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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
—— 1-methylethylpiperazine dihydrochloride 88569-66-8 C7H16N2*2ClH
1-methylethylpiperazine dihydrochloride
—— (2,2-dimethyl-1,3-dithiolan-4-yl)methanol 5694-47-3 C6H12OS2
(2,2-dimethyl-1,3-dithiolan-4-yl)methanol
—— 6-Chlor-4-methyl-2-butylpyrimidin 848499-42-3 C9H13ClN2
6-Chlor-4-methyl-2-butylpyrimidin
—— 5,6-dimethyl-2-(pyridin-3-yl)-1H-benzo[d]imidazole 6507-10-4 C14H13N3
5,6-dimethyl-2-(pyridin-3-yl)-1H-benzo[d]imidazole
—— (E)-dimethyl hex-2-enedioate 70353-99-0 C8H12O4
(E)-dimethyl hex-2-enedioate
—— 4-chloro-7H-pyrrolo[2, 3-c]pyridazine 1269823-02-0 C6H4ClN3
4-chloro-7H-pyrrolo[2, 3-c]pyridazine
—— 6-chloro-7-fluoro-1H-indole 259860-04-3 C8H5ClFN
6-chloro-7-fluoro-1H-indole
—— 2-(4-chlorophenyl)quinoxaline 17286-63-4 C14H9ClN2
2-(4-chlorophenyl)quinoxaline
—— tri(pyridin-3-yl)phosphine 94345-02-5 C15H12N3P
tri(pyridin-3-yl)phosphine
—— 1-(2-Chloroethyl)-4-[3-(trifluoromethyl)phenyl]piperazine dihydrochloride 57061-71-9 C13H18Cl3F3N2
1-(2-Chloroethyl)-4-[3-(trifluoromethyl)phenyl]piperazine dihydrochloride
—— 6-(4-methoxyphenyl)-2-methylimidazo<1,2-a>pyrazin-3(7H)-one hydrochloride 128322-44-1 C14H13N3O2*ClH
6-(4-methoxyphenyl)-2-methylimidazo<1,2-a>pyrazin-3(7H)-one hydrochloride
—— 3-(2-indolyl)indole 27393-85-7 C16H12N2
3-(2-indolyl)indole
—— ((2S,3R)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-4-phenylbutanoyl)-L-leucine 87304-15-2 C21H32N2O6
((2S,3R)-3-((tert-butoxycarbonyl)amino)-2-hydroxy-4-phenylbutanoyl)-L-leucine
—— (+)-5-bromo-1-methyl-2-trityliso-indoline 194805-14-6 C28H24BrN
(+)-5-bromo-1-methyl-2-trityliso-indoline
—— 5-(3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)oxazole 1403469-16-8 C15H18BNO3
5-(3-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)oxazole
—— α-(4-pyridyl-1-oxide)-N-tert-butyl-nitrone 66893-81-0 C10H14N2O2
α-(4-pyridyl-1-oxide)-N-tert-butyl-nitrone
—— 1H-pyrazolo[1,5-a]pyridin-5-one 156969-42-5 C7H6N2O
1H-pyrazolo[1,5-a]pyridin-5-one
—— ethyl 2-(6′-cyan-5′-oxo-3′,5′-dihydro-2′H-spiro[[1,3]dioxolane-2,1′-indolizine]-7′-yl)acetate 58610-65-4 C15H16N2O5
ethyl 2-(6′-cyan-5′-oxo-3′,5′-dihydro-2′H-spiro[[1,3]dioxolane-2,1′-indolizine]-7′-yl)acetate
—— (S)-N-methyl-8-(1-((2'-methyl-4',6'-dideutero-[4,5'-bipyrimidin]-6-yl)amino)propan-2-yl)quinoline-4-carboxamide 1476074-39-1 C23H23N7O
(S)-N-methyl-8-(1-((2'-methyl-4',6'-dideutero-[4,5'-bipyrimidin]-6-yl)amino)propan-2-yl)quinoline-4-carboxamide
—— benzyl 2,3,4-tri-O-benzyl-α-D-mannopyranoside 57783-76-3 C34H36O6
benzyl 2,3,4-tri-O-benzyl-α-D-mannopyranoside
—— 2-Amino-4-chloro-6-hydroxypyrimidine monohydrate 410530-71-1 C4H4ClN3O*H2O
2-Amino-4-chloro-6-hydroxypyrimidine monohydrate
—— Ethyl 4-(2-methylbut-3-yn-2-ylamino)benzoate 171898-68-3 C14H17NO2
Ethyl 4-(2-methylbut-3-yn-2-ylamino)benzoate
—— Pyrimido[4,5-g]quinazoline 260-75-3 C10H6N4
Pyrimido[4,5-g]quinazoline
—— (6R)-L-erythro-5,6,7,8-tetrahydrobiopterin 62989-33-7 C9H15N5O3
(6R)-L-erythro-5,6,7,8-tetrahydrobiopterin
—— 5-amino-1,3-bis-n-propyluracil 51038-42-7 C10H17N3O2
5-amino-1,3-bis-n-propyluracil
—— ethyl 4-((3-nitropyridin-2-yl)amino)benzoate 78750-62-6 C14H13N3O4
ethyl 4-((3-nitropyridin-2-yl)amino)benzoate
—— trans-4-phenylcyclohexanecarboxylic acid 1466-73-5 C13H16O2
trans-4-phenylcyclohexanecarboxylic acid
—— 3-chloro-1-trifluoromethanesulfonyloxybenzene 86364-03-6 C7H4ClF3O3S
3-chloro-1-trifluoromethanesulfonyloxybenzene
—— diketene acetal (3,9-bis(ethylidene)-2,4,8,10-tetraoxaspiro<5,5>undecane) 65967-52-4 C11H16O4
diketene acetal (3,9-bis(ethylidene)-2,4,8,10-tetraoxaspiro<5,5>undecane)
—— 4-aminopiperidine dihydrochloride 35621-01-3 C5H12N2*2ClH
4-aminopiperidine dihydrochloride
—— (4-methoxyphenyl)(4-(trifluoromethyl)phenyl)methanone 6185-76-8 C15H11F3O2
(4-methoxyphenyl)(4-(trifluoromethyl)phenyl)methanone
—— 4-(dimethylamino)-1,1-dimethoxy-but-3-en-2-one 67751-23-9 C8H15NO3
4-(dimethylamino)-1,1-dimethoxy-but-3-en-2-one
—— 2-Amino-3-(2-fluorbenzoyl)-thiophen 40017-70-7 C11H8FNOS
2-Amino-3-(2-fluorbenzoyl)-thiophen
—— 1-phenyl-1H-pyrazole 670-96-2 C9H8N2
1-phenyl-1H-pyrazole
—— monoallyl diglycidyl isocyanurate 69731-45-9 C12H15N3O5
monoallyl diglycidyl isocyanurate
—— retro-2 1429192-00-6 C19H16N2OS
retro-2
—— 2-(2,3-Dichlorobenzylidene)-3-oxobutanoic acid methyl ester 74073-22-6 C12H10Cl2O3
2-(2,3-Dichlorobenzylidene)-3-oxobutanoic acid methyl ester
—— 5-bromo-2-(methoxymethyl)pyridine 1000787-43-8 C7H8BrNO
5-bromo-2-(methoxymethyl)pyridine
—— 1-((tert-butoxycarbonyl)(methyl)amino)cyclopropane-1-carboxylic acid 119145-87-8 C10H17NO4
1-((tert-butoxycarbonyl)(methyl)amino)cyclopropane-1-carboxylic acid
—— 4,5-dimethylthiophene-2-sulfonyl chloride 74616-28-7 C6H7ClO2S2
4,5-dimethylthiophene-2-sulfonyl chloride
—— 290-37-9 C4H4N2
—— ethyl 5-chloro-7-morpholinopyrazolo[1,5-a]pyrimidine-2-carboxylate 1232224-64-4 C13H15ClN4O3
ethyl 5-chloro-7-morpholinopyrazolo[1,5-a]pyrimidine-2-carboxylate
—— (S)-3-hydroxyhexanoic acid 66997-60-2 C6H12O3
(S)-3-hydroxyhexanoic acid
—— 2,6-Dimethoxy-3,5-pyridinediamine HCl 56216-28-5 C7H15Cl4N3O2
2,6-Dimethoxy-3,5-pyridinediamine HCl
—— 4-hydroxyethylpiperazine hydrochloride 5712-71-0 C6H14N2O*ClH
4-hydroxyethylpiperazine hydrochloride
—— (3Z)-3-[[4-[(4,6-dimethylpyrimidin-2-yl)sulfamoyl]phenyl]hydrazinylidene]-6-oxocyclohexa-1,4-diene-1-carboxylic acid 2315-08-4 C19H17N5O5S
(3Z)-3-[[4-[(4,6-dimethylpyrimidin-2-yl)sulfamoyl]phenyl]hydrazinylidene]-6-oxocyclohexa-1,4-diene-1-carboxylic acid
—— triphenylborane-pyridine 971-66-4 C23H20BN
triphenylborane-pyridine
—— [(2R)-2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methyl methanesulfonate 67914-86-7 C14H15Cl2N3O5S
[(2R)-2-(2,4-dichlorophenyl)-2-(1,2,4-triazol-1-ylmethyl)-1,3-dioxolan-4-yl]methyl methanesulfonate
—— t-butyl 16-bromohexadecanoate 865200-89-1 C20H39BrO2
t-butyl 16-bromohexadecanoate
—— 2-methyl-3,5,7,8-tetrahydro-4H-thiopyrano[4,3-d]pyrimidin-4-one 284028-90-6 C8H10N2OS
2-methyl-3,5,7,8-tetrahydro-4H-thiopyrano[4,3-d]pyrimidin-4-one