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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
—— 3-(p-methylphenyl)pyridine 90395-49-6 C12H11N
3-(p-methylphenyl)pyridine
—— 2-nitro-4-(3-pyridyl)toluene 4373-62-0 C12H10N2O2
2-nitro-4-(3-pyridyl)toluene
—— 3-(quinolin-3-yl)acrylic acid 67752-27-6 C12H9NO2
3-(quinolin-3-yl)acrylic acid
—— [2,4-17O2]uracil 66-22-8 C4H4N2O2
[2,4-17O2]uracil
—— 2-bromo-4-isopropoxy-1-methylbenzene 1254062-68-4 C10H13BrO
2-bromo-4-isopropoxy-1-methylbenzene
—— 2-isopropoxy-5-methyl-4-(piperidin-4-yl)aniline dihydrochloride 1380575-45-0 C15H24N2O*2ClH
2-isopropoxy-5-methyl-4-(piperidin-4-yl)aniline dihydrochloride
—— 1-(2-bromoethyl)-3-(prop-1-en-2-yl)-1H-benzo[d]imidazol-2(3H)-one 136081-17-9 C12H13BrN2O
1-(2-bromoethyl)-3-(prop-1-en-2-yl)-1H-benzo[d]imidazol-2(3H)-one
—— 2,7-diamino-6-(2,6-dichlorophenyl)-pyrido[2,3-d]-pyrimidine 26752-70-5 C13H9Cl2N5
2,7-diamino-6-(2,6-dichlorophenyl)-pyrido[2,3-d]-pyrimidine
—— methyl (S)-3-(4-(bis(2-hydroxyethyl)amino)phenyl)-2-((tert-butoxycarbonyl)amino)propanoate 1217651-06-3 C19H30N2O6
methyl (S)-3-(4-(bis(2-hydroxyethyl)amino)phenyl)-2-((tert-butoxycarbonyl)amino)propanoate
—— norbornane-2,3-diol 14440-78-9 C7H12O2
norbornane-2,3-diol
—— melphalan methyl ester hydrochloride 62978-52-3 C14H20Cl2N2O2*ClH
melphalan methyl ester hydrochloride
—— 2-morpholin-4-yl-4-oxo-4H-chromen-8-yl trifluoromethanesulfonate 351002-11-4 C14H12F3NO6S
2-morpholin-4-yl-4-oxo-4H-chromen-8-yl trifluoromethanesulfonate
—— 1-(2-bromopyridin-4-yl)ethanone 111043-06-2 C7H6BrNO
1-(2-bromopyridin-4-yl)ethanone
—— N,N-bis(diphenylphosphino)isopropylamine 60981-68-2 C27H27NP2
N,N-bis(diphenylphosphino)isopropylamine
—— 2-(trimethylstannyl)thiophene 37496-13-2 C7H12SSn
2-(trimethylstannyl)thiophene
—— 7-hydroxy-2-(p-tolyl)-4H-chromen-4-one 78298-69-8 C16H12O3
7-hydroxy-2-(p-tolyl)-4H-chromen-4-one
—— Lithium-8-chinolinolat 25387-93-3 C9H6NO*Li
Lithium-8-chinolinolat
—— (±)-(1R,2R,3aS,8bS)-2,3,3a,8b-tetrahydro-2-hydroxy-1-[(E)-(3S,4RS)-3-hydroxy-4-methyl-1-octen-6-ynyl]-1H-cyclopenta[b]-benzofuran-5-butanoic acid 88430-50-6 C24H30O5
(±)-(1R,2R,3aS,8bS)-2,3,3a,8b-tetrahydro-2-hydroxy-1-[(E)-(3S,4RS)-3-hydroxy-4-methyl-1-octen-6-ynyl]-1H-cyclopenta[b]-benzofuran-5-butanoic acid
—— 4-(1-(R)-t-butoxycarbonyl-1-aminomethyl)phenol 501692-32-6 C12H17NO3
4-(1-(R)-t-butoxycarbonyl-1-aminomethyl)phenol
—— N,N'-dibenzylviologen dichloride 1102-19-8 C24H22N2*2Cl
N,N'-dibenzylviologen dichloride
—— 2,3,4-tri-O-benzyl-D-glucopyranosideuronic acid benzyl ester 4539-78-0 C34H34O7
2,3,4-tri-O-benzyl-D-glucopyranosideuronic acid benzyl ester
—— (1R,8S,9S)‐bicyclo[6.1.0]non‐4‐yn‐9‐ylmethanol 1263166-90-0 C10H14O
(1R,8S,9S)‐bicyclo[6.1.0]non‐4‐yn‐9‐ylmethanol
—— 1-ethyl-3-methylimidazolium perchlorate 65039-04-5 C6H11N2*ClO4
1-ethyl-3-methylimidazolium perchlorate
—— 1,4-dihydro-1-beta-D-ribofuranosyl-3-pyridinecarboxamide 19132-12-8 C11H16N2O5
1,4-dihydro-1-beta-D-ribofuranosyl-3-pyridinecarboxamide
—— (+/-)-9,10-dihydroxy-3<i>c</i>-isobutyl-(11b<i>r</i>)-1,3,4,6,7,11b-hexahydro-pyrido[2,1-<i>a</i>]isoquinolin-2-one 89929-27-1 C17H23NO3
(+/-)-9,10-dihydroxy-3<i>c</i>-isobutyl-(11b<i>r</i>)-1,3,4,6,7,11b-hexahydro-pyrido[2,1-<i>a</i>]isoquinolin-2-one
—— ethyl ester of 1-cyclopropyl-6-nitro-4-oxo-7-chloro-1,4-dihydroquinoline-3-carboxylic acid 127625-17-6 C15H13ClN2O5
ethyl ester of 1-cyclopropyl-6-nitro-4-oxo-7-chloro-1,4-dihydroquinoline-3-carboxylic acid
—— 3,3'-di-tert-butyl-2'-(4,8-di-tert-butyl-2,10-dimethoxydibenzo[d,f][1,3,2]dioxaphosphepin-6-yloxy)-5,5'-dimethoxybiphenyl-2-ol 108609-96-7 C44H57O8P
3,3'-di-tert-butyl-2'-(4,8-di-tert-butyl-2,10-dimethoxydibenzo[d,f][1,3,2]dioxaphosphepin-6-yloxy)-5,5'-dimethoxybiphenyl-2-ol
—— 1-(n-hexyl)-1,2-dicarba-closo-dodecaborane 20740-05-0 C8H24B10
1-(n-hexyl)-1,2-dicarba-closo-dodecaborane
—— 4,6-dichloro-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazolo[3,4-d]pyrimidine 1037479-62-1 C10H10Cl2N4O
4,6-dichloro-1-(tetrahydro-2H-pyran-2-yl)-1H-pyrazolo[3,4-d]pyrimidine
—— N<sup>2'</sup>-deacetyl-N<sup>2'</sup>-[3-(methyldithio)-1-oxopropyl]maytansine 138148-68-2 C36H50ClN3O10S2
N<sup>2'</sup>-deacetyl-N<sup>2'</sup>-[3-(methyldithio)-1-oxopropyl]maytansine
—— 1-Ethyl-3-hydroxy-5,6,7,8-tetrahydro-isoquinoline-4-carbonitrile 53661-27-1 C12H14N2O
1-Ethyl-3-hydroxy-5,6,7,8-tetrahydro-isoquinoline-4-carbonitrile
—— 3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt 1321816-57-2 C5H14NO*C22H14F3N2O7S
3-[2-fluoro-5-(2,3-difluoro-6-methoxybenzyloxy)-4-methoxyphenyl]-2,4-dioxo-1,2,3,4-tetrahydrothieno[3,4-d]pyrimidine-5-carboxylic acid choline salt
—— 2,2,2-Trifluoroethanol sodium salt 420-87-1 C2H3F3NaO
2,2,2-Trifluoroethanol sodium salt
—— 2-hydroxy-6-(methoxymethoxy)benzaldehyde 84290-49-3 C9H10O4
2-hydroxy-6-(methoxymethoxy)benzaldehyde
—— 2',3',5'-tri-O-benzoylinosine 6741-88-4 C31H24N4O8
2',3',5'-tri-O-benzoylinosine
—— dihydrocholesterol 80-97-7 C27H48O
dihydrocholesterol
—— (5α)-cholestan-3β-ol 80-97-7 C27H48O
(5α)-cholestan-3β-ol
—— (5β)-cholestan-3α-ol 80-97-7 C27H48O
(5β)-cholestan-3α-ol
—— (5β)-cholestan-3β-ol 80-97-7 C27H48O
(5β)-cholestan-3β-ol
—— (5α)-cholestan-3α-ol 80-97-7 C27H48O
(5α)-cholestan-3α-ol
—— 2',3'-anhydroinosine 31766-13-9 C10H10N4O4
2',3'-anhydroinosine
—— diethyl 1,4-dioxaspiro[4.5]decane-8,8-dicarboxylate 1256546-71-0 C14H22O6
diethyl 1,4-dioxaspiro[4.5]decane-8,8-dicarboxylate
—— 2-chloro-5-vinylthiophene 105414-82-2 C6H5ClS
2-chloro-5-vinylthiophene
—— pneumocandin B<sub>0</sub> 135575-42-7 C50H80N8O17
pneumocandin B<sub>0</sub>
—— 3,3,20,20-bis(ethylene-dioxy)-17α-hydroxy-19-norpregna-5(10),9(11)-diene 54201-84-2 C24H34O5
3,3,20,20-bis(ethylene-dioxy)-17α-hydroxy-19-norpregna-5(10),9(11)-diene
—— 2-((10S,13S)-10,13-dimethyl-3-oxo-6,7,8,10,12,13,14,15-octahydro-3H-cyclopenta[a]phenanthren-17-yl)-2-oxoethyl acetate 37413-91-5 C23H26O4
2-((10S,13S)-10,13-dimethyl-3-oxo-6,7,8,10,12,13,14,15-octahydro-3H-cyclopenta[a]phenanthren-17-yl)-2-oxoethyl acetate
—— Fmoc-Gly-NH2 115057-37-9 C17H16N2O3
Fmoc-Gly-NH2
—— 10-nitro-(20S)-camptothecin 86639-62-5 C20H15N3O6
10-nitro-(20S)-camptothecin
—— 1-cyclopropylprop-2-en-1-ol 24897-34-5 C6H10O
1-cyclopropylprop-2-en-1-ol
—— ethyl 2-chloro-4-(methylsulfanyl)pyrimidine-5-carboxylate 643086-93-5 C8H9ClN2O2S
ethyl 2-chloro-4-(methylsulfanyl)pyrimidine-5-carboxylate