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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
—— 7-Chloroquinaldamide 65147-97-9 C10H7ClN2O
7-Chloroquinaldamide
—— 1,1'-dimethyl-[2,2'-bipyridine]-1,1'-diium iodide 23484-62-0 C12H14N2*2I
1,1'-dimethyl-[2,2'-bipyridine]-1,1'-diium iodide
—— octahydro-quinolin-7-one 90608-26-7 C9H15NO
octahydro-quinolin-7-one
—— L-Ergothionine hydrochloride 6072-08-8 C9H16N3O2S+
L-Ergothionine hydrochloride
—— tert-butyl (1R)-2-(hydroxymethyl)cyclopropane-1-carboxylate 85428-59-7 C9H16O3
tert-butyl (1R)-2-(hydroxymethyl)cyclopropane-1-carboxylate
—— 5'-amino-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-3-ol 939376-59-7 C10H15N3O
5'-amino-3,4,5,6-tetrahydro-2H-[1,2']bipyridinyl-3-ol
—— 5,6-diamino-2-sulfanylidene-1H-pyrimidin-4-one;sulfuric acid;hydrate 207226-25-3 C4H10N4O6S2
5,6-diamino-2-sulfanylidene-1H-pyrimidin-4-one;sulfuric acid;hydrate
—— 2-(4'-Methoxypyrimidin-2'-yl)essigsaeure 66621-78-1 C7H8N2O3
2-(4'-Methoxypyrimidin-2'-yl)essigsaeure
—— N-methyl-1-(pyridin-2-yl)piperidin-4-amine 405058-06-2 C11H17N3
N-methyl-1-(pyridin-2-yl)piperidin-4-amine
—— ethyl 1-methyl-5-[4-(methyloxy)phenyl]-1H-pyrazole-3-carboxylate 852816-12-7 C14H16N2O3
ethyl 1-methyl-5-[4-(methyloxy)phenyl]-1H-pyrazole-3-carboxylate
—— [1-(3,4-dichlorobenzoyl)-5-methoxy-2-methylindol-3-yl]acetic acid 402849-26-7 C19H15Cl2NO4
[1-(3,4-dichlorobenzoyl)-5-methoxy-2-methylindol-3-yl]acetic acid
—— O-(2,3-di-O-benzyl-4,6-O-benzylidene-β-D-glucopyranosyl)-(1->4)-1,6:2,3-dianhydro-β-D-mannopyranose 99541-22-7 C33H34O9
O-(2,3-di-O-benzyl-4,6-O-benzylidene-β-D-glucopyranosyl)-(1->4)-1,6:2,3-dianhydro-β-D-mannopyranose
—— methylamine; iodide, compound with mercury (II)-bromide 14965-49-2 CH5N*HI*Br4Hg2
methylamine; iodide, compound with mercury (II)-bromide
—— 1,3-difluoro-2-iodo-5-propylbenzene 159255-82-0 C9H9F2I
1,3-difluoro-2-iodo-5-propylbenzene
—— 1, 3-dimethyl-2-oxo-3-((phenylsulfonyl)methyl)indoline-5-carbonitrile 1588429-82-6 C18H16N2O3S
1, 3-dimethyl-2-oxo-3-((phenylsulfonyl)methyl)indoline-5-carbonitrile
—— 5-ethylamino-4-methyl-1,2-benzoquinone-2-oxime 174909-38-7 C9H12N2O2
5-ethylamino-4-methyl-1,2-benzoquinone-2-oxime
—— 2-Chloro-3-fluoro-4,5-diiodopyridine 153035-02-0 C5HClFI2N
2-Chloro-3-fluoro-4,5-diiodopyridine
—— 1-[4-(pyridin-2-yl)phenyl]-4(S)-hydroxy-5(S)-2,5-diamino-6-phenyl-2-azahexane trihydrochloride 198904-87-9 C22H26N4O*3ClH
1-[4-(pyridin-2-yl)phenyl]-4(S)-hydroxy-5(S)-2,5-diamino-6-phenyl-2-azahexane trihydrochloride
—— VC29QG46TR 97143-65-2 C17H22N2O2
VC29QG46TR
—— 4-Amino-4-(trifluoromethyl)cyclohexan-1-ol hydrochloride 1803606-71-4 C7H13ClF3NO
4-Amino-4-(trifluoromethyl)cyclohexan-1-ol hydrochloride
—— 2-amino-5,6,7,8-tetrahydropyrido-[4,3-d]pyrimidine dihydrochloride 157327-50-9 C7H10N4*2ClH
2-amino-5,6,7,8-tetrahydropyrido-[4,3-d]pyrimidine dihydrochloride
—— 8-((3R,4S)-4-Ethylpyrrolidin-3-yl)-3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazine dihydrochloride 2050038-84-9 C14H19Cl2N5
8-((3R,4S)-4-Ethylpyrrolidin-3-yl)-3H-imidazo[1,2-a]pyrrolo[2,3-e]pyrazine dihydrochloride
—— bis[2-bromo-5-(2-methoxyethoxy)phenyl]acetylene 388111-07-7 C20H20Br2O4
bis[2-bromo-5-(2-methoxyethoxy)phenyl]acetylene
—— 4-chloro-7-iodo-6-methyl-quinoline 507242-73-1 C10H7ClIN
4-chloro-7-iodo-6-methyl-quinoline
—— 5-bromo-7-fluoro-1,4-dihydrocyclopenta[b]indol-3(2H)-one 869194-30-9 C11H7BrFNO
5-bromo-7-fluoro-1,4-dihydrocyclopenta[b]indol-3(2H)-one
—— tert-butyl 5-hydroxy-1H-indazole-1-carboxylate 1337879-67-0 C12H14N2O3
tert-butyl 5-hydroxy-1H-indazole-1-carboxylate
—— 1,3-difluoro-5-(4-propylcyclohexyl)benzene 144261-13-2 C15H20F2
1,3-difluoro-5-(4-propylcyclohexyl)benzene
—— N,N'-bis(2,3-diacetoxypropyl)-5-acetamido-2,4,6-triiodoisophthalamide 174416-65-0 C24H28I3N3O11
N,N'-bis(2,3-diacetoxypropyl)-5-acetamido-2,4,6-triiodoisophthalamide
—— tert-Butyl (1R,4R,5R)-5-hydroxy-2-azabicyclo[2.2.2]octane-2-carboxylate 2306246-27-3 C12H21NO3
tert-Butyl (1R,4R,5R)-5-hydroxy-2-azabicyclo[2.2.2]octane-2-carboxylate
—— Iridium;2-phenylpyridine;tetrachloride 92220-65-0 C44H36Cl4Ir3N4-4
Iridium;2-phenylpyridine;tetrachloride
—— 3-((S)-1-((tert-butoxycarbonyl)amino)-2-((1S,3S,5S)-3-cyano-2-azabicyclo[3.1.0]hexan-2-yl)-2-oxoethyl)adamantan-1-yl 2,2,2-trifluoroacetate 1194836-75-3 C25H32F3N3O5
3-((S)-1-((tert-butoxycarbonyl)amino)-2-((1S,3S,5S)-3-cyano-2-azabicyclo[3.1.0]hexan-2-yl)-2-oxoethyl)adamantan-1-yl 2,2,2-trifluoroacetate
—— 2-fluoro-4-iodo-3-methoxypyridine 1227580-53-1 C6H5FINO
2-fluoro-4-iodo-3-methoxypyridine
—— (8S,9R)-(-)-N-benzylcinchonidium chloride 69221-14-3 C26H29N2O*Cl
(8S,9R)-(-)-N-benzylcinchonidium chloride
—— 17β-Acetoxyestra-4,6-dien-3-on 2590-41-2 C20H26O3
17β-Acetoxyestra-4,6-dien-3-on
—— Tert-butyl 7-hydroxy-5-thia-2-azaspiro[3.4]octane-2-carboxylate 1453315-70-2 C11H19NO3S
Tert-butyl 7-hydroxy-5-thia-2-azaspiro[3.4]octane-2-carboxylate
—— O-[(2R,3R,4R,5R)-5-[[bis(4-methoxyphenyl)-phenylmethoxy]methyl]-4-hydroxy-2-[6-(2-methylpropanoylamino)purin-9-yl]oxolan-3-yl] 1,1-dioxo-1,4-thiazinane-4-carbothioate 1219089-85-6 C40H44N6O9S2
O-[(2R,3R,4R,5R)-5-[[bis(4-methoxyphenyl)-phenylmethoxy]methyl]-4-hydroxy-2-[6-(2-methylpropanoylamino)purin-9-yl]oxolan-3-yl] 1,1-dioxo-1,4-thiazinane-4-carbothioate
—— Hydron;1-(oxetan-3-yl)ethanamine;chloride 2055842-00-5 C5H12ClNO
Hydron;1-(oxetan-3-yl)ethanamine;chloride
—— cis-4-Methylamino-cyclohexanol-(1) 22348-38-5 C7H15NO
cis-4-Methylamino-cyclohexanol-(1)
—— endo-BCN-PEG2-Biotin 1393600-24-2 C27H42N4O6S
endo-BCN-PEG2-Biotin
—— 4-N-benzoyl-3'-deoxy-5'-O-(4,4'-dimethoxytrityl)cytidine 2-cyanoethyl N,N-diisopropylphosphoramidite 157327-96-3 C46H52N5O8P
4-N-benzoyl-3'-deoxy-5'-O-(4,4'-dimethoxytrityl)cytidine 2-cyanoethyl N,N-diisopropylphosphoramidite
—— 1-(1H-imidazol-2-yl)piperazine dihydrochloride 1795503-50-2 C7H14Cl2N4
1-(1H-imidazol-2-yl)piperazine dihydrochloride
—— 2,4-dichloro-<l>benzothieno<2,3-d>pyrimidine 76872-40-7 C10H4Cl2N2S
2,4-dichloro-<l>benzothieno<2,3-d>pyrimidine
—— (R)-2,2,2-Trifluoro-1-(tetrahydro-2H-pyran-4-YL)ethanamine hcl 1821820-77-2 C7H13ClF3NO
(R)-2,2,2-Trifluoro-1-(tetrahydro-2H-pyran-4-YL)ethanamine hcl
—— [1-(3-Aminopyridin-2-yl)piperidin-4-yl]methanol 1094233-96-1 C11H17N3O
[1-(3-Aminopyridin-2-yl)piperidin-4-yl]methanol
—— duetero-pyridinium triflate 52193-54-1 CF3O3S*C5H6N
duetero-pyridinium triflate
—— 5-((3a<i>S</i>)-2,5,5-trioxo-(3a<i>r</i>,6a<i>c</i>)-octahydro-5λ<sup>6</sup>-thieno[3,4-<i>d</i>]imidazol-4<i>t</i>-yl)-pentanoic acid 7553-43-7 C10H16N2O5S
5-((3a<i>S</i>)-2,5,5-trioxo-(3a<i>r</i>,6a<i>c</i>)-octahydro-5λ<sup>6</sup>-thieno[3,4-<i>d</i>]imidazol-4<i>t</i>-yl)-pentanoic acid
—— N-(9-((2R,6S)-6-(hydroxymethyl)-4-tritylmorpholin-2-yl)-6-oxo-6,9-dihydro-1H-purin-2-yl)isobutyramide 956139-24-5 C33H34N6O4
N-(9-((2R,6S)-6-(hydroxymethyl)-4-tritylmorpholin-2-yl)-6-oxo-6,9-dihydro-1H-purin-2-yl)isobutyramide
—— (S)-Piperidine-3-carboxylic acid ethyl ester; compound with (2R,3R)-2,3-dihydroxy-succinic acid 83602-38-4 C4H6O6*C8H15NO2
(S)-Piperidine-3-carboxylic acid ethyl ester; compound with (2R,3R)-2,3-dihydroxy-succinic acid
—— <i>N</i>'-(3,5-dibromo-pyrazin-2-yl)-<i>N</i>,<i>N</i>-dimethyl-formamidine 60450-47-7 C7H8Br2N4
<i>N</i>'-(3,5-dibromo-pyrazin-2-yl)-<i>N</i>,<i>N</i>-dimethyl-formamidine
—— tert-butyl (3,3-bis(hydroxymethyl)cyclobutyl)carbamate 1639838-86-0 C11H21NO4
tert-butyl (3,3-bis(hydroxymethyl)cyclobutyl)carbamate