-88-1 C24H26N2O3S
(R)-1-acetyl-5-[2-(phenylsulfonyl)ethyenyl]-3-(N-methylpyrrolidin-2-ylmethyl)-1H-indole
—— cis-1,3-dibenzyl-2-oxoimidazolidine-4,5-dicarboxylic acid 51591-75-4 C19H18N2O5
cis-1,3-dibenzyl-2-oxoimidazolidine-4,5-dicarboxylic acid
—— 1R,4S-menthadienol 3886-78-0 C10H16O
1R,4S-menthadienol