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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
—— (2-(3,4-dihydroisoquinolin-2(1H)-yl)phenyl)methanamine 937599-97-8 C16H18N2
(2-(3,4-dihydroisoquinolin-2(1H)-yl)phenyl)methanamine
—— methyl (S)-(-)-2,3,4,9-tetrahydro-1H-pyrido<3,4-b>indole-3-carboxylate hydrochloride 83159-19-7 C13H14N2O2*ClH
methyl (S)-(-)-2,3,4,9-tetrahydro-1H-pyrido<3,4-b>indole-3-carboxylate hydrochloride
—— (Trans,Trans)-4-Propyl-[1,1-Bicyclohexyl]-4-Carboxylic Acid 65355-32-0 C16H28O2
(Trans,Trans)-4-Propyl-[1,1-Bicyclohexyl]-4-Carboxylic Acid
—— (E)-3-(dimethylamino)-1-mesitylprop-2-en-1-one 78830-43-0 C14H19NO
(E)-3-(dimethylamino)-1-mesitylprop-2-en-1-one
—— methyl 2-(1H-4-bromoindol-3-yl)-2-oxoacetate 425640-16-0 C11H8BrNO3
methyl 2-(1H-4-bromoindol-3-yl)-2-oxoacetate
—— ethyl 2,2-dimethyl-2H-pyrano[2,3-b]pyridine-6-carboxylate 260402-24-2 C13H15NO3
ethyl 2,2-dimethyl-2H-pyrano[2,3-b]pyridine-6-carboxylate
—— Bis-(dibenzo<d,f>-1,3,2λ<sup>3</sup>-dioxaphosphepino)-2,2'-dioxobiphenyl 122605-42-9 C36H24O6P2
Bis-(dibenzo<d,f>-1,3,2λ<sup>3</sup>-dioxaphosphepino)-2,2'-dioxobiphenyl
—— spliceostatin A 391611-36-2 C28H43NO8
spliceostatin A
—— 3-amino-quinolin-4-ol; hydrochloride 129377-66-8 C9H8N2O*ClH
3-amino-quinolin-4-ol; hydrochloride
—— 2,2-difluoro-N-[(1R,2S)-3-methyl-1-{[1-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-1H-indazol-5-yl]oxy}-1-phenylbutan-2-yl]propanamide 1893415-00-3 C27H28F2N4O3
2,2-difluoro-N-[(1R,2S)-3-methyl-1-{[1-(1-methyl-6-oxo-1,6-dihydropyridin-3-yl)-1H-indazol-5-yl]oxy}-1-phenylbutan-2-yl]propanamide
—— Δ<sup>5,7</sup>-Pregnen-3,20-diethylenketal 5488-51-7 C25H36O4
Δ<sup>5,7</sup>-Pregnen-3,20-diethylenketal
—— 1-(benzyloxycarbonyl)-1,4,7,10-tetraazacyclododecane 331230-41-2 C16H26N4O2
1-(benzyloxycarbonyl)-1,4,7,10-tetraazacyclododecane
—— ethyl 7-oxo-4H-pyrazolo[1,5-a]pyrimidine-6-carboxylate 29274-18-8 C9H9N3O3
ethyl 7-oxo-4H-pyrazolo[1,5-a]pyrimidine-6-carboxylate
—— Ethyl 7-hydroxypyrazolo[1,5-a]pyrimidine-6-carboxylate 43024-61-9 C9H9N3O3
Ethyl 7-hydroxypyrazolo[1,5-a]pyrimidine-6-carboxylate
—— 5-METHYLPYRAZOLO[1,5-A]PYRIMIDIN-7-OL 16082-26-1 C7H7N3O
5-METHYLPYRAZOLO[1,5-A]PYRIMIDIN-7-OL
—— methyl benzo[b]thiophene-6-carboxylate 1423-65-0 C10H8O2S
methyl benzo[b]thiophene-6-carboxylate
—— 3-bromo-4,5,6,7-tetrahydro-benzo[b]thiophene-7-one 274925-56-3 C8H7BrOS
3-bromo-4,5,6,7-tetrahydro-benzo[b]thiophene-7-one
—— tert-butyl N-[[2-(chloromethyl)-1-(4,4,4-trifluorobutyl)-1H-1,3-benzodiazol-5-yl]methyl]carbamate 1243325-71-4 C18H23ClF3N3O2
tert-butyl N-[[2-(chloromethyl)-1-(4,4,4-trifluorobutyl)-1H-1,3-benzodiazol-5-yl]methyl]carbamate
—— 2-[2-(4-chlorophenoxy)ethoxy]-5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidine 1609980-39-3 C15H15ClN4O2
2-[2-(4-chlorophenoxy)ethoxy]-5,7-dimethyl-[1,2,4]triazolo[1,5-a]pyrimidine
—— 4,5-dichloro-1H-indole-2-carboxylic acid 231295-84-4 C9H5Cl2NO2
4,5-dichloro-1H-indole-2-carboxylic acid
—— 4-Ethyl-5-hydroxypentanoic acid lactone 73805-43-3 C7H12O2
4-Ethyl-5-hydroxypentanoic acid lactone
—— (1-methyl-1H-indol-6-yl)boronic acid 346585-03-3 C9H10BNO2
(1-methyl-1H-indol-6-yl)boronic acid
—— 3-bromo-6-chlorocarbazole 51501-58-7 C12H7BrClN
3-bromo-6-chlorocarbazole
—— tert-butyl 4-(prop-2-yn-1-yloxy)piperidine-1-carboxylate 1219827-56-1 C13H21NO3
tert-butyl 4-(prop-2-yn-1-yloxy)piperidine-1-carboxylate
—— 6-Cyanbenzo<b>thiophen-2-carbonsaeure-ethylester 105191-16-0 C12H9NO2S
6-Cyanbenzo<b>thiophen-2-carbonsaeure-ethylester
—— 5-bromo-3-iodo-1H-pyrazolo[3,4-c]pyridine 1357947-08-0 C6H3BrIN3
5-bromo-3-iodo-1H-pyrazolo[3,4-c]pyridine
—— 6-bromo-8-fluoro-3,4-dihydro-1H-quinolin-2-one 1194459-25-0 C9H7BrFNO
6-bromo-8-fluoro-3,4-dihydro-1H-quinolin-2-one
—— 3-Ethylenolether von Androst-4-en-3.17-dion 972-46-3 C21H30O2
3-Ethylenolether von Androst-4-en-3.17-dion
—— N-methylquinoxalin-6-amine 1338986-47-2 C9H9N3
N-methylquinoxalin-6-amine
—— (+/-)-<i>cis</i>-octahydro-isoquinolin-4a-ol; hydrochloride 81562-78-9 C9H17NO*ClH
(+/-)-<i>cis</i>-octahydro-isoquinolin-4a-ol; hydrochloride
—— diethyl cyclohexane 1,3-dicarboxylate 72903-26-5 C12H20O4
diethyl cyclohexane 1,3-dicarboxylate
—— N-(9H-fluoren-9-ylmethoxycarbonyl)-3-O-(2-acetamido-2-deoxy-α-D-galactopyranosyl)-L-threonine allyl ester 301843-65-2 C30H36N2O10
N-(9H-fluoren-9-ylmethoxycarbonyl)-3-O-(2-acetamido-2-deoxy-α-D-galactopyranosyl)-L-threonine allyl ester
—— 2,6-dimethylimidazo[2,1-b]thiazole-5-carboxylic acid 1007875-19-5 C8H8N2O2S
2,6-dimethylimidazo[2,1-b]thiazole-5-carboxylic acid
—— (E)-3-(benzo[d][1,3]dioxol-5-yl)-N-propylacrylamide 116591-96-9 C13H15NO3
(E)-3-(benzo[d][1,3]dioxol-5-yl)-N-propylacrylamide
—— (2E)-2-(pyridin-2-ylhydrazinylidene)naphthalen-1-one 10335-31-6 C15H11N3O
(2E)-2-(pyridin-2-ylhydrazinylidene)naphthalen-1-one
—— Bicyclo[4.1.0]heptan-2-amine 78293-48-8 C7H13N
Bicyclo[4.1.0]heptan-2-amine
—— 1-methyl-4-(4-nitro-1H-pyrazol-1-yl)piperidine 1201935-35-4 C9H14N4O2
1-methyl-4-(4-nitro-1H-pyrazol-1-yl)piperidine
—— ethyl {4-amino-3-[(3-chloro-5-cyanophenyl)oxy]-2-fluorophenyl}acetate 770719-11-4 C17H14ClFN2O3
ethyl {4-amino-3-[(3-chloro-5-cyanophenyl)oxy]-2-fluorophenyl}acetate
—— (1-Benzyl-5-ethenyl-1-azoniabicyclo[2.2.2]octan-2-yl)-(6-methoxyquinolin-4-yl)methanol;chloride 77481-82-4 C27H31ClN2O2
(1-Benzyl-5-ethenyl-1-azoniabicyclo[2.2.2]octan-2-yl)-(6-methoxyquinolin-4-yl)methanol;chloride
—— 1,1-dicyano-4-(N,N-dimethylamino)-2-methoxy-1,3-butadiene 95689-38-6 C9H11N3O
1,1-dicyano-4-(N,N-dimethylamino)-2-methoxy-1,3-butadiene
—— 1-purin-9-yl-ξ-<i>D</i>-1-deoxy-ribofuranose 550-33-4 C10H12N4O4
1-purin-9-yl-ξ-<i>D</i>-1-deoxy-ribofuranose
—— 5-methyl-4,5,6,7-tetrahydro-1H-indole 128277-88-3 C9H13N
5-methyl-4,5,6,7-tetrahydro-1H-indole
—— (8R,9R,13S,14R,17R)-13-ethyl-17-ethynyl-17-hydroxy-1,2,4,6,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one 1095-74-5 C21H28O2
(8R,9R,13S,14R,17R)-13-ethyl-17-ethynyl-17-hydroxy-1,2,4,6,7,8,9,11,12,14,15,16-dodecahydrocyclopenta[a]phenanthren-3-one
—— phenyl 2-deoxy-1-thio-2-(2,2,2-trichloroethoxycarbonylamino)-β-D-galactopyranoside 868230-98-2 C15H18Cl3NO6S
phenyl 2-deoxy-1-thio-2-(2,2,2-trichloroethoxycarbonylamino)-β-D-galactopyranoside
—— 6-chloro-2-(chloromethyl)thiazolo[5,4-b]pyridine 1256478-41-7 C7H4Cl2N2S
6-chloro-2-(chloromethyl)thiazolo[5,4-b]pyridine
—— 5,5-dimethyl-1,3,2-dioxathiane-2,2-dioxide 1755-97-1 C5H10O4S
5,5-dimethyl-1,3,2-dioxathiane-2,2-dioxide
—— 6-bromo-2-(piperidin-1-yl)quinoline 1637483-38-5 C14H15BrN2
6-bromo-2-(piperidin-1-yl)quinoline
—— cis-4-phenyl-L-proline hydrochloride 82087-67-0 C11H13NO2*ClH
cis-4-phenyl-L-proline hydrochloride
—— macrosphelide A 172923-77-2 C16H22O8
macrosphelide A
—— 2,3,4,6-Tetra-O-benzyl 1-O-p-nitrobenzoyl D-glucopyranoside 54423-54-0 C41H39NO9
2,3,4,6-Tetra-O-benzyl 1-O-p-nitrobenzoyl D-glucopyranoside